Comparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery

Susan HuaThe School of Biomedical Sciences and Pharmacy, The University of Newcastle, Callaghan, NSW, AustraliaBackground: The purpose of this study was to determine the most appropriate dialysis equilibrium method to assess liposomal gel formulations containing hydrophobic drugs, to give the most...

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Autor principal:	Hua S
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/8e9a0c3a312b42afb440a307888a2aae
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spelling	oai:doaj.org-article:8e9a0c3a312b42afb440a307888a2aae2021-12-02T08:08:33ZComparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery1178-2013https://doaj.org/article/8e9a0c3a312b42afb440a307888a2aae2014-01-01T00:00:00Zhttp://www.dovepress.com/comparison-of-in-vitro-dialysis-release-methods-of-loperamide-encapsul-a15664https://doaj.org/toc/1178-2013 Susan HuaThe School of Biomedical Sciences and Pharmacy, The University of Newcastle, Callaghan, NSW, AustraliaBackground: The purpose of this study was to determine the most appropriate dialysis equilibrium method to assess liposomal gel formulations containing hydrophobic drugs, to give the most accurate indication of drug release.Methods: Loperamide hydrochloride-encapsulated liposomes, composed of L-α-phosphatidylcholine and cholesterol (molar ratio of 2:1), were prepared according to the method of dried lipid film hydration. The liposomes were incorporated into a carbopol gel (0.5%, weight/weight). The release of the drug from the nanoparticles was assessed using a number of variations of the dialysis technique, taking into account solubility parameters and formulation. Method 1 (below saturation point) and Method 2 (above saturation point) used a dilution method to evaluate how drug concentration and solubility affects the in vitro drug-release profile of loperamide hydrochloride, while Methods 3 (below saturation point) and 4 (above saturation point) evaluated how drug concentration and the gel base affect the release profile.Results: In Method 1, the liposomes showed a rapid release of just over 60% in the first 3 hours and then a slower, sustained release to just over 70% at 24 hours. Method 2 showed a gradual, sustained release profile with the liposomes with 55% release at 24 hours. In Method 3, the liposomes showed a rapid burst release of 98% at 2 hours. In Method 4, the liposomal gel had a rapid release of 60% within 3 hours and then a more gradual, sustained release with 86% release at 24 hours. The free drug suspension in Methods 2 and 4 showed a limited release across the dialysis membrane, in comparison to Methods 1 and 3, which showed a complete release in a timely manner.Conclusion: This study has demonstrated that the actual method used for equilibrium dialysis plays a significant role in determining the true characteristics of a topical nanoformulation, with Method 3 providing the most accurate indication of the release of a hydrophobic drug from a topical liposomal formulation.Keywords: liposomes, gel, in vitro drug release, transdermal, topical, loperamideHua SDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 735-744 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Hua S Comparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery
description	Susan HuaThe School of Biomedical Sciences and Pharmacy, The University of Newcastle, Callaghan, NSW, AustraliaBackground: The purpose of this study was to determine the most appropriate dialysis equilibrium method to assess liposomal gel formulations containing hydrophobic drugs, to give the most accurate indication of drug release.Methods: Loperamide hydrochloride-encapsulated liposomes, composed of L-α-phosphatidylcholine and cholesterol (molar ratio of 2:1), were prepared according to the method of dried lipid film hydration. The liposomes were incorporated into a carbopol gel (0.5%, weight/weight). The release of the drug from the nanoparticles was assessed using a number of variations of the dialysis technique, taking into account solubility parameters and formulation. Method 1 (below saturation point) and Method 2 (above saturation point) used a dilution method to evaluate how drug concentration and solubility affects the in vitro drug-release profile of loperamide hydrochloride, while Methods 3 (below saturation point) and 4 (above saturation point) evaluated how drug concentration and the gel base affect the release profile.Results: In Method 1, the liposomes showed a rapid release of just over 60% in the first 3 hours and then a slower, sustained release to just over 70% at 24 hours. Method 2 showed a gradual, sustained release profile with the liposomes with 55% release at 24 hours. In Method 3, the liposomes showed a rapid burst release of 98% at 2 hours. In Method 4, the liposomal gel had a rapid release of 60% within 3 hours and then a more gradual, sustained release with 86% release at 24 hours. The free drug suspension in Methods 2 and 4 showed a limited release across the dialysis membrane, in comparison to Methods 1 and 3, which showed a complete release in a timely manner.Conclusion: This study has demonstrated that the actual method used for equilibrium dialysis plays a significant role in determining the true characteristics of a topical nanoformulation, with Method 3 providing the most accurate indication of the release of a hydrophobic drug from a topical liposomal formulation.Keywords: liposomes, gel, in vitro drug release, transdermal, topical, loperamide
format	article
author	Hua S
author_facet	Hua S
author_sort	Hua S
title	Comparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery
title_short	Comparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery
title_full	Comparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery
title_fullStr	Comparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery
title_full_unstemmed	Comparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery
title_sort	comparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/8e9a0c3a312b42afb440a307888a2aae
work_keys_str_mv	AT huas comparisonofinvitrodialysisreleasemethodsofloperamideencapsulatedliposomalgelfortopicaldrugdelivery
_version_	1718398613036466176

Comparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery

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