FORMULATION AND OPTIMIZATION OF BIOACTIVE-LOADED POLYMERIC NANOPARTICLE – QUALITY BY DESIGN (QBD) STRATEGY EMPLOYING CENTRAL COMPOSITE DESIGN
DOI:
https://doi.org/10.22159/ajpcr.2025v18i11.56023Keywords:
Resveratrol, Poly(lactic-co-glycolic acid),, Nanoparticles, Quality by design,, Drug delivery, Bioavailability.Abstract
Objective: This study aimed to apply a quality by design (QbD) framework, utilizing central composite design (CCD), to systematically develop and optimize resveratrol-loaded polymeric nanoparticles. The overarching goal was to enhance the solubility, stability, and bioavailability of resveratrol, thereby improving its anti-depressant activity.
Methods: Resveratrol nanoparticles were formulated using the solvent evaporation technique, incorporating poly(lactic-co-glycolic acid) (PLGA) as the biodegradable polymer and Poloxamer 188 as the stabilizing surfactant. High-shear homogenization was employed to ensure uniform particle formation. The nanoparticles were subsequently freeze-dried and characterized for key physicochemical parameters, including particle size, polydispersity index (PDI), zeta potential (ZP), encapsulation efficiency (EE), and in vitro drug release profile.
Results: The CCD trial formulations containing PLGA and Poloxamer 188 at 60–80 mg and 2–3% concentration, respectively, exhibited particle sizes ranging from 236 to 461 nm with narrow size distribution (PDI: 0.15–0.22), and ZP values between −25 and −30 mV, indicating stable colloidal systems. EE varied from 60% to 90%, depending on the formulation variables. In vitro release studies demonstrated a prolonged drug release pattern, with approximately 97% of resveratrol released over a 48-h period. Based on the outcome of the optimization tool, PLGA and Poloxamer 188 were selected at a concentration of 63.56 mg and 2.20%, respectively, and the average particle size at 295.3±8.96 nm, PDI (0.19±0.01), EE (80.33±1.53), zetapotential (−27.00±1.00), and cumulative drug release was 99.33±1.15% for 48 h.
Conclusion: The QbD-driven development approach enabled the successful formulation of resveratrol-loaded PLGA nanoparticles with enhanced physicochemical and release properties. This nanoformulation offers a promising strategy for improving the bioavailability and therapeutic efficacy of resveratrol, supporting its potential application in clinical settings.
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1. Kalidas S, Geetha P. Development and optimization of astragalin-loaded polymeric nanoparticles using central composite factorial design. Int J Appl Pharm. 2022;15(5):69-77. doi: 10.22159/ijap.2022v14i5.44315
2. Aqil F, Munagala R, Jeyabalan J, Vadhanam MV. Bioavailability of phytochemicals and its enhancement by drug delivery systems. Cancer Lett. 2013;334(1):133-41. doi: 10.1016/j.canlet.2013.02.032, PMID 23435377
3. Jain AK, Thareja S. In vitro and in vivo characterization of pharmaceutical nanocarriers used for drug delivery. Artif Cells Nanomed Biotechnol. 2019;47(1):524-39. doi: 10.1080/21691401.2018.1561457, PMID 30784319
4. Prabhu RH, Patravale VB, Joshi MD. Polymeric nanoparticles for targeted treatment in oncology: Current insights. Int J Nanomedicine. 2015;10:1001-18. doi: 10.2147/IJN.S56932, PMID 25678788
5. Biswas R, Kapat P, Ghosh A, Sarkhel S, Sarkar T, Das D. Pharmaceutical polymers in drug delivery: An overview. Int J Pharm Pharm Sci. 2025;17(7):1-8. doi: 10.22159/ijpps.2025v17i7.54498
6. Borgheti-Cardoso LN, Viegas JS, Silvestrini AV, Caron AL, Praça FG, Kravicz M, et al. Nanotechnology approaches in the current therapy of skin cancer. Adv Drug Deliv Rev. 2020;153:109-36. doi: 10.1016/j. addr.2020.02.005, PMID 32113956
7. Saha M, Saha DR, Ulhosna T, Sharker SM, Shohag MH, Islam MS, et al. QbD based development of resveratrol-loaded mucoadhesive lecithin/ chitosan nanoparticles for prolonged ocular drug delivery. J Drug Deliv Sci Technol. 2021;63:102480. doi: 10.1016/j.jddst.2021.102480
8. Chung JH, Lee JS, Lee HG. Resveratrol-loaded chitosan–γ-poly (glutamic acid) nanoparticles: Optimization, solubility, UV stability, and cellular antioxidant activity. Colloids Surf B Biointerfaces. 2020;186:110702. doi: 10.1016/j.colsurfb.2019.110702, PMID 31862561
9. Ramalingam P, Ko YT. Improved oral delivery of resveratrol from N-trimethyl chitosan-g-palmitic acid surface-modified solid lipid nanoparticles. Colloids Surf B Biointerfaces. 2016;139:52-61. doi: 10.1016/j.colsurfb.2015.11.050, PMID 26700233
10. Eltaib L. Polymeric nanoparticles in targeted drug delivery: Unveiling the impact of polymer characterization and fabrication. Polymers (Basel). 2025;17(7):833. doi: 10.3390/polym17070833, PMID 40219222
11. Jyothi D, Priya S, James JP. Development and optimization of polymeric nanoparticles of glycyrrhizin: Physicochemical characterizationand antioxidant activity. Int J Appl Pharm. 2024;16:166-71. doi: 10.22159/ ijap.2024v16i1.49164
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