Central composite design for formulation and optimization of solid lipid nanoparticles to enhance oral bioavailability of Acyclovir

Treatment of herpes simplex infection requires high and frequent doses of oral acyclovir to attain its maximum therapeutic effect. The current therapeutic regimen of acyclovir is known to cause unwarranted dose-related adverse effects, including acute kidney injury. For this reason, a suitable deliv...

Full description

Bibliographic Details
Main Authors: Hassan, Haniza, Adam, Siti Khadijah, Alias, Ekram, Meor Mohd Affandi, Meor Mohd Redzuan, Shamsuddin, Ahmad Fuad, Basir, Rusliza
Format: Article
Published: Multidisciplinary Digital Publishing Institute 2021
_version_ 1825937693329063936
author Hassan, Haniza
Adam, Siti Khadijah
Alias, Ekram
Meor Mohd Affandi, Meor Mohd Redzuan
Shamsuddin, Ahmad Fuad
Basir, Rusliza
author_facet Hassan, Haniza
Adam, Siti Khadijah
Alias, Ekram
Meor Mohd Affandi, Meor Mohd Redzuan
Shamsuddin, Ahmad Fuad
Basir, Rusliza
author_sort Hassan, Haniza
collection UPM
description Treatment of herpes simplex infection requires high and frequent doses of oral acyclovir to attain its maximum therapeutic effect. The current therapeutic regimen of acyclovir is known to cause unwarranted dose-related adverse effects, including acute kidney injury. For this reason, a suitable delivery system for acyclovir was developed to improve the pharmacokinetic limitations and ultimately administer the drug at a lower dose and/or less frequently. In this study, solid lipid nanoparticles were designed to improve the oral bioavailability of acyclovir. The central composite design was applied to investigate the influence of the materials on the physicochemical properties of the solid lipid nanoparticles, and the optimized formulation was further characterized. Solid lipid nanoparticles formulated from Compritol 888 ATO resulted in a particle size of 108.67 ± 1.03 nm with an entrapment efficiency of 91.05 ± 0.75%. The analyses showed that the optimum combination of surfactant and solid lipid produced solid lipid nanoparticles of good quality with controlled release property and was stable at refrigerated and room temperature for at least 3 months. A five-fold increase in oral bioavailability of acyclovir-loaded solid lipid nanoparticles was observed in rats compared to commercial acyclovir suspension. This study has presented promising results that solid lipid nanoparticles could potentially be used as an oral drug delivery vehicle for acyclovir due to their excellent properties.
first_indexed 2024-03-06T11:03:23Z
format Article
id upm.eprints-96316
institution Universiti Putra Malaysia
last_indexed 2024-03-06T11:03:23Z
publishDate 2021
publisher Multidisciplinary Digital Publishing Institute
record_format dspace
spelling upm.eprints-963162023-01-31T02:00:06Z http://psasir.upm.edu.my/id/eprint/96316/ Central composite design for formulation and optimization of solid lipid nanoparticles to enhance oral bioavailability of Acyclovir Hassan, Haniza Adam, Siti Khadijah Alias, Ekram Meor Mohd Affandi, Meor Mohd Redzuan Shamsuddin, Ahmad Fuad Basir, Rusliza Treatment of herpes simplex infection requires high and frequent doses of oral acyclovir to attain its maximum therapeutic effect. The current therapeutic regimen of acyclovir is known to cause unwarranted dose-related adverse effects, including acute kidney injury. For this reason, a suitable delivery system for acyclovir was developed to improve the pharmacokinetic limitations and ultimately administer the drug at a lower dose and/or less frequently. In this study, solid lipid nanoparticles were designed to improve the oral bioavailability of acyclovir. The central composite design was applied to investigate the influence of the materials on the physicochemical properties of the solid lipid nanoparticles, and the optimized formulation was further characterized. Solid lipid nanoparticles formulated from Compritol 888 ATO resulted in a particle size of 108.67 ± 1.03 nm with an entrapment efficiency of 91.05 ± 0.75%. The analyses showed that the optimum combination of surfactant and solid lipid produced solid lipid nanoparticles of good quality with controlled release property and was stable at refrigerated and room temperature for at least 3 months. A five-fold increase in oral bioavailability of acyclovir-loaded solid lipid nanoparticles was observed in rats compared to commercial acyclovir suspension. This study has presented promising results that solid lipid nanoparticles could potentially be used as an oral drug delivery vehicle for acyclovir due to their excellent properties. Multidisciplinary Digital Publishing Institute 2021 Article PeerReviewed Hassan, Haniza and Adam, Siti Khadijah and Alias, Ekram and Meor Mohd Affandi, Meor Mohd Redzuan and Shamsuddin, Ahmad Fuad and Basir, Rusliza (2021) Central composite design for formulation and optimization of solid lipid nanoparticles to enhance oral bioavailability of Acyclovir. Molecules, 26 (18). art. no. 5432. pp. 1-19. ISSN 1420-3049 https://www.mdpi.com/1420-3049/26/18/5432 10.3390/molecules26185432
spellingShingle Hassan, Haniza
Adam, Siti Khadijah
Alias, Ekram
Meor Mohd Affandi, Meor Mohd Redzuan
Shamsuddin, Ahmad Fuad
Basir, Rusliza
Central composite design for formulation and optimization of solid lipid nanoparticles to enhance oral bioavailability of Acyclovir
title Central composite design for formulation and optimization of solid lipid nanoparticles to enhance oral bioavailability of Acyclovir
title_full Central composite design for formulation and optimization of solid lipid nanoparticles to enhance oral bioavailability of Acyclovir
title_fullStr Central composite design for formulation and optimization of solid lipid nanoparticles to enhance oral bioavailability of Acyclovir
title_full_unstemmed Central composite design for formulation and optimization of solid lipid nanoparticles to enhance oral bioavailability of Acyclovir
title_short Central composite design for formulation and optimization of solid lipid nanoparticles to enhance oral bioavailability of Acyclovir
title_sort central composite design for formulation and optimization of solid lipid nanoparticles to enhance oral bioavailability of acyclovir
work_keys_str_mv AT hassanhaniza centralcompositedesignforformulationandoptimizationofsolidlipidnanoparticlestoenhanceoralbioavailabilityofacyclovir
AT adamsitikhadijah centralcompositedesignforformulationandoptimizationofsolidlipidnanoparticlestoenhanceoralbioavailabilityofacyclovir
AT aliasekram centralcompositedesignforformulationandoptimizationofsolidlipidnanoparticlestoenhanceoralbioavailabilityofacyclovir
AT meormohdaffandimeormohdredzuan centralcompositedesignforformulationandoptimizationofsolidlipidnanoparticlestoenhanceoralbioavailabilityofacyclovir
AT shamsuddinahmadfuad centralcompositedesignforformulationandoptimizationofsolidlipidnanoparticlestoenhanceoralbioavailabilityofacyclovir
AT basirrusliza centralcompositedesignforformulationandoptimizationofsolidlipidnanoparticlestoenhanceoralbioavailabilityofacyclovir