DEVELOPMENT OF ANTI-RETROVIRAL DRUG LOADED SOLID -LIPID NANOPARTICLES

Authors

  • ANITA H. PAGAR Department of Pharmaceutics, MGV’S Pharmacy College, Panchavati, Nashik-422003, Maharashtra State, Affiliated to Savitribai Phule Pune University, Pune, India https://orcid.org/0009-0008-7706-0139
  • ASHISH Y. PAWAR Department of Pharmaceutics, MGV’S Pharmacy College, Panchavati, Nashik-422003, Maharashtra State, Affiliated to Savitribai Phule Pune University, Pune, India https://orcid.org/0000-0002-2532-7064
  • SANTOSH R. TAMBE Department of Pharmaceutics, MGV’S Pharmacy College, Panchavati, Nashik-422003, Maharashtra State, Affiliated to Savitribai Phule Pune University, Pune, India

DOI:

https://doi.org/10.22159/ijap.2026v18i3.56189

Keywords:

Solid lipid nanoparticles, Antiretroviral drug delivery, Nanocarriers controlled release, Drug encapsulation, In vitro drug release, High shear homogenization, HIV therapy, Drug targeting

Abstract

Objective: This project aims to develop and evaluate solid lipid nanoparticles (SLNs) of an antiviral drug to improve bioavailability, reduce dosing frequency, and enhance patient compliance. SLNs offer a nanocarrier system that addresses the poor solubility, low oral bioavailability, and systemic side effects associated with conventional antiretroviral therapy.

Methods: SLNs of dolutegravir were prepared using high shear homogenization followed by ultrasonication. Biocompatible lipids such as glyceryl monostearate were used as the lipid matrix, and Poloxamer 188 served as the stabilizer. To optimize the formulation, lipid content, surfactant type, concentration, and sonication parameters were systematically varied. The prepared formulations were evaluated for particle size, zeta potential, drug entrapment efficiency, and in-vitro drug release profile to determine the optimum conditions for SLN development.

Results: The optimized solid lipid nanoparticle (SLN) formulation exhibited a particle size in the range of 257–412 nm with a negative zeta potential (ZP), indicating good physical stability and low aggregation tendency. A high drug entrapment efficiency (%EE) (>85%) confirmed effective incorporation of the drug within the lipid matrix. In vitro release studies demonstrated a biphasic release pattern, characterized by an initial burst release followed by sustained drug release over 24 hours. Differential Scanning Colorimetry (DSC) and Fourier Trasform Infrared Spectrocopy (FTIR) analyses revealed no significant drug–lipid interactions, confirming formulation compatibility. Transmission Electron Microscopy (TEM) analysis showed spherical nanoparticles with smooth surfaces and uniform morphology. Overall, the formulation displayed desirable physicochemical and release characteristics suitable for sustained drug delivery.

Conclusion: The study demonstrates that solid lipid nanoparticles (SLNs) are a promising delivery system for antiretroviral drugs, offering sustained release, improved pharmacokinetic behavior, and reduced dosing frequency. However, further in vivo studies are required to confirm their therapeutic efficacy and biodistribution profile.

References

1. UNAIDS. World AIDS Day 2022: global HIV & AIDS statistics – fact sheet. UNAIDS. 2023.

2. Deeks SG, Lewin SR, Havlir DV. The end of AIDS: HIV infection as a chronic disease. Lancet. 2013;382(9903):1525-33.

3. Sharma A, Jadhav S. Drug delivery strategies for improving the bioavailability of antiretroviral drugs. J Control Release. 2015;219:679-94.

4. Scioli Montoto S, Muraca G, Ruiz ME. Solid lipid nanoparticles for drug delivery: pharmacological and biopharmaceutical aspects. Front Mol Biosci. 2020;7:587997.

5. Dening TJ, Rao S, Thomas N, Prestidge CA. Novel nanostructured solid materials for modulating oral drug delivery from solid-state lipid-based drug delivery systems. AAPS J. 2016;18(1):23-40.

6. Doktorovova S, Souto EB. Nanostructured lipid carrier-based hydrogel formulations for drug delivery: a comprehensive review. Expert Opin Drug Deliv. 2009;6(2):165-76.

7. Pandey R, Sharma A, Zahoor A, Sharma S, Khuller GK, Prasad B. Poly(DL-lactide-co-glycolide) nanoparticle-based inhalable sustained drug delivery system for experimental tuberculosis. J Antimicrob Chemother. 2003;52(6):981-6.

8. Sanna V, Pala N, Sechi M. Targeted therapy using nanotechnology: focus on cancer. Int J Nanomedicine. 2014;9:467-83.

9. Chandni SV, Viral S, Umesh U. Solid lipid nanoparticles: a review. J Curr Pharm Res. 2011;1(4):351-8.

10. Hou D, Xie C, Huang K, Zhu C. The production and characteristics of solid lipid nanoparticles (SLNs). Biomaterials. 2003;24(10):1781-5.

11. Prabhakaran E, Hasan A, Karunanidhi P. Solid lipid nanoparticles: a review. Sci Rev Chem Commun. 2012;2:80-102.

12. Castelli F, Puglia C, Sarpietro MG, Rizza L, Bonina F. Characterization of indomethacin-loaded lipid nanoparticles by differential scanning calorimetry. Int J Pharm. 2005;304(1-2):231-8.

13. Padhye SG, Nagarsenker MS. Simvastatin solid lipid nanoparticles for oral delivery: formulation development and in vivo evaluation. Indian J Pharm Sci. 2013;75(5):591-8.

14. Joshy KS, Sharma CP, Kalarikkal N, Sandeep K, Thomas S, Pothen LA. Evaluation of in vitro cytotoxicity and cellular uptake of zidovudine-loaded solid lipid nanoparticles modified with Aloe vera in glioma cells. Mater Sci Eng C Mater Biol Appl. 2016;66:40-50.

15. Shaikh NA, Lala RR. Formulation development of dolutegravir sodium loaded nanolipid carriers for improved solubility and permeability. Int J Pharm Sci Res. 2021;12:3654-65.

16. Singh S, Dobhal AK, Jain A, Pandit JK, Chakraborty S. Formulation and evaluation of solid lipid nanoparticles of a water-soluble drug: zidovudine. Chem Pharm Bull (Tokyo). 2010;58(5):650-5.

17. Nachammai K, Nair KG, Velmurugan R, Pavithra KS. Sustained-release study on mefenamic acid and mosapride loaded solid lipid nanoparticles: in vitro characterization. Res J Pharm Technol. 2020;13(11):5391-8.

18. Manjunath K, Venkateswarlu V. Pharmacokinetics, tissue distribution and bioavailability of clozapine solid lipid nanoparticles after intravenous and intraduodenal administration. J Control Release. 2005;107(2):215-28.

19. Kamarullah W, Indrajaya E, Emmanuella J. Potency of luteolin with solid lipid nanoparticle-PEG modification for artemisinin-resistant Plasmodium falciparum infection. Indones J Trop Infect Dis. 2018;7(3):80-5.

20. Al Haj NA, Abdullah R, Ibrahim S, Bustamam A. Tamoxifen drug-loaded solid lipid nanoparticles prepared by hot high-pressure homogenization technique. Am J Pharmacol Toxicol. 2008;3(3):219-24.

21. Shi F, Zhao JH, Liu Y, Wang Z, Zhang YT, Feng NP. Preparation and characterization of solid lipid nanoparticles loaded with frankincense and myrrh oil. Int J Nanomedicine. 2012;7:2033-43.

22. Iqbal A, Zaman M, Amjad MW, Adnan S, Raja MAG, Rizvi SFH, et al. Solid lipid nanoparticles of mycophenolate mofetil: an attempt to control the release of an immunosuppressant. Int J Nanomedicine. 2020;15:5603-12.

23. Babu VN, Rao GS, Budha RR, Alavala RR, Desu PK, Babu GK, et al. Development, characterization and optimization of solid lipid nanoparticles of alpha-mangostin by central composite design approach. J Appl Pharm Sci. 2023;13(8):140-50.

24. Mendoza-Muñoz N, Urbán-Morlán Z, Leyva-Gómez G, Zambrano-Zaragoza ML, Quintanar-Guerrero D. Solid lipid nanoparticles: an approach to improve oral drug delivery. Int J Pharm Pharm Sci. 2021;24:509–532.

25. Dudhat K. Novel nanoparticulate systems for idiopathic pulmonary fibrosis: a review. Asian J Pharm Clin Res. 2020;13(11).

Published

23-03-2026

How to Cite

PAGAR, A. H., PAWAR, A. Y., & TAMBE, S. R. (2026). DEVELOPMENT OF ANTI-RETROVIRAL DRUG LOADED SOLID -LIPID NANOPARTICLES. International Journal of Applied Pharmaceutics, 18(3). https://doi.org/10.22159/ijap.2026v18i3.56189

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