DESIGN AND OPTIMIZATION OF ACYCLOVIR LOADED SOLID LIPID NANOPARTICLES: A SUSTAINED RELEASE APPROACH
DOI:
https://doi.org/10.22159/ijap.2025v17i1.51877Keywords:
ASLN, Acyclovir, Drug delivery, Zero-order kinetics, Sustained releaseAbstract
Objective: This study aims to develop Acyclovir-Loaded Solid Lipid Nanoparticles (ASLN) prepared through homogenisation and evaluate their efficacy.
Methods: ASLN were formulated using Gelucire 43/01, Polyvinylpyrrolidone (PVP), Tween 80, and Stearic acid in varying ratios through solvent evaporation and homogenisation. Lipids and Acyclovir were melted together and then emulsified using a homogeniser. Particle size distribution was assessed by Dynamic Light Scattering (DLS), and Zeta Potential was measured using electrophoretic mobility. The cumulative drug release profile was analyzed to determine sustained release characteristics. Zero-order kinetic modelling was applied to elucidate the release mechanism, indicating diffusion rate-limited drug release. Comparative studies with marketed Acyclovir formulations were conducted to assess efficacy and performance.
Results: All formulations exhibited satisfactory characteristics: Particle size of 185.6±4.28 nm, Zeta potential of-24.15±5.43 mV, Polydispersity Index of 0.192±3.11, and Drug Entrapment Efficiency of 77.06±4.3%. In vitro release studies of ASLN formulation F12 showed prolonged drug release (90.88% cumulative release by the 8th hour), in sustained drug availability. Comparative studies highlighted the efficacy of ASLN compared to commercial acyclovir products. The kinetic analysis confirmed zero-order kinetics and diffusion rate-limited drug release for all formulations.
Conclusion: In conclusion, the formulation of ASLN using Gelucire 43/01, Polyvinylpyrrolidone (PVP), Tween 80, and Stearic acid produced nanoparticles with favourable characteristics. These included appropriate particle size, zeta potential, and high drug entrapment efficiency. In vitro studies demonstrated sustained drug release, suggesting ASLN as promising carriers for enhancing Acyclovir's therapeutic efficacy.
Downloads
References
Mahmood S, Kiong KC, Tham CS, Chien TC, Hilles AR, Venugopal JR. Pegylated lipid polymeric nanoparticle encapsulated acyclovir for in vitro controlled release and ex vivo gut sac permeation. AAPS Pharm Sci Tech. 2020;21(7):285. doi: 10.1208/s12249-020-01810-0, PMID 33057878.
Delshadi R, Bahrami A, McClements DJ, Moore MD, Williams L. Development of nanoparticle delivery systems for antiviral agents: a review. J Control Release. 2021 Mar 10;331:30-44. doi: 10.1016/j.jconrel.2021.01.017, PMID 33450319.
Hassan H, Bello RO, Adam SK, Alias E, Meor Mohd Affandi MM, Shamsuddin AF. Acyclovir loaded solid lipid nanoparticles: optimization characterization and evaluation of its pharmacokinetic profile. Nanomaterials (Basel). 2020;10(9):1785. doi: 10.3390/nano10091785, PMID 32916823.
Pandey M, Choudhury H, Abdul Aziz A, Bhattamisra SK, Gorain B, SU JS. Advancement on sustained antiviral ocular drug delivery for herpes simplex virus keratitis: recent update on potential investigation. Pharmaceutics. 2020;13(1):1. doi: 10.3390/pharmaceutics13010001, PMID 33374925.
Kondel R, Shafiq N, Kaur IP, Singh MP, Pandey AK, Ratho RK. Effect of acyclovir solid lipid nanoparticles for the treatment of herpes simplex virus (HSV) infection in an animal model of HSV-1 infection. Pharm Nanotechnol. 2019;7(5):389-403. doi: 10.2174/2211738507666190829161737, PMID 31465287.
Seyfoddin A, Al Kassas R. Development of solid lipid nanoparticles and nanostructured lipid carriers for improving ocular delivery of acyclovir. Drug Dev Ind Pharm. 2013;39(4):508-19. doi: 10.3109/03639045.2012.665460, PMID 22424312.
Kukhanova MK, Korovina AN, Kochetkov SN. Human herpes simplex virus: life cycle and development of inhibitors. Biochemistry (Mosc). 2014;79(13):1635-52. doi: 10.1134/S0006297914130124, PMID 25749169.
El Assal MI. Acyclovir loaded solid lipid nanoparticle-based cream: a novel drug delivery system. Int J Drug Deliv Technol. 2017;7(1):52-62. doi: 10.25258/ijddt.v7i1.8917.
Alsaad A, Hussien A, Ghareeb M. Solid lipid nanoparticles (SLN) as a novel drug delivery system: a theoretical review. Syst Rev Pharm. 2020;11(5):259-73. doi: 10.31838/srp.2020.5.39.
German Cortes J, Vilar Hernandez M, Rafael D, Abasolo I, Andrade F. Solid lipid nanoparticles: multitasking nano-carriers for cancer treatment. Pharmaceutics. 2023;15(3):831. doi: 10.3390/pharmaceutics15030831, PMID 36986692, PMCID PMC10056426.
Beloqui A, Solinis MA, Gascon AR, Del Pozo Rodriguez A, Des Rieux A, Preat V. Mechanism of transport of saquinavir loaded nanostructured lipid carriers across the intestinal barrier. J Control Release. 2013;166(2):115-23. doi: 10.1016/j.jconrel.2012.12.021, PMID 23266764.
Gill S, Lobenberg R, KU T, Azarmi S, Roa W, Prenner EJ. Nanoparticles: characteristics mechanisms of action and toxicity in pulmonary drug delivery a review. J Biomed Nanotechnol. 2007;3(2):107-19. doi: 10.1166/jbn.2007.015.
Jenning V, Thunemann AF, Gohla SH. Characterisation of a novel solid lipid nanoparticle carrier system based on binary mixtures of liquid and solid lipids. Int J Pharm. 2000;199(2):167-77. doi: 10.1016/s0378-5173(00)00378-1, PMID 10802410.
Choi KO, Aditya NP, KO S. Effect of aqueous pH and electrolyte concentration on structure stability and flow behavior of non ionic surfactant based solid lipid nanoparticles. Food Chem. 2014 Mar 15;147:239-44. doi: 10.1016/j.foodchem.2013.09.095, PMID 24206712.
El Gizawy SA, El Maghraby GM, Hedaya AA. Formulation of acyclovir loaded solid lipid nanoparticles: design optimization and in vitro characterization. Pharm Dev Technol. 2019;24(10):1287-98. doi: 10.1080/10837450.2019.1667385, PMID 31507232.
Karpe M, Mali N, Kadam V. Formulation development and evaluation of acyclovir orally disintegrating tablets. J Appl Pharm Sci. 2012 Mar;2(3). doi: 10.7324/JAPS.2012.2317.
Madkhali OA. Perspectives and prospective on solid lipid nanoparticles as drug delivery systems. Molecules. 2022;27(5):1543. doi: 10.3390/molecules27051543, PMID 35268643.
Mahmood A, Ahmad M, Sarfraz RM, Minhas MU, Yaqoob A. Formulation and in vitro evaluation of acyclovir loaded polymeric microparticles: a solubility enhancement study. Acta Pol Pharm. 2016;73(5):1311-24. PMID 29638071.
Nugrahani I, Mussadah MV. Development and validation analysis of acyclovir tablet content determination method using FTIR. Int J Appl Pharm. 2016;8(3):43-7. doi: 10.22159/ijap.2016v8i3.12946.
SG, Chandrakala V, Srinivasan S. Development and evaluation of microsponge gel of an antifungal drug. Int J Curr Pharm Sci. 2023;15(1):30-41. doi: 10.22159/ijcpr.2023v15i1.2069.
Parthiban R, Sathishkumar S, Surendhar S, Ramakrishnan P. Design and evaluation of acyclovir loaded solid lipid nanoparticles for sustained release. Drug Invent Today. 2020;14(1):108.
Bhatnagar A, Bhatnagar E. Evaluation of a combination of gingival physiotherapy flossing and brushing technique through in-office observation. Int J Curr Pharm Sci. 2023;15(3):34-6. doi: 10.22159/ijcpr.2023v15i3.3007.
Rajadhyax A, Shinde U, Desai H, Mane S. Hot melt extrusion in engineering of drug cocrystals: a review. Asian J Pharm Clin Res. 2021;14(8):10-9. doi: 10.22159/ajpcr.2021.v14i8.41857.
Gupta B, Sharma R. Formulation and in vitro characterization of the solid lipid nanoparticles of naftopidil for enhancing oral bioavailability. Asian J Pharm Clin Res. 2023;16(2):77-82. doi: 10.22159/ajpcr.2023.v16i2.46465.
Phalak SD, Bodke V, Yadav R, Pandav S, Ranaware M. A systematic review on nano drug delivery system: solid lipid nanoparticles (SLN). Int J Curr Pharm Sci. 2024;16(1):10-20. doi: 10.22159/ijcpr.2024v16i1.4020.
Published
How to Cite
Issue
Section
Copyright (c) 2025 DEEVAN PAUL AMARNATH
This work is licensed under a Creative Commons Attribution 4.0 International License.