International Journal of Applied Pharmaceutics
International Journal of Applied Pharmaceutics (Int J App Pharm) is a peer-reviewed, bimonthly (onward March 2017) open-access journal devoted to excellence and research in pharmaceutics. This journal publishes original research work that contributes significantly to adding scientific knowledge in conventional dosage forms, formulation development and characterization, controlled and novel drug delivery, biopharmaceutics, pharmacokinetics, molecular drug design, polymer-based-drug delivery, nanotechnology, nanocarrier-based drug delivery, novel routes and modes of delivery; responsive delivery systems, prodrug design, development and characterization of the targeted drug delivery systems, ligand carrier interactions, etc. Studies on analytical method developments and physical pharmacy are part of the journal's scope. Furthermore, pharmacological and toxicological studies of Active Pharmaceutical Ingredients (APIs) and their formulations are considered. The journal publishes original research work either as an Original Article or a Short Communication. Review Articles on a current topic in the mentioned fields are also considered for publication in the journal. Special issues on dedicated subjects or conference proceedings within the broader stated scope of the journal shall be considered for publication. Articles in the concerned may be permitted beyond the scope but on the merit of quality and when within the theme of the conference/special issue. Onward 2021, for instant and swift access to current applied research that may have an impact on the subjects of the journal's scope, including allied subjects having an impact on mass human/living population, especially the cases of endemic/ pandemics (like COVID-19 and H1N1, others), are considered. International Journal of Applied Pharmaceutics is a (Q2) Scopus-indexed journal. Abstracting and Indexing Google Scholar, Scopus [Q2], EMBASE, SCI mago (SJR), CNKI (China Knowledge Resource Integrated Database), CAS, CASSI (American Chemical Society), Open-J-Gate, OAI, LOCKKS, OCLC (World Digital Collection Gateway), UIUC.
Proceedings of MPCST Sponsored International Conference On "The Future of Drug Safety: From Clinical Trials to Real World
Copyright (c) 2025 Abstract book https://creativecommons.org/licenses/by/4.0
DEVELOPMENT AND OPTIMIZATION OF MESOPOROUS SILICA NANOPARTICLE LOADED HYDROGEL OF ALLICIN FOR WOUND HEALING
Objective: The objective of this study was to develop and optimize a mesoporous silica nanoparticle (MSN)-loaded hydrogel formulation of allicin to enhance its stability, sustained release, and skin permeation for effective wound healing. Methods: Allicin was characterized through organoleptic, UV, solubility, FTIR, and DSC studies. MCM-41 MSNs were selected as carriers due to superior encapsulation efficiency and solubility enhancement. MSN-loaded hydrogels were formulated using a factorial design and evaluated for physicochemical properties, in vitro release, ex vivo permeation using Franz diffusion cells, and statistical optimization via ANOVA. Drug release kinetics were modeled using Zero-order, First-order, Higuchi, and Korsmeyer–Peppas equations. Accelerated stability studies were performed under ICH conditions for six months. Results: Hydrogel formulations were stable, skin-compatible, and demonstrated uniform drug content (97.68–98.92%). In vitro release showed biphasic profiles with optimized formulations GF7 (94.26±4.18%) and GF5 (93.85±4.06%) achieving maximum release at 12 h. Ex vivo permeation confirmed superior performance of GF7 (95.42±3.65%) and GF5 (94.74±3.45%) with high flux (34.56 and 33.96 µg/cm²/h) and permeability coefficients (1.73×10⁻³ and 1.70×10⁻³ cm/h). ANOVA demonstrated significant influence of Carbopol and propylene glycol, and validation of optimized batch GF5 confirmed high model reliability (desirability 0.980). Release followed first-order kinetics (R² = 0.9789) with anomalous diffusion. Stability studies showed minimal changes in pH, viscosity, spreadability, drug content, and permeation over six months. Conclusion: The MSN-based hydrogel system successfully enhanced allicin’s solubility, stability, sustained release, and skin permeation, offering a promising strategy for topical delivery of unstable phytoconstituents.
Copyright (c) 2025 GAURAVI SUNILRAO KHERDE, RAHUL DNYANESHWAR KHAIRE, VIKAS DAMU KUNDE https://creativecommons.org/licenses/by/4.0
PREPARATION AND OPTIMIZATION OF GEPIRONE HCL SR MATRIX TABLETS USING HPMC K100M AND POLYOX WSR N80
Objective: In adults, Gepirone Hydrochloride (HCl) is most commonly employed as a first-line treatment for Major Depressive Disorder (MDD). The elimination half-life of Gepirone HCl is approximately 5 h necessitates the development of sustained release formulation. In the current research, two polymers HPMC K100M and Polyox WSR N80 were used in combination by adopting a central composite design with an objective to minimize burst release and sustain drug release for 24 h. Methods: The SR matrix tablets of Gepirone HCl were prepared by wet granulation method. Optimization of Gepirone HCl SR matrix tablets was achieved through central composite design (CCD). The selected CQAs were concentration of polymer HPMC K100M in the range of 20 to 40 mg per tablet and concentration of Polyox WSR N80 in the range of 30 to 50 mg per tablet. Three responses selected for optimization vis-à-vis Q 1 (Cumulative percent drug release from SR matrix tablet in 1 h), t 50 (time taken for release of 50% of API) and Q 18 (Cumulative percent drug release from SR matrix tablet at 18 h). Results: Fourier Transform Infra Red (FT-IR) and Differential Scanning Calorimetry (DSC) study for the physical mixture of Gepirone HCl with HPMC K100M and Polyox WSR N80 in 1:1 ratio demonstrated compatibility. The granules exhibited improved flowability and compressibility. The optimized formulation (run 7) passed all the quality control tests for tablets. Scanning electron microscopy for tablet of run 7 exhibited a homogenous and porous gel network. In vitro dissolution study showed that the integration of two polymers HPMC K100M and Polyox WSR N80 were effective in minimizing the initial burst release, and sustained release of Gepirone HCl over 24 h. Conclusion: Hence, the development of a once-daily formulation aligns with modern patient-centric approaches in pharmaceutical design, catering to convenience and improving quality of life for patients requiring long-term therapy.
Copyright (c) 2025 ANJAN KUMAR, Dinesh Das, Ch Niranjan Patra https://creativecommons.org/licenses/by/4.0
BIOANALYTICAL METHOD DEVELOPMENT AND VALIDATION OF REMDESIVIR IN HUMAN PLASMA BY LC-MS/MS AS PER ICH M10 GUIDELINE
Objective: Remdesivir, an adenosine analogue prodrug widely used during Coronavirus disease 2019 (COVID-19) pandemic. In this research, the objective was to develop a cost-effective and robust bioanalytical method capable of accurately quantifying remdesivir in human clinical studies as per ICH M10 guideline. Methods: Development of a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method with electro spray ionisation (ESI) source primarily involved extensive chromatographic optimization trials. Among various tested columns, Waters Symmetry C18 (5 µm, 3.9 mm×150 mm) demonstrated most consistent and well-defined chromatographic response when used with a highly organic acidified mobile phase, achieving a short run time of 3 min. For extraction method optimization, multiple approaches were evaluated, with protein precipitation emerging as preferred technique with environmentally friendly reagent use. Results: Bioanalytical method validation was performed well as per ICH M10 (International Council for harmonisation of Technical Requirements for pharmaceuticals for Human Use) guidelines. The method demonstrated good linearity from 50-5000 ng/ml, with a correlation coefficient (R²) of 0.9978. The within-run and between-run precision for all quality control (QC) levels remained up to 6.65%, while accuracy ranged from 95.22-110.74%. Remdesivir was stable under freeze-thaw, auto sampler, bench top and long-term settings, with a percentage change of±15%. The paired t-test analysis revealed no significant difference between fresh and stability samples (p>0.1). Conclusion: Validated calibration range of 50–5000 ng/ml is suitable for bioanalysis of remdesivir in human clinical studies involving intravenous infusion, considering reported Cmax of approximately 2229 ng/ml. This study highlights the integration of advanced LC-MS/MS techniques for quantification of remdesivir using remdesivir D5 as an internal standard in human plasma.
Copyright (c) 2025 SUBHRANSHU PANDA, TUSHAR CHAVAN, RAVINDRA BHAVSAR https://creativecommons.org/licenses/by/4.0
DEVELOPMENT AND VALIDATION OF HPLC METHOD FOR THE DETERMINATION OF RESVERATROL IN BULK DOSAGE FORM, COMMERCIAL TABLET, AND MULTIWALLED CARBON NANOTUBES-BASED FORMULATION
Objective: Resveratrol (RES), a polyphenol, is a promising option to treat multiple diseases due to its anticancer, cardioprotective, anti-inflammatory, and antioxidant activities. The present study was designed to develop and validate a simple, precise, rapid and reproducible analytical method for the detection of RES in different formulations. Methods: A novel analytical technique was developed and validated for the detection of RES via ultrafast liquid chromatography utilizing C18 column. Methanol along with high-performance liquid chromatography (HPLC) grade water (40:60) was used as a mobile phase with a rate of flow of 0.8 ml/min. This technique has been validated following the International Conference for Harmonization (ICH) Q2 (R1) guidelines. The method's accuracy was determined through the percent recovery within the limit of 95 to 105%. Results: The method demonstrated linearity within the 2-10 µg/ml range, exhibiting a regression coefficient of 0.997. The precision of the method was indicated by the percentage RSD, which was recorded to be less than 2%. Limit of detection (LOD), and limit of quantification (LOQ) were found to be 1.6 µg/ml and 4.8 µg/ml, respectively. The proposed approach has been proved to be robust because the response did not significantly change due to a change in the rate of flow, along with the composition of the mobile phase. Conclusion: The results of the study demonstrated that the developed method has passed all the validation test parameters and can be applied for the estimation of RES in bulk dosage form, commercial tablet, and developed multiwalled carbon nanotube (MWCNTs)-based formulations.
Copyright (c) 2025 NEHA SHARMA, YACHANA MISHRA, NEELAM SHARMA, VIJAY MISHRA https://creativecommons.org/licenses/by/4.0
COMPUTATIONAL SCREENING OF NATURAL COMPOUNDS AS POTENTIAL AURORA A KINASE INHIBITORS FOR LEUKEMIA CANCER TREATMENT: A MULTI-STEP IN SILICO APPROACH
Objective: The overexpression of aurora a kinase is associated with leukaemia as it is an essential regulator of mitotic progression, rendering it a promising therapeutic target. This study employed a multi-step in silico strategy that incorporated computational screening, molecular docking, Density Functional Theory (DFT) analysis, free energy calculations (MM-GBSA), and Molecular Dynamics (MD) simulations to evaluate the potential of natural compounds as Aurora A kinase inhibitors. Methods: An initial virtual screening of 3,093 natural compounds from the Selleckchem library was performed. Drug-likeness was assessed using Lipinski’s Rule of Five, which filters compounds based on key pharmacokinetic parameters: molecular weight (≤ 500 Da), LogP (≤ 5), hydrogen bond donors (≤ 5), and hydrogen bond acceptors (≤ 10). A total of 2,045 compounds that satisfied all these criteria were selected for further analysis and bioactivity evaluation. Results: After ML-based QSAR screening, molecular docking identified 683 ligands with binding affinities of ≤-6.0 kcal/mol. Out of all natural compounds, PubChem CID: 94381 (Coumarin 7) and PubChem CID: 1830 (7-Iodo-7-deaza-D-guanosine) showed minimal RMSD (0.1-0.3 nm), and high hydrogen bonding (2-6 stable contacts) during the 100 ns MD simulations, suggesting stable binding within the aurora A kinase active site. The strong binding affinity of MM-GBSA was further validated by the binding free energy calculations, which showed favourable values of ΔG =-27.93 kcal/mol (94381) and -27.50 kcal/mol (1830). Conclusion: Further, with a dipole moment of 2.80 D, 1830 had great electrical stability, and the lowest HOMO-LUMO gap (-0.1580 eV/-0.1311 eV) was observed in 94381, according to DFT calculations, which indicated significant reactivity. Additionally, synthetic accessibility scores of 3.19 and 4.00, respectively, and iLOGP (integrative octanol–water partition coefficient) values of 2.46 (94381) and 1.57 (1830), both compounds showed ideal drug-like characteristics and may be developed further.
Copyright (c) 2025 johra khan https://creativecommons.org/licenses/by/4.0
BOX-BEHNKEN DESIGN-BASED DEVELOPMENT OF ECO-FRIENDLY RP-HPLC ANALYTICAL METHOD FOR THE QUANTIFICATION OF ERASTIN FROM THE MESOPOROUS SILICA NANOPARTICLES
Objective: Globally, cancer remains a major source of illness and mortality. Approximately 30% of initial glioblastomas and 80% of all malignant ones are gliomas. Erastin (ERT) is a small molecule that kills cancer cells through ferroptosis and treats brain cancer. The current work aims to optimize, establish, and validate a High-Performance Liquid Chromatography (HPLC) method with sufficient sensitivity and specificity to measure ERT in Mesoporous Silica Nanoparticles (MSNs). The HPLC method was optimized using the Design of Experiments (DoE) technique. The novelty of this project is the development of the DoE-based HPLC method for quantifying ERT from the MSNs. Methods: The Box-Behnken Design (BBD) was used for the method optimization, and buffer ratio, injection volume, buffer pH, and flow rate were used as the independent factors. The dependent variables were retention time (RT) of ERT, peak area of ERT, and tailing factor (TF) of ERT. The optimized chromatographic conditions were: buffer ratio of 80%, buffer pH 3.8, flow rate 0.9 ml/min, and injection volume 8 µl**. The established HPLC method was validated as per International Council for Harmonisation (ICH) Q2 (R1) recommendations. Results: The optimization of the HPLC method was done using BBD, and the desirability value was found to be 0.992. The established method showed good linearity (R2 = 0.9991) with a 12-500 ng/ml range, and LOD and LOQ were 2.71 ng and 6.25 ng, respectively. The Mesoporous Silica Nanoparticle (MSNs) matrix did not affect the specificity of our validated HPLC method for the analysis of ERT. Analysing the formulation's surface morphology helped confirm the synthesized MSNs. The proposed HPLC method was effectively used to calculate the medication loaded in the MSNs and to measure the amount of ERT entrapped. The % entrapment efficiency (EE) for ERT in MSNs was found to be 76.07±2.56%, and the % drug loading (DL) for ERT in MSNs was found to be 14±1.87%. The established HPLC method for estimating ERT was found to be environmentally friendly with an overall analytical greenness (AGREE) score of 0.6. Conclusion: The established HPLC method was developed, optimized, and validated as per ICH Q2 R1 guidelines. The HPLC method was found to be eco-friendly as per the AGREE analysis.
Copyright (c) 2025 ASHUTOSH GUPTA, RACHANA S. P., SUDHEER MOORKOTH, NAMDEV DHAS https://creativecommons.org/licenses/by/4.0
NEUROPROTECTIVE EFFECTS OF DONEPEZIL AND FLUOXETINE VIA GSK-3 PATHWAY IN A TRANSGENIC DROSOPHILA MODEL OF ALZHEIMER'S DISEASE: NEUROPSYCHIATRIC AND BEHAVIOURAL ANALYSIS
Objective: This study investigates the neuroprotective effects of Donepezil and Fluoxetine in a transgenic Drosophila melanogaster model of AD, with a specific focus on modulation of the GSK-3 signalling pathway. Methods: Transgenic Drosophila flies expressing the UAS-ELAV-GAL4 system were divided into four groups: (1) Normal, (2) Disease Control, (3) Donepezil 100 µM (DPZ), and (4) Fluoxetine 10 µM (FLX), treated for 21 d. Behavioural assays (negative geotaxis, open field) were conducted to assess locomotor function. Biochemical analyses, including oxidative stress markers (CAT, MDA, GSH) and neurotransmitters (dopamine, serotonin, acetylcholine), were measured. Immunohistochemistry was used to qualitatively assess the expression of Aβ, GSK-3, and neuroinflammatory cytokines (IL-6, IL-1β, TNF-α) in fly brains. Results: Transgenic Drosophila melanogaster expressing AD pathology exhibited elevated levels of oxidative stress markers, neurotransmitter deficits, and marked neuroinflammation. Donepezil and Fluoxetine significantly (p≤0.05) reduced MDA levels and restored CAT and GSH levels, indicating improved antioxidant defence. Both treatments also reversed reductions in dopamine, serotonin, and acetylcholine levels significantly (p≤0.05) when compared to the control group, suggesting neurochemical restoration. Immunohistochemistry revealed decreased Aβ, GSK-3, and pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) following treatment, with Fluoxetine demonstrating comparatively greater modulation. Histological analysis confirmed improved neuronal integrity, particularly in the Fluoxetine-treated group, indicating superior neuroprotective efficacy. Conclusion: Donepezil and Fluoxetine confer neuroprotection by enhancing locomotor function, reducing oxidative stress, restoring neurotransmitter balance, and attenuating neuroinflammation. Notably, Fluoxetine’s modulation of serotonergic-GSK-3 signalling suggests it may augment standard AD therapy by targeting both cholinergic and non-cholinergic mechanisms, offering a promising adjunctive strategy for disease management.
Copyright (c) 2025 PRIYANKA LG, BHARAT B. J., K. L. KRISHNA https://creativecommons.org/licenses/by/4.0
DEVELOPMENT AND OPTIMIZATIONS OF TRANSETHOSOMAL GEL LOADED WITH RUBIA CORDIFOLIA EXTRACT FOR TREATMENT OF PSORIASIS
Objective: This study aimed to develop and optimize a transethosomal gel loaded with Rubia cordifolia extract to enhance its topical delivery and therapeutic efficacy for the treatment of psoriasis. Methods: A box–behnken factorial design was employed to optimize transethosome formulations using three independent variables: Phospholipon 90 G, sodium deoxycholate, and ethanol concentration. Vesicle size, zeta potential, and entrapment efficiency were evaluated as responses. The optimized batch was incorporated into a gel using Carbopol 940 and Gellan gum. The formulations were assessed for physicochemical properties, ex-vivo skin permeation, and accelerated stability. Results: Among 17 formulations, the optimized batch (F13), selected based on desirability and experimental validation, showed a vesicle size of 111.73 nm, zeta potential of −28.15 mV, and entrapment efficiency of 86.54%. The optimized transethosomal gel (TF3) exhibited pH of 6.02 ± 0.04, viscosity of 21,873 ± 157 cP, spreadability of 30.92 ± 1.15 g·cm/s, and drug content of 98.42 ± 0.95%. TF3 demonstrated sustained drug release (91.05 ± 2.32% over 12 h), steady-state flux of 7.59 µg/cm²/h for TF3 formulation and remained stable over three months under accelerated conditions. Conclusion: The optimized transethosomal gel effectively enhanced the solubility, stability, and skin permeation of Rubia cordifolia extract. While permeation enhancement was demonstrated, anti-psoriatic efficacy validation through in vitro and in vivo studies is required to confirm therapeutic potential for psoriasis management. These findings suggest promising translational value, warranting further in vivo and clinical investigations.
Copyright (c) 2025 POOJA GAJANAN AKOSHKAR, RAHUL DHYANESHWAR KHAIRE https://creativecommons.org/licenses/by/4.0
IMPROVED BIOAVAILABILITY OF ATORVASTATIN AND FENOFIBRATE THROUGH TERNARY SOLID DISPERSIONS: A POLYMER-SUPPORTED METHOD FOR THE ULTIMATE SOLUBILITY ENHANCEMENT
Objective: This study aimed to improve the solubility and dissolution rate of a fixed-dose combination of atorvastatin (ATR) and fenofibrate (FEN) characterized by poor solubility via solid dispersion techniques. Methods: Soluplus and Kollidon were used for formulating binary solid dispersion (BSD), and PVP and Kollidon were used for ternary solid dispersion (TSD) employing the solvent evaporation technique. Saturation solubility studies and in vitro drug release were done to quantify improvements in solubility and drug dissolution. Further characterization of solid dispersions was carried out by differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray diffraction (XRD), and Fourier-transform infrared spectroscopy (FTIR). Results: Among binary systems, the SF8 formulation (drug-to-Soluplus® ratio of 1:4) showed an edge in solubilization enhancement, dissolution rate, and other physicochemical properties. The ternary composition KDF11 exhibited the best performance in terms of solubility and dissolution rate. In vivo, pharmacokinetic studies reaffirmed that drug bioavailability was greatly improved. SF8 BSD increased solubility by 17-fold. ATR solid dispersion produced 2.87 times more Cmax and 2.56 times more AUC₀–₂₄ₕ while FEN nanoformulation produced 3.56 times more Cmax and 3.44 times more AUC₀–₂₄ₕ after their pure drug counterparts. Cmax increased 2.87-fold for ATR. These increases can be understood to be attributed to the conversion of the crystalline structure into an amorphous state, thereby enhancing solubility and facilitating a more favorable concentration gradient across gastrointestinal and systemic barriers. Conclusion: The study demonstrated that in the ternary system, solid dispersion formulations were very much better than binary dispersions in improving the solubility and dissolution of poorly soluble drug combinations. TSD offers a viable strategy for enhancing FDC bioavailability with potential application in the effective management of hyperlipidemia.
Copyright (c) 2025 RAMESH BALASAHEB NAWALE, SANJEEV KUMAR SAHU, MANISH VYAS https://creativecommons.org/licenses/by/4.0
QUALITY BY DESIGN-BASED RP-HPLC METHOD DEVELOPMENT, DEGRADATION KINETICS, AND INTEGRATED GREEN AND BLUE ASSESSMENT FOR TEPOTINIB
Objective: Tepotinib, a recent Food and Drug Administration (FDA) approved anticancer drug, currently lacks an official pharmacopeial RP-HPLC method for quantification, and its degradation kinetics remain unexplored. This study aimed to develop a rapid, robust, and eco-friendly RP-HPLC method for the quantification of tepotinib and to investigate its degradation kinetics. Methods: An Analytical Quality by Design (AQbD) approach was employed. The critical method parameters were screened using a Plackett–Burman design and further optimized through a Central Composite Design. Chromatographic separation was achieved on a SunFire C18 column (250 × 4.6 mm, 5 µm) using a methanol: 0.1% OPA (52:48, v/v) mobile phase at a flow rate of 1.0 mL/min with UV detection at 272 nm. Forced degradation studies were conducted under hydrolytic, oxidative, and thermal stress. The resulting degradation kinetics were then determined. The method was validated according to the ICH Q2(R2) guidelines. Greenness and sustainability were evaluated using various green analytical metrics and the Efficient-Valid-Green (EVG) framework. Results: The developed method achieved efficient separation of tepotinib in only five minutes with a retention time of 2.4 min. Method validation confirmed excellent linearity over 22.5–157.5 µg/ml (R² = 0.9995),%RSD for intra-and inter-day precision were 0.7 and 0.5 %, mean recovery was 99.94 %. LOD and LOQ were 0.38 µg/ml and 1.14 µg/ml, respectively. Forced degradation studies revealed significant degradation under hydrolytic, oxidative, and thermal conditions, following zero-order kinetics. The greenness assessment indicated a low ecological impact, reduced solvent consumption, and minimal waste generation. Conclusion: An AQbD-based, environmentally friendly RP-HPLC method was successfully developed and validated for quantifying tepotinib and was applied to study its degradation kinetics. This method offers environmental sustainability and is suitable for routine pharmaceutical quality control of tepotinib.
Copyright (c) 2025 SYAMALA P. N. S., SREEDEVI ADIKAY https://creativecommons.org/licenses/by/4.0
DETERMINATION OF PROTEIN TRANSPORTERS FOR THE ABSORPTION OF ZN-PEPTIDES FROM HOLOTHURIA SCABRA THROUGH NETWORK PHARMACOLOGY WITH MOLECULAR SIMULATION APPROACH
Objective: This study aimed to identify key genes and proteins involved in zinc homeostasis and to evaluate the potential of sea cucumber (Holothuria scabra) peptides as zinc-binding agents targeting the zinc transporter protein ZIP2, which plays a central role in zinc deficiency. Methods: Bioinformatics analyses were conducted to identify genes associated with zinc deficiency and related pathways. Protein–protein interaction (PPI) networks were used to determine key target genes involved in zinc homeostasis. Molecular docking simulations assessed the binding affinity of six H. scabra peptides to the ZIP2 protein compared with ZnSO₄ and Zn-carnosine as controls. Molecular dynamics (MD) simulations, including RMSD and RMSF analyses, were performed to evaluate the stability and interaction dynamics of the most promising peptide–protein complex. Results: A total of 90 target genes associated with zinc deficiency were identified, involving multiple biological processes and pathways. Ten key protein-coding genes were found to play significant roles in zinc homeostasis, including nine zinc transporter genes (SLC39A2, SLC30A3, SLC39A4, SLC30A2, SLC30A4, SLC39A13, SLC29A8, TEX11, and C904f84) and one zinc-sensing receptor gene (GPR39). PPI network analysis revealed SLC39A2 (ZIP2) as the central gene in zinc homeostasis. Among the six tested peptides, the PY peptide exhibited the most favorable binding affinity to ZIP2 (-6.1 kcal/mol), surpassing both control compounds. MD simulations indicated stable interaction of the PY peptide at the active site of ZIP2 throughout the observation period. Conclusion: The study highlights SLC39A2 (ZIP2) as a pivotal protein in zinc homeostasis and identifies the PY peptide from H. scabra as a promising zinc-binding agent. These in silico findings provide a foundation for future in vitro and in vivo investigations into potential peptide-based interventions for zinc deficiency.
Copyright (c) 2025 GITA SYAHPUTRA, MELVA LOUISA, MASTERIA YUNOVILSA PUTRA, RINA WIJAYANTI, NUNIK GUSTINI, A’LIYATUR ROSYIDAH https://creativecommons.org/licenses/by/4.0
DEVELOPMENT AND CHARACTERIZATION OF GLYCYRRHIZIN-LOADED BUCCAL FILM-O-SPRAY: A NOVEL APPROACH TO RECURRENT APHTHOUS STOMATITIS THERAPY
Objective: Recurrent aphthous stomatitis (RAS), affecting 5–50% of the population, is characterized by painful oral ulcers. Conventional therapies often lead to side effects, drug resistance, and secondary infections, underscoring the need for safer and more effective alternatives. This study aimed to develop a glycyrrhizin-based film-forming spray (FFS_GLY) to enhance mucosal drug delivery, prolong retention, and provide rapid relief from oral ulcers. Methods: A 3³ Box–behnken design was employed to optimize the concentrations of HPMC-E15, Eudragit-S100, and propylene glycol (PG), considering drying time and viscosity as dependent variables. The optimized formulation (F4) was evaluated for physicochemical properties, mucoadhesion, and mucosal drug retention. Each actuation of the spray was standardized to deliver 3 mg of glycyrrhizin. Preclinical efficacy was assessed in wistar rats with acetic acid–induced oral ulcers, supported by histopathological analysis. Results: The optimized F4 formulation demonstrated a drying time of 75.12±0.05 seconds and viscosity of 19.28±0.019 cPs. It exhibited strong mucoadhesive strength (577.5±0.016 dynes/cm²; 0.05775 N/cm²) and sustained mucosal retention (6.105 mg/cm²) for up to 24 h. Consistent dose delivery was achieved with each spray actuation. In vivo studies showed significant reduction in ulcer diameter compared to controls, while histopathological evaluation confirmed enhanced epithelial regeneration and angiogenesis. Conclusion: The developed FFS_GLY formulation demonstrated favourable physicochemical characteristics, excellent mucosal retention, and significant therapeutic efficacy in preclinical models. These findings establish FFS_GLY as a safe, effective, and promising alternative for the management of recurrent aphthous stomatitis.
Copyright (c) 2025 AYESHA SYED, PREETI KARWA, SOHAL MALLICK, PRITHIVIRAJAN S. https://creativecommons.org/licenses/by/4.0
FORMULATION AND EVALUATION OF EFFERVESCENT GRANULES CONTAINING ANTIRETROVIRAL AGENT SOLID DISPERSIONS FOR CHILDREN AND ELDERS: SOLUBILITY ENHANCEMENT, DISSOLUTION RATE AND INTEGRATION INHIBITION EFFECT
Objective: Dolutegravir inhibits viral replication by blocking the integrase strands. To treat human immunodeficiency virus (HIV), it is one of the medications used in children and the elderly. It is difficult to get a high oral bioavailability of dolutegravir because of these population issues with swallowing and ineffective absorption, as well as the drug's intrinsic poor solubility and instability in stomach acid. To address these problems, we created and described effervescent granules containing a solid dolutegravir dispersion. Methods: The melt granulation process was used with various categories and quantities of polymers to develop solid dispersion-based effervescent granules. The solid dispersions were prepared using four different methods: Physical Mixing, Co-grinding, Kneading and fusion methods. Drug-to-carrier ratios of 1:1, 1:2, 1:3, and 1:4 were investigated. To develop solid dispersions, three generations of polymers are selected [crystalline carrier (mannitol), Amorphous carriers [polyethene glycol (PEG 4000), polyvinyl pyrrolidone (PVP K90), hydroxypropyl methylcellulose (HPMC E5LV), sulfobutylether-Captisol (captisol)], poloxamer 188 and poloxamer 407]. Results: The DTG and the chosen polymer are compatible, according to FTIR studies; DSC and XRD results reveal crystalline changes of DTG; surface morphology reveals that pure DTG has a crystalline prismatic shape. Second, a total of 12 formulations of the effervescent granules containing the solid dispersion were developed using various excipients such as sweeteners, gas generators, pH modulators, and glidants/lubricants. The results show that all 12 formulations had a good release profile within 5 min. F3 shows the highest drug content (99.5±0.11), the highest percentage of drug release 99.5% within 5 min and the effervescent cessation time 19.5±2.12 sec. The good release profile of F3 may be attributed to the combination of cetyl alcohol and sodium starch glycolate. Conclusion: Additional in vivo and clinical research may be conducted on the final effervescent granule product to develop it into a dolutegravir delivery system with high bioavailability for older people and children.
Copyright (c) 2025 SUNITHA SAMPATHI, LAKSHMI DEVI GOTTEMUKKULA, B. AISHWARYA, M. JYOTHIRADITYA, B. MANIKANTH https://creativecommons.org/licenses/by/4.0
DESIGN OF NABUMETONE-LOADED TEMPERATURE-RESPONSIVE GEL FOR COLORECTAL DELIVERY USING LIPID NANOCARRIERS IN VITRO/IN VIVO EVALUATION
Objective: This study aimed to develop a novel thermosensitive in situ gel incorporating nabumetone-loaded solid lipid nanoparticles (NAB-SLP-TSG) for rectal delivery to enhance bioavailability and sustain drug retention. Methods: NAB-SLPs were prepared and optimized using Central Composite Design and evaluated for particle size, encapsulation efficiency, surface charge, and morphology. The optimized SLPs were incorporated into a temperature-sensitive gel and characterized for gelation behavior, rheology, mucoadhesiveness, in vitro drug release, pharmacokinetics, rectal mucosal safety, and retention. Results: Optimized NAB-SLPs demonstrated an encapsulation efficiency of 89.62±1.34%, drug loading of 14.85±1.13%, mean particle size of 161.43±2.17 nm, PDI of 0.29±0.07, and zeta potential of −20.45±0.63 mV. FTIR and XRD confirmed drug encapsulation and its amorphous dispersion in the lipid matrix. The NAB-SLP-TSG exhibited a gelation temperature of 32.81±0.73 °C, gelation time of 15.32±2.37 s, and mucoadhesive strength of (11.09±0.42)×10² dyne/cm². In vitro, a biphasic release profile was observed. In vivo, the formulation significantly enhanced NAB absorption and bioavailability without causing rectal tissue irritation, while ensuring prolonged local retention. Conclusion: Unlike previously reported thermosensitive rectal gels for drugs like diclofenac or insulin, this formulation uniquely combines γ-Polyglutamic acid (γ-PGA) to significantly enhance mucoadhesion and solid lipid nanoparticles (SLPs) to sustain rectal retention. This dual approach distinctly advances prior systems by improving both residence time and systemic availability of nabumetone, offering a novel and superior alternative for rectal NSAID delivery.
Copyright (c) 2025 DALIA A. GABER, MOHAMMED A. AMIN, MOSTAFA A. MOHAMED https://creativecommons.org/licenses/by/4.0
DEVELOPMENT AND VALIDATION OF A STABILITY-INDICATING HPTLC METHOD FOR VERAPAMIL ANALYSIS USING THE AQBD APPROACH
Objective: To develop selective, precise and accurate High Performance Thin Layer Chromatography (HPTLC) method for forced degradation study of Verapamil by implementing AQbD (Analytical quality by design) approach. To optimize chromatographic conditions and detection wavelength for efficient separation and quantification of Verapamil using AQbD. To perform a forced degradation study on Verapamil as per International Council for Harmonisation (ICH) guideline. To validate the developed HPTLC method as per ICH Q2(R2) guideline. Methods: The method employs TLC aluminium plates precoated with silica gel 60F254 as the stationary phase. The mobile phase consists of toluene, ethyl acetate, methanol, and ammonia in a volumetric ratio of 4:2:3.5:0.5. Verapamil quantification was performed in reflective mode at a wavelength of 276 nm. The method was validated for linearity, precision, accuracy, recovery, and robustness. Results: The HPTLC method exhibited strong retention for verapamil with an Rf value of 0.72. Calibration curve analysis demonstrated excellent linearity over a concentration range of 200-1000 ng/band with a correlation coefficient (R²) of 0.9961. The slope and intercept were determined as 0.0013x+0.0074. The detection and quantitation limits were found to be 0.3008 ng/band and 0.9116 ng/band, respectively. The method showed high precision, accuracy, and robustness, ensuring its reliability for pharmaceutical applications. Conclusion: The validated HPTLC method provides an efficient and reliable approach for the quantitative analysis of verapamil in synthetic mixtures. Its precision, sensitivity, and rapid analytical capabilities make it a suitable technique for pharmaceutical quality control and routine analysis.
Copyright (c) 2025 GAYATRI S. BADGUJAR, DHRUVI PRAJAPATI https://creativecommons.org/licenses/by/4.0
DESIGN AND EVALUATION OF MULTIFUNCTIONAL 3D-PRINTED SCAFFOLDS FOR BONE TISSUE REGENERATION AND LOCALIZED INFECTION MANAGEMENT
Objective: The research objective was to create tobramycin-loaded Poly(lactic acid) (PLA) scaffolds produced by 3D printing and coat them with either chitosan or Eudragit RS100 for maximizing bone tissue development alongside localized antibacterial treatments. Methods: PLA scaffolds with pore size 300μm was manufactured through Fused deposition modeling (FDM) based on CAD designs. The scaffolds integrated tobramycin through dipping into solutions containing chitosan and Eudragit RS100 at concentrations of 1%, 2%, and 3%. Scaffold morphology test by SEM analysis followed by chemical compatibility evaluation using FTIR and XRD techniques. Drug release behavior, along with degradation study, is carried out in phosphate-buffered saline (PBS) and simulated body fluid (SBF). The antibacterial effect against E. coli was determined by zone of inhibition assay. Results: SEM proved definite porous scaffolds with homogenous coating of drug-polymer. The results of FTIR and XRD indicated that there was no chemical interaction and this was an indication of stable physical incorporation. Biphasic in vitro release of tobramycin was observed and long-term release was found in the 3% polymer-coated scaffolds (TBMC3, TBME3). The Fickian diffusion release was given in drug release (R 2>0.97). Antibacterial tests revealed increased inhibition of E. coli with an increase in the quantity of the polymers. Bioactivity in SBF chronic-degradation indicated gradual weight-decrease (up to 1.48 g) and the development of mineral deposition in the scaffold over 60 d. Conclusion: The 3D-printed PLA scaffolds containing tobramycin and having chitosan or Eudragit RS100 coatings showed beneficial aspects in terms of morphological structure combined with acceptable physicochemical and biological properties. Sustained drug release, anti-bacterial with biodegradable nature, makes these scaffolds suitable candidates for bone tissue engineering applications and infection control implants.
Copyright (c) 2025 SWATI SWAGATIKA SWAIN, VEERA VENKATA SATYANARAYANA REDDY KARRI https://creativecommons.org/licenses/by/4.0
MIXED POLYMERIC NANOMICELLES LOADED WITH MECLIZINE HYDROCHLORIDE: PREPARATION AND CHARACTERIZATION
Objective: The goal of this study was to make meclizine hydrochloride (MLZ) into nanomicelles using soluplus®® with TPGS or Tween 80 to make MLZ more soluble and easier to absorb when taken by mouth. Methods: The maximum absorbance wavelength of MLZ was found, and calibration curves were made in both methanol and phosphate buffer pH 6.8 with 0.25% sodium lauryl sulfate (SLS). Nanomicelles were made by directly dissolving soluplus®® with either TPGS or Tween 80. The selected formulations were examined to determine particle size (PS), polydispersity index (PDI), zeta potential, drug content, dissolution rate, drug trapping efficiency, drug loading and in vitro drug release. Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and field emission scanning electron microscopy (FESEM) were used to study the best formulation, F17, further (soluplus®: Tween 80 = 50:25). Results: The best formula was F17, which had a PZ of 57.75±1.0 nm, a PDI of 0.086±0.006, an EE% of 98.88±0.5%, a zeta potential of+3.90±0.18, a solubility factor of 7.56±0.12 mg/ml, drug content of 98.59%±0.28, drug loading of 24.86±0.11, and a 90 min release rate of 94%. The One-Way ANOVA test showed that there were statistically significant impacts on EE% (p<0.05), but not on PS (p>0.05). PDI did not exhibit any significant results (p>0.05). Stability tests of the best formula indicated that the PS and EE% stayed pretty consistent for at least three months. Conclusion: Nanomicelles are effective carriers for enhancing the solubility of MLZ in the mouth, thereby increasing its availability to the body. Nanomicelles have a flawless dissolving profile, which makes them an attractive option for use in pharmaceuticals.
Copyright (c) 2025 HIND KHALID OMAR, SHAIMAA NAZAR ABD ALHAMMID https://creativecommons.org/licenses/by/4.0
DESIGN AND CHARACTERIZATION OF LULICONAZOLE-ENCAPSULATED TRANSFEROSOMES IN THERMOSENSITIVE OCULAR GEL
Objective: The present study develops and optimizes a thermosensitive in-situ gel containing Luliconazole-loaded transferosomes (LCZ-TFs) to improve ocular bioavailability and therapeutic efficacy through enhanced permeation and prolonged retention. Methods: Transferosomes (TFs) were prepared using the thin film hydration method. To optimize the formulation, a Box-Behnken design was used to study the effects of three variables: the concentration of soya phosphatidylcholine (SPC), Tween 80, and chloroform and evaluated for their influence on vesicle size, polydispersity index (PDI), and percentage entrapment efficiency (EE). Zeta potential and Transmission Electron Microscopy (TEM) analysis were performed for optimized formulation. The optimized transferosome was incorporated into the thermosensitive in-situ gel containing Pluronic F127 (15% w/v) and Pluronic F68 (1% w/v) and evaluated for in vitro drug release using a membrane diffusion technique and ex vivo permeation studies on goat cornea using a modified Franz diffusion cell. Results: The optimized TFs showed a particle size of 205.5 nm, PDI of 0.236, and EE of 77.43%. The zeta potential was recorded at −53.9 mV, indicating good stability. TEM revealed well-formed spherical vesicles. Drug release studies demonstrated a sustained release profile from the transferosomes in situ gel with release kinetics following first-order kinetics and Higuchi model mechanisms. In ex vivo permeation studies, the transferosomes in situ gel showed a 1.68-fold higher permeation than the conventional gel. The formulation passed sterility and isotonicity tests and retained antifungal activity comparable to a marketed product, as shown by its zone of inhibition. Additionally, the hen’s egg test–chorioallantoic membrane (HET-CAM) test confirmed the gel was non-irritant and safe for ocular use. Conclusion: Overall, the transferosomes in situ gel significantly improved ocular retention and prolonged the drug's release, which enhances the therapeutic effectiveness of Luliconazole in treating fungal keratitis.
Copyright (c) 2025 M. DIVYANAND, SNEH PRIYA, MELANIE ASHEL DSOUZA, MURARI UPADHYAY https://creativecommons.org/licenses/by/4.0
MOLECULAR DOCKING AND GRAPHICAL TRAJECTORY ANALYSIS OF CINNAMOMUM ZEYLANICUM COMPOUNDS FOR TARGETING HUMAN MALTASE-GLUCOAMYLASE IN DIABETES MANAGEMENT
Objective: Maltase-glucoamylase is an essential enzyme involved in the final hydrolysis of dietary carbohydrates into glucose, facilitating postprandial glucose absorption. Its heightened activity exacerbates glucose spikes, a hallmark of type 2 diabetes, making it a pivotal target for therapeutic intervention. This research aims to explore the inhibitory potential of phytocompounds from Cinnamomum zeylanicum as promising enzyme inhibitors, with acarbose serving as a reference standard. Methods: Eighteen phytocompounds were screened via molecular docking and molecular dynamics (MD) simulations. Binding affinity, residue interactions, and structural stability were assessed, alongside pharmacokinetic and toxicity profiling using absorption, distribution, metabolism, excretion, and toxicity (ADMET) tools. Results: Alpha-cadinol and cis-4-Benzyl-2,6-diphenyltetrahydropyran emerged as top candidates with binding energies of-10.21 and-10.17 kcal/mol, respectively, surpassing acarbose (-9.11 kcal/mol). Interaction analysis revealed that alpha-cadinol formed hydrogen bonds with TYR A: 1251 and GLY A: 1588, while cis-4-Benzyl-2,6-diphenyltetrahydropyran engaged residues such as HIS A: 1710 and THR A: 1699 through a combination of hydrogen bonding and aromatic interactions. Molecular dynamics simulations confirmed the stability of these complexes, with root mean square deviation values of 0.33 nm for alpha-cadinol and 0.34 nm for cis-4-Benzyl-2,6-diphenyltetrahydropyran, comparable to acarbose. Reductions in solvent accessibility and root mean square fluctuation further demonstrated the stabilising effects of these compounds on the enzyme. Pharmacokinetic profiling revealed favourable absorption and bioavailability for both compounds, suggesting their suitability as oral therapeutics. Conclusion: These findings highlight alpha-cadinol and cis-4-Benzyl-2,6-diphenyltetrahydropyran as potential alternatives to acarbose with possibly improved safety and efficacy profiles. However, in vitro and in vivo validation is necessary to confirm their therapeutic applicability and establish their metabolic stability. This study offers a significant step toward developing novel enzyme inhibitors for effective diabetes management and paves the way for future experimental and clinical exploration.
Copyright (c) 2025 VYSHNAVI VISHWANADHAM RAO, KOPPALA NARAYANAPPA SHANTI, DINESH SOSALAGERE MANJEGOWDA https://creativecommons.org/licenses/by/4.0
OPTIMIZATION AND VALIDATION OF ULTRA PERFORMANCE LIQUID CHROMATOGRAPHY COUPLED WITH TANDEM MASS SPECTROMETRY FOR QUANTIFICATION OF EFAVIRENZ IN HUMAN PLASMA
Objective: This study presents the optimization and validation of a sensitive, rapid, and reliable ultra-performance liquid chromatography method for the quantification of efavirenz in human plasma, using efavirenz 13C6 as the internal standard. Method: The liquid-phase extraction technique was used to isolate the internal standard and the analyte from human plasma. The extracted samples were analyzed using chromatography on an Acentis® Express 90 Å C18 column (5 cm x 4.6 mm, 2.7µm), elution carried out using a mixture of ammonium acetate buffer (5 mmol) and acetonitrile as the mobile phase (70:30). The flow rate was maintained at 0.6 ml/min with an injection volume of 5 µl. The ionization mode was negative ion electrospray, with a source energy of 150 °C. Results: The linearity of the method was confirmed by a correlation coefficient of 0.9979, and the calibration range for efavirenz was found to be 50.00-5000 ng/ml. The precision and accuracy for both intra-day and inter-day measurements showed a %CV of less than 2.3% which is within the acceptable limit. The total run time was 3 min. The mean percentage recovery was 83.9 %. Conclusion: The developed method offers a significantly reduced run time, enhancing analytical throughput and efficiency compared to previously reported methods with longer durations. This makes it particularly suitable for high-throughput analysis in routine quality control or pharmacokinetic studies.
Copyright (c) 2025 GAYATRI S., SURYA M., KARTHIK R., VASUNDRA L. https://creativecommons.org/licenses/by/4.0
FORMULATION AND CHARACTERIZATION OF EFFERVESCENT TABLETS FROM A TRADITIONAL MEDICINE RECIPE FOR DENTAL CARE
Objective: Plant use to treat pathologies is increasingly common in Africa. Our study focuses on a recipe (active ingredient) of traditional medicine that has proven itself in treating dental caries and oral pathologies. This study aims to formulate and evaluate the quality of effervescent tablets based on the recipe (active ingredient) for treating dental caries and oral hygiene. Methods: A physicochemical and pharmacotechnical characterization of the recipe (RMC, pH, Hausner index, Carr index, flow rate) was carried out. Five stoichiometric ratios of the citric acid/sodium bicarbonate combination were used (1:3.32; 1:3.11; 1:3; 1:2.93; 1:2.87). The tablets were obtained after wet granulation. Pharmacotechnical tests were carried out according to the European Pharmacopoeia 10th Ed to determine the most optimal formulation that could promote rapid release of the active ingredient. Results: The recipe constituting the active ingredient has properties with an apparent density of 0.50, and a density after tamping of 0.65. The compressibility index is 23.61, and the Hausner index is 1.30. These fairly weak rheological properties required improvement through granulation. A total of 5 formulations were obtained. Formulations F2 to F5 had a disintegration time of less than 5 min. The friability rate was less than 4.60%, 0.86%, 0.91%, 0.75%, and 1.22 for the formulations respectively F1 to F5 and the hardness 95N, 81.8N, 118N, 103.6N, 89.8N. The stoichiometric ratio of 1:3.11 gave us the most optimal formulation with a disintegration time of 156 seconds, a friability rate of 0.86%, and a pH of 5.13. Conclusion: These results demonstrate the feasibility of a solid form to be redispersed for use in oral hygiene.
Copyright (c) 2025 Boladé Constantin ATCHADE, Salfo OUEDRAOGO, Tata Kadiatou TRAORE, Isanorelle BONOU-SELEGBE, Aimé-Césaire AYENA, Mory GUILAO, Josias B.G YAMEOGO, Bavouma Charles SOMBIE, Hermine Zime DIAWARA, Rasmané SEMDE https://creativecommons.org/licenses/by/4.0
A PEEL-OFF FACE MASK GEL CONTAINING SILYMARIN FOR THE MANAGEMENT OF FACIAL ACNE: FORMULATION AND OPTIMISATION BY RESPONSE SURFACE METHODOLOGY APPROACH
Objective: To prepare and optimise peel-off face mask gel containing silymarin for the management of acne and evaluate its performance in vitro. Methods: This study established Silymarin's identity using Proton NMR and FTIR. A total of 17 peel-off facemask gels containing silymarin were subsequently prepared as per Box Behnken Design and the influence of the formulation components on the critical evaluation parameters was investigated. The optimised formulation was selected based on criteria of maximum spreadability and minimum drying time. The optimised formulation was then subjected to various in vitro evaluation parameters like organoleptic properties, Physiochemical properties, antioxidant activity, antimicrobial activity and stability studies. Results: Statistical analysis from the Box Behnken Design (BBD) revealed that ethanol concentration had a significant inverse relationship with drying time (coefficient: –5.56, p<0.0001), while PVA and Carbopol negatively influenced spreadability (p<0.0001). The optimized formulation, containing 6.01% PVA, 0.632% Carbopol, and 8.3% ethanol, exhibited a drying time of 22.56 min and spreadability of 4.25 cm, with a residual error of 5.15% for drying time and 3.19% for spreadability from predicted values and overall desirability of 0.925. The formulation showed desirable organoleptic properties, a viscosity of 7700±435.88 cP, and a pH of 5.45±0.25, making the formulation suitable for topical application. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) scavenging activity confirmed the antioxidant potential of the peel-off facial mask with an IC 75 value of 525µg/ml. Antimicrobial studies showed a 22.1 mm zone of inhibition against S. aureus, comparable to standard clindamycin gel (23.4 mm). In vitro diffusion studies indicated a sustained drug release (68.1% at 24 h) with Korsmeyer–Peppas model fitting (R² = 0.981, n = 0.481), confirming diffusion-based release mechanism. Stability testing confirmed the formulation retained its key properties under room and accelerated conditions for 30 days. Conclusion: The developed formulation satisfied all the in vitro evaluation criteria for peel-off face mask gels and has potent antioxidant and anti microbial potential. However, further in vivo studies of the formulation in suitable animal models are required to validate its therapeutic efficacy.
Copyright (c) 2025 SINDHOOR S. M., GLADYSTON NETTO, VAISHNAVI, SILNA SASI, SHARMA ABHISHEK RAMVRIKSH https://creativecommons.org/licenses/by/4.0
A VALIDATED ANALYTICAL METHOD FOR RANITIDINE HCL THROUGH LC-MS/MS, HPLC AND QUALITY BY DESIGN APPROACH.
Objective: The current study aimed to develop and validate simple, precise, and highly sensitive LC-MS/MS and HPLC methodologies for the quantitative estimation of Ranitidine HCl in pharmaceutical formulations. The goal was to develop a speedy and dependable technique for routine quality control and regulatory analysis. Methods: Chromatographic separation was achieved using an Atlantis C18 column (150×4.6 mm, 5µm) under isocratic elution mode. The mobile phase consisted of 10 mmol ammonium acetate (solvent A) and acetonitrile (solvent B) in a 10:90 v/v ratio, delivered at a flow rate of 0.7 ml/min. An injection volume of 10µl* was employed, and the run time was 4 min. Ranitidine HCl was eluted at 1.993 min. The method was validated in accordance with ICH Q2 (R1) guidelines for parameters including linearity, sensitivity, accuracy, precision, and robustness. Results: The LC-MS/MS method showed excellent linearity across a concentration range of 5-250 ng/ml with a correlation coefficient (R2) of 0.9998. The limit of detection (LOD) and limit of quantification (LOQ) were determined to be 1.0 ng/ml and 3.0 ng/ml, respectively. Recovery ranged from 95.33% to 97.93% and relative standard deviation (RSD) was 0.69%, confirming the method’s accuracy and precision. Conclusion: The validated LC-MS/MS and HPLC methods are simple and sensitive for the quantification of ranitidine HCl. Both techniques demonstrated robust performance with high accuracy and precision. Their successful application to a commercial formulation confirms their suitability for pharmaceutical quality control and supports regulatory compliance in the routine analysis of ranitidine HCl products.
Copyright (c) 2025 DEBANGANA PAL, BABU B., SM. HABIBUR RAHMAN, KALIRAJAN R., CHANDAN C. https://creativecommons.org/licenses/by/4.0
ANTI-CANCER POSSIBILITY OF ZINGIER OFFICIALE NANOPARTICLES: MECHANISMS AND THERAPEUTIC UNDERSTANDING
Objective: To synthesize and profile green-prepared copper nanoparticles (ZOE-CuNPs) and to determine their cytotoxicity effects on human breast cancer cells. Methods: ZOE-CuNPs were synthesized by green reduction of copper acetate using Zingiber officinale extract. The characterization was done by UV-Vis, XRD, SEM-EDS, and FT-IR techniques. Cytotoxicity was assessed in aline of breast cancer cells. A new breast cancer cell line (AMJ13) using the MTT assay (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyltetrazolium bromide) at 0-100 µM concentrations. Results: Copper nanoparticles were successfully synthesized using Zingiber officinale extract (ZOE-CuNPs) via green synthesis, as established by UV-Vis spectroscopy displayed distinguishing absorption peak at ~439 nm, characteristic of Cu-based nanoparticles; the spectra were unchanged after ageing. XRD noted Cu-based nanocrystalline phases (probably including copper oxides, e. g., Cu 2 O/CuO); a clear assignment would require application of Rietveld alteration against appropriate JCPDS cards with a regular particle dimension of 31 nm, calculated using means of the Debye-Scherrer equation. Scanning electron microscopy demonstrated predominantly quasi-spherical morphology with slight accumulation, although energy-dispersive X-ray spectroscopy confirmed elemental composition (Cu, O, C). FTIR analysis identified spectral shifts in the ranges 3248-3355 cm⁻¹, 1652-1751 cm⁻¹, and 1479-1432 cm⁻¹, indicating gingerol-mediated reduction and stabilization of copper ions through alcohol, carbonyl, and amine functional groups. Cytotoxicity evaluation against breast cancer cells using MTT assay revealed concentration-dependent anticancer activity across six concentrations (0-100 µM), with inhibition rates increasing from 0.00±2.1% (control) to 75.00±2.9% at 100 µM. Analysis(one-way ANOVA, p<0.001) confirmed significant differences between all concentration groups, demonstrating potent dose-dependent cytotoxic efficacy of the green-synthesized ZOE-CuNPs for potential anticancer nanomedicine applications. Conclusion: ZOE-CuNPs exhibit high, concentration-dependent anticancer activities, which are likely mediated through ROS generation and initiation of apoptotic pathways.
Copyright (c) 2025 NAJAT AMEEN SAEED, ABEER MANSOUR ABDEL RASOOL, AYMN YASEEN SHARAF ZEEBAREE https://creativecommons.org/licenses/by/4.0
DESIGN AND STATISTICAL OPTIMIZATION OF MUSKMELON PECTIN-BASED TELMISARTAN ORAL FAST DISSOLVING FILMS THROUGH QUALITY BY DESIGN
Objective: This study aimed to design and statistically optimize oral fast-dissolving films containing telmisartan based on muskmelon pectin using a quality-by-design approach. Methods: Cucumis melo pectin was extracted by acid hydrolysis. The physicochemical properties of muskmelon pectin were evaluated using FTIR, NMR, DSC, and SEM. The fast-dissolving films were made by solvent casting, and they were optimized using a 23-factorial design. A two-way factorial design was used because it effectively assesses the impact of three film-forming polymers, namely muskmelon pectin, apple pectin, and citrus pectin, at two concentrations (0 mg and 350 mg), on important formulation responses such as percentage drug dissolution and dissolution efficiency within 10 min. With a few experimental runs, this strategy enables the investigation of both the independent and combined effects of factors. The Critical Quality Attributes (CQA) of each of the eight formulations were analyzed, including dissolution efficiency (DE%), disintegration time (DT), tensile strength (TS), thickness, and the percentage of drug dissolved in 10 min (PD%). The optimized formulation was evaluated for in vivo bioavailability in Wistar rats. The accelerated stability tests were performed according to ICH guidelines. Results: The extracted muskmelon pectin was found to be amorphous and water-soluble, with a high degree of esterification, and exhibited satisfactory swelling index, viscosity, and pH values. Instrumental analyses using FT-IR, NMR, SEM, XRD, and DSC confirmed the material as pectin. The optimized formulation (F2) demonstrated favorable critical quality attributes, including drug dissolution efficiency at 10 min (DE₁₀min), tensile strength (TS), and percentage drug dissolved at 10 min (PD₁₀min), with drug release reaching approximately 95.61%. In vivo pharmacokinetic studies showed that TMF2 had significantly higher maximum plasma concentration (Cmax) and area under the curve (AUC), and relative bioavailability of 175.85%, showing a 75.85% enhancement over pure telmisartan, indicating the developed formulation significantly boosts drug absorption and may offer superior therapeutic effectiveness. Additionally, stability studies over six months revealed no significant changes in drug content, mechanical strength, or dissolution profiles, confirming the formulation’s stability and suitability for therapeutic use. Conclusion: Telmisartan OFDFs were successfully designed and optimized using muskmelon pectin as a new film-forming agent through 23 factorial designs, which exhibited 95.61% of the drug dissolution in 10 min and dissolution efficiency in 10 min alone, showing its better and efficient drug delivery.
Copyright (c) 2025 THAKUR REKHABAI, SANTOSH KUMAR https://creativecommons.org/licenses/by/4.0
DEVELOPMENT AND EVALUATION OF SILVER NANOPARTICLES-LOADED PHYTOGEL OF HYDROALCOHOLIC EXTRACT OF FICUS VIRENS BARK: FORMULATION, OPTIMIZATION, AND ANTIMICROBIAL EFFICACY
Objective: This study aimed to develop, optimize, and characterize a transdermal phytogel incorporating silver nanoparticles (AgNPs) loaded with Ficus virens hydroalcoholic bark extract, using Carbopol 940 as the gelling agent, to enhance antimicrobial efficacy and formulation stability. Methods: This research involved the preparation of phytogel formulations by systematically varying the concentrations of Carbopol 940 and silver nanoparticles combined with hydroalcoholic Ficus virens bark extract (FV-BE). A Central composite design (CCD) was employed to optimize the formulations and evaluate the influence of independent factors on key formulation attributes. Comprehensive physicochemical evaluations, including measurements of pH, viscosity, spreadability, extrudability, drug content, entrapment efficiency, and stability, are conducted to ensure suitability for topical application. The nanoparticulate system was described via zeta potential, particle size, and polydispersity index (PDI) study. To further understand the release mechanisms, in vitro drug release and kinetic modeling were performed. The agar well diffusion method was used to evaluate the antibacterial activity against Aspergillus niger, Pseudomonas aeruginosa, Staphylococcus aureus, and Escherichia coli. Results: The optimized formulation (F7) containing 0.75% w/w Carbopol 940 and 0.02% w/w AgNPs with FV-BE exhibited desirable physicochemical properties, including suitable viscosity (5517±1.2 cps), spreadability (12.75±1.67 g. cm/s), pH (6.64±0.097), high entrapment efficiency (90.23±0.37%), and drug content (92.95%±1.12%). The average particle size was 259.5 nm with a PDI of 0.280, and the zeta potential was -26.5 mV, indicating moderate colloidal stability. In vitro drug release studies revealed a complete diffusion-controlled release over 24 h, fitting the Korsmeyer-Peppas model with a non-Fickian diffusion mechanism. The phytogel formulation demonstrated notable antimicrobial activity against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, and Aspergillus niger, with inhibition zones comparable to standard antibiotics. Stability studies confirmed the formulation's robustness under various storage conditions over three months. Conclusion: The developed phytogel incorporating FV-BE and AgNPs is a promising nanocarrier-based system for effective topical antimicrobial therapy. Further in vivo and clinical validations are warranted to advance its therapeutic application.
Copyright (c) 2025 DEEPIKA AGGARWAL, KAMAL SAROHA, MANJUSHA CHOUDHARY, KAMAL KAUSHIK https://creativecommons.org/licenses/by/4.0
SYNTHESIS AND OPTIMIZATION OF MAGNESIUM ALUMINOMETASILICATE-TEMPLATED MESOPOROUS NANOPARTICLES FOR CANNABIDIOL DELIVERY: A NOVEL APPROACH
Objective: Mesoporous nanoparticles (MNPs) have improved practically insoluble drugs' bioavailability and therapeutic efficacy. Novel Magnesium Aluminometasilicate (MAS)-templated synthesis of cannabinoid-loaded mesoporous nanoparticles: Formulation, characterization, and in vitro drug release assessment. Methods: The purity and thermal stability of cannabidiol (CBD) were evaluated by melting point and differential scanning calorimetry analyses. The effects of Magnesium Aluminometasilicate (MAS), triethanolamine, and temperature on entrapment efficiency and particle size were assessed using a Box-Behnken Design (BBD) to optimize the formulation. Scanning Electron Microscopy (SEM), zeta potential, and Polydispersity Index (PDI) were used to analyze the formulation. In vitro drug release and stability studies were conducted. Results: The calibration curve showed linear relationship (R² = 0.9984). Highest solubility was observed in DMSO (60.54±2.47 mg/ml), while phosphate buffer pH 6.8 showed limited solubility (0.31±0.03 mg/ml). Formulation F13 demonstrated optimal entrapment efficiency (87.7%), loading capacity (37.24%), particle size (128.6 nm), and PDI (0.245). Zeta potential (-23.9 mV) confirmed colloidal stability. Release kinetics followed zero-order model (R² = 0.9863) with sustained release (94.04% over 12 h). Accelerated stability studies confirmed excellent stability over six months. Conclusion: The study demonstrates that magnesium aluminometasilicate template-assisted encapsulation of cannabidiol achieved high entrapment efficiency (87.7%), sustained in vitro release (94.04% over 12 h), and excellent stability under accelerated conditions. In vivo bioavailability studies are required to confirm therapeutic potential.
Copyright (c) 2025 PARE PANKAJ RAJENDRA, MANISH KUMAR https://creativecommons.org/licenses/by/4.0
A NOVEL LC-MS/MS TECHNIQUE FOR THE QUANTITATION OF LURBINECTEDIN IN HUMAN PLASMA: APPLICATION OF STABILITY STUDIES
Objective: A linear and precise liquid chromatography coupled with tandem mass spectrometry method was developed and validated for the quantification of lurbinectedin in plasma. Canagliflozin served as an internal standard (IS). Methods: The plasma extraction utilized 5 ml of ethyl acetate as the solvent. The examination was performed utilizing a Zorbax ODS (50 mm × 2.1 mm x 3µ) stationary phase at ambient conditions, with a mobile phase comprising 0.1% HCOOH, acetonitrile, and methyl alcohol in a ratio of 15:50:35. The measurement of the mobile phase's flow rate was recorded at 0.4 ml/min. In positive ionization mode utilizing electrospray, the drug and internal standard were detected, resulting in mass transitions of (m/z): Lurbinectedin, 785.30/711.20 and Canagliflozin (IS), 445.15/267.12. Results: A linear correlation was established between the concentrations of Lurbinectedin and their corresponding peak proportions to canagliflozin across the concentration range of 0.2-3200 ng/ml. The precision for Lurbinectedin, measured both within the same day and across different days, was determined to be ≤5.18%. Inter and intra-day bias ranged from −4.17% to 4.53. The measured average extraction recovery for Lurbinectedin was found to be 99.23%. The measurement of the internal standard's recovery was found to be 98.31%. Lurbinectedin was subjected to thorough assessment regarding its long-term, freeze-thaw, bench top, short-term stability, auto sampler, dry extract, and stock solution stability at both low quality control (QC) and high QC levels, showing consistent stability across all evaluated conditions. Conclusion: The developed method has become a cornerstone of modern clinical laboratories due to its versatility, sensitivity, and precision, and its ability to support both routine clinical diagnostics and cutting-edge personalized medicine.
Copyright (c) 2025 PRATHYUSHA KOTHA, CHANDRASHEKARA RAO BARU, CHAMAKURI KANTLAM https://creativecommons.org/licenses/by/4.0
ENHANCED COMBINED EFFECTS OF GARCINIA COWA BARK EXTRACT AND DOXORUBICIN ON CELL CYCLE REGULATION AND P53 EXPRESSION IN T47D BREAST CANCER CELLS
Objective: To evaluate the effects of ethanol extract of Garcinia cowa bark (EEGCB) and doxorubicin (Dox), both individually and in combination, on cell cycle regulation and protein expression in T47D breast cancer cells. Methods: T47D cells were treated with EEGCB (130 µg/ml), Dox (0.026 µg/ml), and a combination of both, and flow cytometry was used to analyze cell cycle distribution and the expression of p53, Cyclin D, and Cyclin E. Results: EEGCB induced apoptosis in T47D cells, increasing the subG1 population (p<0.0001), while Dox caused G2/M arrest (p<0.0001). Combined treatment enhanced both effects. EEGCB upregulated cyclin D/E, yet the combination reduced their expression, suggesting altered cell cycle regulation. Critically, EEGCB alone or with Dox significantly elevated p53 levels (44.6±0.592% and 37.6±1.662%, respectively; p<0.0001), implicating p53 in its anticancer activity. These results demonstrate EEGCB’s dual pro-apoptotic and cell cycle-disrupting effects, with potential chemosensitizing properties. Conclusion: These findings highlight EEGCB as a potential adjunct to conventional chemotherapy, providing a scientific basis for further exploration in breast cancer therapy.
Copyright (c) 2025 IFORA IFORA, DACHRIYANUS HAMIDI, MERI SUSANTI, FATMA S. WAHYUNI https://creativecommons.org/licenses/by/4.0
DIFFERENCES IN THE EFFECT OF APPLYING 6% AND 12% HYDROXYAPATITE PASTE FROM DUCK EGGSHELLS (ANAS PLATYRHYNCHOS) WITH CASEIN PHOSPHOPEPTIDE-AMORPHOUS CALCIUM PHOSPHATE (CPP-ACP) AS REMINERALIZING MATERIALS ON ENAMEL SURFACE HARDNESS (IN VITRO)
Objective: Dental caries has been the biggest issue in oral health resulting from the demineralization process. Demineralization can reduce the hardness of the tooth enamel surface, causing caries. The purpose of this research was to assess the difference in the effect of applying 6% and 12% hydroxyapatite paste from duck eggshells (Anas platyrhynchos) with casein phosphopeptide amorphous calcium phosphate (CPP-ACP) as remineralizing materials on enamel surface hardness. Methods: This laboratory experimental research used 30 extracted maxillary first premolars as samples, divided into 5 groups. Samples in group I were demineralized and applied with 6% hydroxyapatite paste; group II were demineralized and applied with 12% hydroxyapatite paste; group III were demineralized and applied with CPP-ACP; group IV were demineralized and not given any remineralizing materials; group V were not demineralized and not given any remineralizing materials. The demineralization procedure was done with hydrochloric acid (HCl) solution for 30 min. The remineralization procedure was done for 30 min. All samples were immersed in artificial saliva. This procedure was repeated every day for 14 consecutive days. The analysis of enamel surface hardness was done twice by Microvickers Hardness Tester, the first was after demineralization and second after remineralization. Results: T-paired test result showed an increase in enamel surface hardness after application of the test materials in each group (p<0.05). The result of the one-way ANOVA test showed the application of 6% and 12% hydroxyapatite paste from duck eggshells showed a more significant increase in enamel surface hardness than CPP-ACP paste. Although the numerical value of 12% was higher than 6%, there was no significant difference between the two based on the results of the Post-hoc Bonferroni test (p=1). Conclusion: The application of 6% hydroxyapatite paste, 12% hydroxyapatite paste, CPP-ACP and control group resulted in an increase of enamel surface hardness. The application of 6% and 12% hydroxyapatite paste from duck eggshells showed a significant increase in enamel surface hardness compared to CPP-ACP.
Copyright (c) 2025 Fitri Yunita Batubara, Widi Prasetia, Dennis Dennis, Wandania Farahanny, Nevi Yanti, Cut Nurliza, Trimurni Abidin, Mayvira Annisa, Dina Masrura, William Sahala Markus Sitompul https://creativecommons.org/licenses/by/4.0
FOCUSED INSIGHTS INTO ALZHEIMER’S TREATMENT STRATEGIES: PHARMACOPHORE MODELLING, DFT STUDIES, MD SIMULATIONS AND SH-SY5Y NEUROPROTECTION OF NARINGIN
Objective: Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder involving oxidative stress, protein aggregation, and neurotransmitter imbalance. This study aimed to evaluate the neuroprotective potential of Drynaria quercifolia (DQ) phytoconstituents, particularly DQ5 (naringin), using in silico, in vitro, and pharmacological analyses for multitargeted AD therapy. Methods: Phytocompounds from DQ were analysed through molecular docking to assess binding affinities with AD-related targets, including acetylcholinesterase (AChE), monoamine oxidase-B (MAO-B), and peroxiredoxin-5 (Prdx-5). DQ5 (naringin) was further evaluated using molecular dynamics (MD) simulations and pharmacophore modelling. Density Functional Theory (DFT) was employed to assess molecular stability and reactivity. In vitro assays measured AChE, MAO-B, tyrosinase inhibition, and hydrogen peroxide scavenging. Neuroprotective effects were evaluated using MTT assay on SH-SY5Y neuroblastoma cells. Results: Molecular docking showed strong binding of DQ5 to AChE (-14.182 kcal/mol) and MAO-B (-13.393 kcal/mol). MD simulations confirmed complex stability. DQ5 (naringin) exhibits high stability in its gas-phase optimised structure, and its small HOMO-LUMO gap indicates it may be quite reactive, which could contribute to its biological activity. DQ5 inhibited AChE (IC₅₀ = 8.05±1.02 µg/ml) and 90% SH-SY5Y cell viability. Pharmacokinetic predictions supported favourable drug-likeness and safety profiles. Conclusion: DQ5 (naringin), a key metabolite from DQ, exhibits significant multitarget activity against AD-related enzymes and oxidative stress. The compound's pharmacological properties and neuroprotective effects highlight its promise as a natural therapeutic candidate for addressing multiple pathways involved in AD pathogenesis.
Copyright (c) 2025 SINDHU T. J., JAINEY P. JAMES, ZAKIYA FATHIMA C., RAJALAKSHIMI VASUDEVAN, SHANKAR G. ALEGAON https://creativecommons.org/licenses/by/4.0
DEVELOPMENT AND EVALUATION OF BOSWELLIA-LOADED SOLID LIPID NANOPARTICLE FILMS FOR TRANSDERMAL DELIVERY IN CARRAGEENAN-INDUCED ARTHRITIS MODEL IN RATS
Objective: This study aimed to develop and evaluate a dual-purpose solid lipid nanoparticle (SLN)-chitosan/PVA matrix-based transdermal film incorporating Boswellia serrata extract for enhanced anti-arthritic activity, sustained drug release, and improved biocompatibility. Methods: Boswellia-loaded SLNs were prepared using hot homogenization at 15,000 rpm for 15 min with stearic acid as lipid and Polysorbate 80 as surfactant. The optimized nanoparticles (lipid-to-drug ratio 8:1) were embedded in a chitosan–polyvinyl alcohol (PVA) film-forming matrix. Three formulations (F1–F3) were developed and evaluated for physicochemical properties, drug content uniformity, and swelling index. Advanced techniques, including SEM, FTIR, and zeta analysis, were used for characterization. In vitro drug release was studied via the Franz diffusion cell using a cellulose acetate membrane (pH 7.4), and kinetics were modelled. Antioxidant activity was assessed via DPPH and nitric oxide assays, while anti-inflammatory effects were studied through protease, lipoxygenase, and protein-denaturation assays. Biocompatibility was tested using RAW 264.7 macrophages (MTT assay). In vivo studies included Draize-based skin irritation and carrageenan-induced paw edema models in wistar rats. Results: The F2 formulation exhibited optimal characteristics with a surface pH of 6.4, drug content uniformity of 98.3%, and a swelling index of 152.8%. Particle size distribution (PDI 0.410) and zeta potential (–29.9 mV) confirmed stability. SEM showed spherical particles with smooth surfaces. FTIR revealed characteristic drug-polymer interactions. In vitro drug release followed a biphasic pattern with an initial burst and sustained diffusion, achieving 98.38% release over 6 h. Antioxidant assays showed 89.6% DPPH and 85.9% nitric oxide inhibition. The film significantly inhibited inflammatory enzymes, with results comparable to diclofenac sodium. Cell viability remained>80% even at 200 µg/ml. No signs of dermal irritation were noted. In vivo, the film reduced paw edema by over 50% at 8 h. Conclusion: The HSLN-loaded chitosan/PVA film demonstrated biphasic drug release, potent anti-inflammatory and antioxidant activity, and excellent biocompatibility, making it a promising non-invasive therapeutic strategy for managing arthritis. The biphasic release profile offers rapid symptom relief followed by sustained action, which may reduce dosing frequency and improve patient compliance in chronic RA therapy. Further clinical investigations are warranted.
Copyright (c) 2025 SONIA K., R. VIJAYA, V. JANANI, KIRUBA MOHANDOSS https://creativecommons.org/licenses/by/4.0
DEVELOPMENT AND VALIDATION OF STABILITY-INDICATING RP-HPLC METHOD FOR SIMULTANEOUS DETERMINATION OF DORZOLAMIDE HYDROCHLORIDE AND TIMOLOL MALEATE IN OPHTHALMIC DOSAGE FORM
Objective: This new reverse phase high-performance liquid chromatography (RP-HPLC) method demonstrates superiority over the methods found in official monographs, as it is not included in the United States Pharmacopeia, British Pharmacopeia, or European Pharmacopeia (USP, B. P, Ph Eur). It effectively separates all impurities with excellent resolution from the main analyte, and the spectral purity of the main analyte was confirmed through peak purity analysis in specificity studies involving spiked sample solutions and degradation studies. According to the British Pharmacopeia, impurities B and D are associated with dorzolamide hydrochloride (DZH), while timolol maleate (TIM) includes Impurity G. The USP lists maleic acid and DZH-related compounds B and D for DZH, along with G, B, and D for TIM. Methods: Chromatographic separation was carried out on a Symmetry C8 column using buffer pH 3.0, acetonitrile, and methanol (50:40:10 v/v/v) as mobile phase, at a flow rate of 1.2 ml/min, and a step gradient elution was used. DZH and TIM were detected at 253 nm and 295 nm, respectively, with retention times of 17.6 and 28.4 min. Results: The method was found to be linear (r²>0.999) in the concentration ranges of 50-400 μg/ml for DZH and 12-100 μg/ml for TIM. It was validated for precision (both analytes %RSD = 0.3%), accuracy (recoveries 98.7-100.5%), specificity, and robustness. Forced degradation studies also showed the validity of the method with good resolution between the degradation products and the main peaks. Conclusion: The developed RP-HPLC method is novel, simple, sensitive, precise, accurate, and robust for DZH and TIM in ophthalmic formulations as per the International Council for harmonisation (ICH) for stability studies to perform Quality control (QC) of bulk and finished dosage forms.
Copyright (c) 2025 RAMAKRISHNA K., SRUJAN KUMAR M. https://creativecommons.org/licenses/by/4.0
FORMULATION AND IN VITRO CHARACTERISATION OF ATENOLOL TRANSDERMAL FILM WITH NATURAL POLYSACCHARIDE
Objective: The objective of this research work targeted to create a mechanism for transdermal drug delivery containing atenolol with natural polysaccharide and modified natural polymeric combinations, using solvent evaporation technique and to analyse how polymers affect the transdermal patches physicochemical and drug-release characteristics. Methods: Solvent casting method has been used to formulate transdermal film. Chia seed mucilage (CSM), Carboxymethylated chia seed mucilage, Hydroxypropyl methylcellulose (HPMC) and Gelatin in different combination ratios were used as the polymer. Dibutyl phthalate was chosen as a plasticizer. Results: Result showed that the thickness of all film varied from 0.0546±0.0048 to 0.073±0.0032 mm with uniformity of thickness in each formulation. The average moisture content is found to be ranging between 4.8±0.13 to 5.67±0.14%. All batches had drug contents varying between 96 to 98 percent. All batches showed folding endurance grades exceeding 120. In comparison to formulation samples F1 to F4 (62.39%, 63.03%, 41.90%, and 23.68%, respectively), formulation samples F5 and F6 showed slower cumulative drug release of 35.26% and 34.27% at 480 min. Conclusion: According to the study’s findings, modifying the polymer has an impact on the transdermal film’s physicochemical and drug-release characteristics, and formulating an efficient transdermal film requires an optimum ratio of polymer to plasticizer combination. Higher proportion of modified polymer and plasticizer in the formulation of transdermal film, gives lower percentage drug release from prepared film. Thus, it can be concluded that the increase in the ratio of plasticizer and modified CSM polymer in comparison to unmodified CSM polymer will result in retarding drug release rate.
Copyright (c) 2025 SWARNIM GUPTA, RIMA DAWN, ABHISHEK JANA, DEBARATI KAR, TATHAGATA ROY, PINTU KUMAR DE https://creativecommons.org/licenses/by/4.0
NANOEMULSION-BASED DELIVERY OF TERMINALIA ARJUNA BARK EXTRACT: SNEDDS FORMULATION, OPTIMIZATION, AND IN VIVO EVALUATION
Objective: Terminalia arjuna (T. arjuna), the stem bark of which has long been valued for its strong cardioprotective and antioxidant effects, primarily due to its diverse range of bioactive compounds. Despite its potential, its clinical use has been limited due to its poor water solubility and low oral bioavailability. Methods: In this study, an optimized Self-Nanoemulsifying Drug Delivery System (SNEDDS) of T. arjuna extract was developed to overcome these limitations and improve the oral delivery of the extract. Later, the formulation was subjected to stability analysis and preclinical analysis to check the effectiveness of the developed dosage form. Results: In this research, the SNEDDS formulation was optimized using a reference ratio of the oil (Labrafil), surfactant (Tween 80), and co-surfactant (Transcutol P). The resulting formulation displayed a globule size of 325.66 nm, a polydispersity index (PDI) of 0.252, and a zeta potential of-29.7 mV. The results of the in vivo study showed significant improvements for all groups compared to the control. The standard drug and high-dose SNEDDS groups had the most pronounced effects, while the crude extract and low-dose SNEDDS (500 mg/kg) showed milder responses. The SNEDDS formulation of T. arjuna enhanced both efficacy and safety, highlighting its potential for improving the bioavailability of natural extracts. Conclusion: Overall, the SNEDDS approach is a promising method for enhancing the therapeutic effectiveness of T. arjuna, particularly in managing cardiovascular conditions.
Copyright (c) 2025 PANKAJ, MANISH VYAS, SANJEEV KUMAR SAHU, PALWINDER KAUR https://creativecommons.org/licenses/by/4.0
FORMULATION AND OPTIMIZATION OF A GALLIC ACID-LOADED NAIL SERUM USING FACTORIAL DESIGN FOR ENHANCED NAIL DELIVERY
Objective: Onychomycosis is a persistent fungal infection of the nails, and conventional treatments, including oral antifungals, are often associated with systemic side effects, such as hepatotoxicity, and exhibit high recurrence rates. In response to these challenges, the present project aimed to develop a novel gallic acid-loaded nail serum, a unique approach that leverages the antifungal, antioxidant, and anti-inflammatory properties of gallic acid to formulate a safer and more efficacious topical treatment than conventional therapy. Methods: The formulations were developed using a 2³ factorial design approach to optimize the concentrations of acetone, ethyl acetate, and glycerol for desired viscosity and spreadability. The serum was evaluated for its physical characteristics, viscosity, spreadability, in vitro drug permeation, antifungal activity, and in vitro cytocompatibility using the MTT assay on L929 fibroblast cells, as well as its ex vivo efficacy in a porcine hoof model. Results: The optimized formulation showed appropriate viscosity (755.67 cP) and spreadability (7.22 cm), along with smooth texture, good gloss, and a pH suitable for nails (pH 5.2–5.4). Drug permeation studies revealed that the serum enhanced gallic acid penetration more than an aqueous solution. Antifungal studies showed a better zone of inhibition (22.0±0.5 mm) compared to a marketed antifungal product. Cytocompatibility studies indicated more than 88% cell viability. Ex vivo analysis confirmed significant fungal clearance on infected hoof models. Conclusion: The gallic acid-loaded nail serum developed in this study demonstrated effective antifungal activity, enhanced nail penetration, and favorable physical properties, It offers a natural, safe, and patient-friendly alternative to conventional antifungal treatments for onychomycosis, encouraging further clinical research and potential commercial development.
Copyright (c) 2025 JANE GLENISHA LOBO, JOEL SYLVESTER SALDANHA, DIYA POLALI, JENITTA MARIA CARMEL, ASHWINI MADHAVA https://creativecommons.org/licenses/by/4.0
INVESTIGATING THE ROLE OF PROBIOTICS AND SHORT-CHAIN FATTY ACIDS (SCFAs) IN MODULATING LEPTIN FOR IMPROVED ANTI-DIABETIC EFFECTS IN STREPTOZOTOCIN-NICOTINAMIDE INDUCED TYPE II DIABETES IN RATS
Objective: The gut microbiota, such as Lactobacillus rhamnosus and Bifidobacteriumlongum produces short-chain fatty acids like acetate, propionate, and butyrate from fermentation of undigested fiber, holds promise for managing metabolic diseases, including type II diabetes and obesity. This study explores the potential of probiotics and short-chain fatty acids to modulate leptin for increased anti-diabetic action in rats, offering hope for future diabetes management strategies. Methods: Rats weighing 150 and 200 g were chosen for the study, divided into multiple groups, and given a single dose of nicotinamide and streptozotocin to induce type II diabetes. Probiotics, butyrate, propionate, and glibenclamide were continually given to respective groups after the induction of Type II diabetes. Every week, the animal's body weight was determined. Following the study's conclusion, blood was drawn via retro-orbital puncture to test the following parameters: insulin, leptin, lipid, liver, and kidney profiles. Liver and pancreas were isolated for histopathological analysis. Results: In rats with type II diabetes, fasting blood glucose levels were significantly increased (p<0.001) compared with the normal control group, accompanied by a marked reduction in fasting insulin and leptin levels (p<0.001). Treatment with selected probiotics, butyrate, and propionate caused a significant reduction in blood glucose (p<0.001) and a significant increase in fasting insulin and leptin levels (p<0.001), indicating improved pancreatic function relative to diabetic controls. Diabetic rats displayed severe diabetic dyslipidaemia, with elevated atherogenic lipoproteins and reduced HDL-C (p<0.001). Administration of probiotics, butyrate, and propionate led to a significant reduction in atherogenic lipid levels (p<0.01) and a marked increase in HDL-C compared with diabetic controls. Liver and kidney function markers were significantly elevated in diabetic control rats (p<0.01), whereas these elevations were notably reduced (p<0.01) in all treatment groups. Among these, the combination of butyrate and probiotics exhibited the most pronounced therapeutic benefits (p<0.001 vs. other treatments). Histopathological evaluation revealed severe hepatic and pancreatic abnormalities in diabetic controls, whereas treatment groups exhibited restoration of normal tissue architecture. Notably, butyrate-treated rats showed prominent β-cell hyperplasia and hypertrophy, further supporting enhanced pancreatic regeneration and overall therapeutic efficacy. Conclusion: This finding suggested that butyrate, in combination with probiotics, has more anti-diabetic effects than individual treatment by increasing the levels of Leptin. These results could potentially lead to the development of novel therapeutic strategies for managing type II diabetes.
Copyright (c) 2025 P. RAJYALAKSHMI DEVI, MOTE SRINATH, B. MAHESHWARI REDDY, KOPPALA R. V. S CHAITANYA, M. VINYAS https://creativecommons.org/licenses/by/4.0
A COMPREHENSIVE REVIEW OF VARIOUS ANALYTICAL METHOD AVAILABLE FOR THE DETERMINATION OF FOOD COLOURS CONSIDERING DIFFERENT REGULATORY ASPECTS
Food additives have been an integral part since ancient times in the preservation and enhancement of food. Ancient civilization had evolved from simple preservation techniques to sophisticated synthetic compounds that transformed over thousands of years. This review article focuses on various food additives such as: acidity regulators, emulsifying and stabilizing agents, antioxidants, colorants, flavouring agents, leavening agents, bulking agents, and preservatives. Particular emphasis is placed on the colorants in food and divided it into three main categories: natural, nature-identical, and synthetic. Food colours have a different regulatory framework across all the countries. However, few differences have been seen among FDA of United States, EFSA of European Union, and FSSAI of India. India has approved only nine synthetic colour additives while the FDA allows 19, EU allows food colours of 43 altogether-natural and synthetic. The analytical techniques employed for the analysis of food colours are validated HPLC, UV-Visible spectrophotometry, and Mass spectrometry methods. Coupled Ultra-High-Performance Liquid Chromatography (UHPLC) with tandem mass spectrometry (MS/MS) techniques have led to highly sensitive methods for determination of food colours in different food matrices. For this reason, the understanding of such analytical methods has ensured compliance toward regulatory limits; Inturn, food safety standards within the global food chain supply.
Copyright (c) 2025 KRISHNAVENI NAGAPPAN, SHARAN RAJ RAJMOHAN, MOHIT ANANDA, AISWARYA MAHENDRAN, BALAGEE MUTHUKUMAR, PADMA PRIYA V. https://creativecommons.org/licenses/by/4.0
UNLOCKING AVOCADO’S POTENTIAL: EXPLORING PREBIOTIC-INFUSED CELLULOSE MATRICES FOR PROBIOTIC STABILITY ENHANCEMENT
The stability and effectiveness of probiotics in functional foods and nutritional supplements are considerably influenced by their ability to survive harsh stomach conditions. The escalating interest in gut microbiome modulation has propelled the use of probiotics and prebiotics in functional food development. Avocados, rich in fibre and prebiotic properties, constitute an ideal basis for supporting the growth of the advantageous intestinal microbiota. The combination of prebiotics derived from the layer with cellulose matrices has shown improved probiotic survival rates, increased intestinal colonization, and an improvement in health benefits in preliminary studies. This new approach not only improves the stability of probiotics but also offers a further prebiotic effect that supports intestinal health. A schematic diagram illustrates the interplay between avocado-derived prebiotics, probiotics, and gut microbiota, enhancing conceptual clarity. The results suggest that this synergy could play a crucial role in the development of more effective and stable probiotic products for the nutraceutical and functional food industry. Future research must focus on the optimization of formulations, conducting large-scale clinical tests, and long-term benefits of these improved probiotic delivery systems. Future research should focus on personalized formulations and large-scale clinical validation to substantiate their therapeutic potential.
Copyright (c) 2025 JATIN M., BISHOP ADHIKARI, ALIN BOSE J., PIYUSH KUMAR, RAMAN RAJESHKUMAR https://creativecommons.org/licenses/by/4.0
AN OVERVIEW OF BILAYER TABLET TECHNOLOGY: DESIGN, MANUFACTURING, AND THERAPEUTIC APPLICATIONS
Bilayer tablets are innovative drug delivery systems designed to enhance therapeutic efficacy by enabling the simultaneous or sequential release of active pharmaceutical ingredients. They offer distinct advantages in managing diseases requiring combination therapy or controlled release. This system enables the incorporation of two different drugs or release profiles within a single unit, enhancing patient compliance and therapeutic outcomes. Bilayer tablets are particularly beneficial for drugs with narrow therapeutic windows, those requiring sustained release, or those with poor bioavailability. This review outlines the formulation strategies, types of bilayer tablets, manufacturing challenges, evaluation parameters, and current regulatory considerations.
Copyright (c) 2025 VEERENDRA UMESH DHOKE, SHUBHAM S. GUPTA, BHAGYASHRI R. DHAKATE, RAKSHA PUROHIT, PRIYANKA A. MANDAL, SHUBHAM KAMBLE https://creativecommons.org/licenses/by/4.0
ADVANCEMENTS IN LIPID-BASED NANOTHERANOSTICS FOR MANAGING ATHEROSCLERO-SIS: A REVIEW
Atherosclerosis, a complicated and chronic inflammatory disorder, is the main cause of various cardiovascular issues, including coronary heart assaults and strokes. Acute myocardial infarction and stroke can be partially prevented with current clinical measures, such as statin medications, but the risk is still very high. The concept of combinatorial therapy using both diagnosis and therapeutics through a single platform is known as theranostics. As evident from pre-clinical and clinical studies, nano-based theranostics are widely used in cancer detection and treatment. Solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), and nanoliposomes are examples of synthetic/natural lipid-based delivery systems that have drawn much interest as nano-scaled drug delivery system due to their potential benefits, which include easy large-scale production, relatively low toxicity, and composition accessibility. Traditionally, for the study and evaluate the effects of therapy on atherosclerosis, x-ray angiography was used. Nevertheless, measuring the amount of stenosis brought on by plaques remains the main objective of clinical studies for atherosclerosis. Several high-risk plaque features, such as a thin fibrous cap, a big necrotic core, macrophage infiltration, neovascularization, and intraplaque bleeding, can now be investigated using cutting-edge imaging methods. This review summarises nanotheranostic for diagnosing and treating atherosclerosis and the different strategies for targeting atherosclerotic plaque.
Copyright (c) 2025 MANIGANDAN DHORAI, IMRANKHAN NIZAM, KALAISLEVI ASAITHAMBI, GOWTHAMARJAN KUPPUSAMY https://creativecommons.org/licenses/by/4.0
NANOTECHNOLOGY IN PAEDIATRIC DRUG DELIVERY: ADVANCES, CHALLENGES, AND REGULATORY CONSIDERATIONS-A REVIEW
Children's growth and physiology are basically different from that of adults, so paediatric pharmacotherapy is dissimilar in challenge. The traditional formulations of medicines are not suitable for children, as they face issues of poor taste, insusceptibility of dosage flexibility, and potential miscalculation of dosage. Nanotechnology of nanoscale dimensions holds great promise in solving paediatric drug delivery issues. In this article, the prospect of nanocarriers, such as liposomes, polymeric nanoparticles, and solid lipid nanoparticles, is discussed in paediatric medicine. Nanoformulations have been found to increase oral bioavailability by 60% and decrease dosing frequency by 50%, with improved therapeutic response in paediatric patients. Today, at least four FDA-approved nanoformulations are on the market for paediatric applications, such as liposomal amphotericin B for fungal infections and pegylated liposomal doxorubicin for paediatric oncology, showing the increasing clinical use of nanotechnology in paediatric medicine. However, there are huge challenges remaining: long-term safety of nanomaterials in developing organisms, scalable manufacturing, regulatory hurdles, and ethical considerations for paediatric clinical trials. The review will highlight the continued need for interdisciplinarity to overcome the challenges and reach the potential of nanotechnology for enhancing paediatric health outcomes. Future directions include stimuli-responsive and personalized nanocarriers, combination therapy, and theranostic nanoparticles. With further research and development, nanotechnology can potentially revolutionize paediatric pharmacotherapy with more effective, safer, and patient-compliant drug delivery.
Copyright (c) 2025 Gowtham AA, Giridhara M, Gurubaran S, Sanjai Rajagopal, Nagasamy Venkatesh Dhandapani https://creativecommons.org/licenses/by/4.0
ORGANIC ORIGIN GLUCIDES ALDITOLS AS CARRIERS FOR OPTIMIZING SOLUBILIZATION AND DRUG RELEASE
Organic-origin glucides and alditols-such as glucose, fructose, lactose, xylitol, erythritol, and maltitol-have demonstrated notable potential in enhancing the dissolution rate and solubility of sparingly water-soluble drugs when incorporated as carriers in solid dispersions (SDs). Although synthetic polymers are widely used in the design of SD formulations, they have major disadvantages including the tendency to recrystallize during storage, higher viscosity, and redundant bulk in the final dosage forms. On the other hand, naturally derived carriers with low molecular weight offer certain advantages, such as high-water affinity, good thermal behavior, and better molecular interaction, and do not suffer from the disadvantage of increasing the bulk of the dosage form. Here, we focus on the characteristics of glucides and alditols that make them favorable substitutes for those based on polymers as core carriers, as outlined in this review. We also discuss organic historical studies, new solutions, and prospects for using these compounds to improve the solubility and release of highly hydrophobic pharmaceutical ingredients.
Copyright (c) 2025 MOHAMMED A. AMIN, MOSTAFA A. MOHAMED, DALIA A. GABER, HEBA ALI SOLIMAN https://creativecommons.org/licenses/by/4.0
PHYTOSOME TECHNOLOGY IN CANCER TREATMENT ENHANCES THE BIOAVAILABILITY OF SECONDARY METABOLITES
Phytosome technology represents a major breakthrough in the delivery of plant-derived secondary metabolites for cancer therapy, addressing fundamental limitations such as poor aqueous solubility, rapid metamorphosis, and reduced bioavailability, which hinders clinical translation. The secondary metabolites flavonoids, terpenoids, alkaloids, and phenolic resins exhibit potent anticancer activities by modulating crucial oncogenic nerve pathways e.g., NF-κB (Nuclear Factor kappa-light-chain-enhancer of activated B cells), PI3K (Phosphoinositide 3-kinase), causing apoptosis and inhibiting angiogenesis. However, their hydrophobic nature and volatility in the physiological environment limit their curative efficacy. Phytosomes, which are molecular complexes containing phytochemicals and phospholipids, increase lipid solubility, prevent bioactive compounds from degrading, and facilitate target delivery to the tumor, resulting in refined absorption, dispersed circulation, and reduced systemic toxicity. Preclinical studies have shown that phytosome encapsulation can increase anticancer activity by up to fivefold and synergizes with conventional chemotherapeutics, resulting in increased efficacy in breast and colorectal tumor models. This review critically examines the structural and mechanistic foundations of phytosome technology, its application in improving the pharmacokinetics and therapeutic indices of secondary metabolites, and recent innovations, including nanoparticle incorporation and codelivery systems. By integrating metabolomic profiling with nanocarrier design, phytosomes hold promise as a cornerstone for next-generation, natural product-based precision oncology, overcoming bioavailability barriers and potentiating anticancer effects to advance clinical translation.
Copyright (c) 2025 MUJIBULLAH SHEIKH, ZOYA SHEIKH, ARFANA SHEIKH, MAHIN KHAN, VAISHNAVI SHETE https://creativecommons.org/licenses/by/4.0
RECENT ADVANCES IN NANOCARRIERS FOR TARGETED CANCER THERAPY
One treatment option is detailed re-evaluating cancer for a very innovative and efficacious form of therapy. Nanocarrier-based delivery systems have offered an impetus in the form of targeted cancer drug delivery under better drug solubility, controlled release, and selective accumulation in tumour tissue. This review intends to address the major advances in applying nanocarrier-based cancer treatment, such as liposomes, polymeric nanoparticles, dendrimers, micelles, and carbon-and inorganic nanoparticle-based medication. Every type of nanocarrier has very clear and peculiar features that determine the increase in bioavailability and tumour targeting through passive (enhanced permeability retention effect) and active targeting (ligand-receptor interactions, pH-sensitive mechanisms, and stimuli-responsive drug release). Nanocarriers, including liposomes, polymeric nanoparticles, dendrimers, and micelles, have shown significant promise in targeted cancer therapy due to their ability to improve drug solubility, prolong circulation time, and enhance site-specific delivery while minimising systemic toxicity. Among the various platforms discussed, polymeric nanoparticles-particularly those utilising biodegradable polymers like PLGA-emerged as the most promising due to their tunable surface properties, sustained drug release profiles, and favorable biocompatibility. Despite their advantages, challenges such as biological heterogeneity, off-target accumulation, and regulatory barriers hinder clinical translation. Future efforts should focus on developing smart nanocarriers capable of stimuli-responsive release and patient-specific adaptability to overcome these limitations. The future of cancer therapy can, therefore, be expected to see a fantastic horizon in patient outcomes with the integration of such innovative platforms coming from nanocarrier with personalized medicine approaches.
Copyright (c) 2025 MAYUR R. DANDEKAR, UMESH B. TELRANDHE, YASH SALVE, ISHA MIRZAPURE https://creativecommons.org/licenses/by/4.0
NANOTECHNOLOGY REVOLUTION IN TREATING VULVOVAGINAL CANDIDIASIS: A BREAKTHROUGH BEYOND CONVENTIONAL THERAPIES
Vulvovaginal candidiasis is an extremely common infection; millions of women all over the world are affected. The main etiologic agent responsible for its development is Candida albicans. It is characterize by burning, itching and the presence of a thick and white discharge. VVC may be divided into two categories: simple and complex. Recurring forms of the disease pose difficult challenges to clinical management. An ability to form Candida biofilms on vaginal mucosa may be one of the reasons for the development of resistant infections, further increasing resistance towards treatment. The complications in managing infection due to the constantly rising resistance of Candida to commonly used antifungal drugs call for alternative therapies. The conventional methods of treatments, which include topical and oral antifungals, too often result in limited success with recurrence or side effects against such resistant strains. Nanotechnology therefore presents a promising alternative, as Nano-drug delivery systems enhance localized drug delivery by allowing more precise targeting of fungal cells. It can, therefore, overcome the resistance and deficiencies of the conventional mode of therapy. Various studies continue in nano medicine to develop better therapies in order to handle VVC with better outcome and management.
Copyright (c) 2025 Devanth D Gowda, Sharanya Paramshetti, Mohit Angolkar, Darshan Patil, Asha Spandana KM https://creativecommons.org/licenses/by/4.0
HARNESSING ARTIFICIAL INTELLIGENCE: TRANSFORMING CLINICAL TRIALS FOR THE FUTURE
To evaluate the impact of artificial intelligence (AI) technologies on clinical trial processes, identify quantitative benefits, and determine areas requiring further research. A comprehensive literature review was conducted examining AI applications across clinical trial phases. The study analysed machine learning (ML), natural language processing (NLP), computer vision, reinforcement learning (RL), and other AI technologies as applied to clinical research processes. AI implementations have delivered substantial quantitative benefits across various aspects of clinical trials (CT). International Business Machine (IBM) Watson enabled an 80% increase in patient accrual to breast cancer trials within just 11 mo. In silico medicine’s generative tensorial reinforcement learning (GENTRL) platform accelerated the drug discovery timeline by a factor of 15, reducing it to just 46 days. Saama Technologies' deep learning (DL) approach detected 30% more anomalous data cases compared to traditional methods. Pfizer’s use of AI-driven quantitative systems pharmacology (QSP) models led to a 60% reduction in Phase 2 dose cohorts. AiCure’s AI-powered monitoring system achieved 25% higher medication adherence and completed trials 30% faster. Meanwhile, Unlearn. AI’s digital twin technology enabled a 30% reduction in control group size without compromising statistical power. These outcomes highlight AI’s powerful role in improving the efficiency, speed, and quality of CT. AI is trans formatively enhancing CT through improved recruitment efficiency, protocol optimization, data quality management, and patient monitoring. However, challenges remain in data quality, algorithm interpretability, regulatory compliance, workflow integration, and bias mitigation. Future research should focus on advanced predictive modelling, explainable AI development, federated learning for privacy preservation, AI-human collaboration models, real-world data integration, and standardized validation procedures. Ethical considerations and regulatory frameworks specifically addressing AI in CT require further development to realize the full potential of these technologies.
Copyright (c) 2025 MOHAN KUMAR MAHADEVAPPA, GONNA NANDI KRISHNAN, VIVEK REDDY MURTHANNAGARI, JANA ARUN https://creativecommons.org/licenses/by/4.0
NANO-ENABLED THERAPEUTICS: EXPLORING BIOEQUIVALENCE AND BIOAVAILABILITY FRONTIERS
The advancement of nanotechnology has significantly transformed pharmaceutical sciences, especially in enhancing the bioavailability and bioequivalence (BE) of drugs with poor solubility and permeability. Nanoparticulate drug delivery systems including nanoparticles, nanocrystals, nanoemulsions, and liposomes exhibit unique physicochemical properties such as increased surface area, improved dissolution rates, and enhanced permeability. These characteristics collectively contribute to superior therapeutic efficacy. For example, a 25-fold increase in the bioavailability of poorly soluble drugs such as retinoic acid has been reported by the use of solid lipid nanoparticles (SLNs), which act as protective lipid matrices, augmenting drug stability and allowing sustained release. This comprehensive review explores the fundamental concepts of bioavailability and BE as they pertain to nanoformulations, focusing on key factors that influence the absorption, distribution, metabolism, and excretion of nanosized drugs. It emphasizes the mechanistic pathways by which nanocarriers overcome biological barriers, including the gastrointestinal (GI) tract and first-pass metabolism, thereby improving pharmacokinetic (PK) profiles. Furthermore, the review discusses analytical methodologies and regulatory considerations critical to evaluating the BE of nanoformulated drugs. It highlights challenges in establishing equivalency arising from altered pharmacokinetic and pharmacodynamic (PD) behaviors unique to these formulations. A comparative analysis of conventional versus nanoformulated drugs illustrates the clinical implications of nanotechnology in drug delivery, such as dose reduction, improved patient compliance, and minimized adverse effects. Additionally, recent advancements in formulation strategies and characterization techniques are synthesized, showcasing how surface modifications, size optimization, and targeting moieties enhance oral bioavailability. By evaluating preclinical and clinical studies, this article provides valuable insights into the translational potential of nanoformulations. It also identifies existing gaps and future directions in regulatory frameworks and standardized BE testing. In summary, this review offers a holistic understanding of nanotechnology’s role in improving drug bioavailability and BE, serving as an essential resource for pharmaceutical scientists, clinicians, and regulatory authorities aiming to leverage nanoformulations for enhanced therapeutic outcomes. Despite notable progress, significant challenges remain especially in achieving scalable manufacturing, ensuring reproducibility of formulations and navigating complex regulatory landscapes. These challenges stress on the urgent need for internationally harmonized standards and robust quality control systems to support clinical translation.
Copyright (c) 2025 ARAVINDA PAI, CHANDRASHEKAR K. S., BHAVANA BHAT B., VIDHI ANSUL SAXENA, VENKATESH KAMATH B. https://creativecommons.org/licenses/by/4.0
REGULATORY RELIANCE PATHWAYS: OPPORTUNITIES, CHALLENGES AND FUTURE DIRECTIONS
Regulatory reliance allows national agencies to use assessments from trusted regulators instead of repeating the same work. This accelerates approvals, decreases workload, and allows patients to receive safe and effective medications more quickly. Many countries use different forms of reliance procedures, such as work-sharing, mutual recognition, abridged, and verification. These methods are common in regions like the European Union, the United Kingdom, South Africa, and Latin America. Various programs like Project Orbis and The World Health Organization’s (WHO) Collaborative Registration Procedure have reduced review times through collaboration between countries, thereby minimizing resource use and enabling work-sharing. Project Orbis and the Access Consortium have shown the importance of collaborative efforts and their essentiality when dealing with life-threatening diseases. Numerous countries in the Middle East and Asia have used these reliance methods to streamline regulatory processes particularly in public health emergencies. In South African countries, the impact is a 68% reduction in time with regulatory reliance as compared to regular processes. Additionally, the reliance guidelines of WHO initiated the UK’s International Recognition Procedure. During the COVID-19 pandemic regulatory reliance played a pivotal role and facilitated rapid vaccination approvals through international collaboration. Some challenges exist, such as unclear legislation, concerns about independence and legal limitations. Future research should focus on standardizing legislation, modernizing technology like the use of AI-driven evaluations, and improving collaboration as they help to strengthen global coordination to respond to emergencies more promptly. This article explains the reliance pathway and how regulatory decisions from trusted agencies help low-and middle-income countries.
Copyright (c) 2025 GURRAM GNANESHWARI, KIRAN NAGARAJ, SHAILEE DEWAN, VIGNESH MANOHARAN, PRADEEP MANOHAR MURAGUNDI https://creativecommons.org/licenses/by/4.0
MOLECULAR AND EPIGENETIC MECHANISMS OF COVID-19-RELATED CARDIOVASCULAR COMPLICATIONS: MULTIOMICS BIOMARKERS AND PRECISION MEDICINE APPROACHES
COVID-19 has emerged as a significant precipitant of acute cardiovascular complications, collectively termed COVID-19-associated acute cardiovascular syndrome. Approximately one-third of hospitalized patients experience myocardial injury, with elevated cardiac troponins correlating with disease severity and mortality. The pathogenesis involves direct viral invasion of cardiomyocytes and endothelial cells via the ACE2 receptor, immune-mediated inflammation (notably cytokine storm), endothelial dysfunction, and prothrombotic states. These mechanisms are further modulated by genetic and epigenetic factors, including DNA methylation changes and host genetic polymorphisms, which influence individual susceptibility to cardiac complications. Multiomics integration—encompassing microRNA expression, exosomal biomarkers, glycomic profiling, and genomic data—has enabled the identification of novel molecular signatures for risk stratification and therapeutic targeting. For instance, specific miRNA signatures have been shown to predict responsiveness to anti-inflammatory therapies, offering the potential to personalize treatment strategies based on individual molecular profiles. Classic biomarkers such as high-sensitivity troponins, NT-proBNP, and myoglobin, alongside emerging molecular and epigenetic markers, provide valuable insights into the mechanisms linking SARS-CoV-2 infection to myocardial injury, arrhythmia, and long-term cardiovascular sequelae. This review synthesizes current evidence on the molecular, genetic, and epigenetic underpinnings of COVID-19-related cardiovascular disease, highlighting the promise of precision medicine approaches for early diagnosis, prognostication, and targeted intervention in post-COVID-19 cardiovascular risk management.
Copyright (c) 2025 KETAKI DAWALE, PANKAJ JAMBHOLKAR, VASANT WAGH https://creativecommons.org/licenses/by/4.0
ADVANCED NANOCARRIERS FOR OCULAR DRUG DELIVERY: STRATEGIES TO OVERCOME OCULAR BARRIERS
Ocular drug delivery is confronted with significant challenges because of the eye's specific anatomy and physiological barriers, including the blood-retinal and corneal epithelium. Traditional dose formulations often experienced rapid precorneal clearance and low absorption. Recent advances in nanotechnology, such as liposomes, cubosomes, glycerosomes, nano wafers, microneedles, vectors for gene therapy, olaminosomes, bilosomes, and exosomes, offer promising alternatives to bypass these limitations. These techniques facilitate longer ocular retention, controlled release, targeted distribution, enhanced drug solubility, and improved patient compliance. For instance, glycerosomes and nanoliposomes enhance permeability and biocompatibility; nanogels and cubosomes have structural advantages for drug stabilization and sensitivity; microneedles offer a minimally invasive approach to achieve epithelial barriers; exosomes enable targeted bioactivity and intracellular delivery; and olaminosomes, which are made of lipid-based vesicles and oleylamine, offer great entrapment efficiency and corneal adherence. In contrast, bilosomes, which incorporate bile salts, improve corneal permeability. The present work provides comprehensive insights into nanocarrier approaches for improving ocular bioavailability, along with related patents and clinical trials in this field.
Copyright (c) 2025 DIVYA, RUPA MAZUMDER, ANJNA RANI, RAKHI MISHRA https://creativecommons.org/licenses/by/4.0