Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo

Xingyan Liu1, Hong Liu1, Jianqiang Liu2, Zhiwei He1, Congcong Ding1, Guoliang Huang1, Weihua Zhou3, Leshan Zhou31China-America Cancer Research Institute, of Guangdong Medical College, 2School of Pharmacy, Guangdong Medical College, Dongguan, Guangdong, People&rsquo;s Republic of China; 3Cent...

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Autores principales:	Xingyan Liu1 Hong Liu, Jianqiang Liu, Zhiwei He, et al
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/7defe5bf98ae47f096781b13825c86fe
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spelling	oai:doaj.org-article:7defe5bf98ae47f096781b13825c86fe2021-12-02T02:06:14ZPreparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo1176-91141178-2013https://doaj.org/article/7defe5bf98ae47f096781b13825c86fe2011-01-01T00:00:00Zhttp://www.dovepress.com/preparation-of-a-ligustrazine-ethosome-patch-and-its-evaluation-in-vit-a6161https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Xingyan Liu1, Hong Liu1, Jianqiang Liu2, Zhiwei He1, Congcong Ding1, Guoliang Huang1, Weihua Zhou3, Leshan Zhou31China-America Cancer Research Institute, of Guangdong Medical College, 2School of Pharmacy, Guangdong Medical College, Dongguan, Guangdong, People&rsquo;s Republic of China; 3Central South University, Changsha, Hunan, People&rsquo;s Republic of ChinaBackground: The purpose of this study was to develop a transdermal ligustrazine patch containing a stable formulation and with good entrapment efficiency, release rate, and transdermal absorption.Methods: Ligustrazine ethosomes were prepared by ethanol injection-sonication, with entrapment efficiency as an indicator. Using acrylic resin as the primary constituent, the ligustrazine ethosome patch was prepared by adding succinic acid as a crosslinking agent and triethyl citrate as a plasticizer. In vitro release and transdermal permeation studies were carried out. Finally, a pharmacokinetic study was carried out in rats to explore relative bioavailability. The formulations of ligustrazine ethosome were 1% (w/v) phospholipid, 0.4% (w/v) cholesterol, and 45% (v/v) ethanol.Results: Ligustrazine ethosomes were obtained with an average particle size of 78.71 &plusmn; 1.23 nm and an average entrapment efficiency of 86.42% &plusmn; 1.50%. In vitro transdermal testing of the ligustrazine ethosome patches showed that the cumulative 24-hour amount of ligustrazine was up to 183 &plusmn; 18 &micro;g/cm2. The pharmacokinetic results revealed that the relative bioavailability was 209.45%.Conclusion: Compared with conventional ligustrazine administration, ligustrazine ethosome patches could promote better drug absorption and increase bioavailability. This study demonstrates that the transdermal action of the ligustrazine ethosome patch was comparatively good.Keywords: ligustrazine, ethosomes, patch Xingyan Liu1 Hong LiuJianqiang LiuZhiwei Heet alDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 241-247 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Xingyan Liu1 Hong Liu Jianqiang Liu Zhiwei He et al Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo
description	Xingyan Liu1, Hong Liu1, Jianqiang Liu2, Zhiwei He1, Congcong Ding1, Guoliang Huang1, Weihua Zhou3, Leshan Zhou31China-America Cancer Research Institute, of Guangdong Medical College, 2School of Pharmacy, Guangdong Medical College, Dongguan, Guangdong, People&rsquo;s Republic of China; 3Central South University, Changsha, Hunan, People&rsquo;s Republic of ChinaBackground: The purpose of this study was to develop a transdermal ligustrazine patch containing a stable formulation and with good entrapment efficiency, release rate, and transdermal absorption.Methods: Ligustrazine ethosomes were prepared by ethanol injection-sonication, with entrapment efficiency as an indicator. Using acrylic resin as the primary constituent, the ligustrazine ethosome patch was prepared by adding succinic acid as a crosslinking agent and triethyl citrate as a plasticizer. In vitro release and transdermal permeation studies were carried out. Finally, a pharmacokinetic study was carried out in rats to explore relative bioavailability. The formulations of ligustrazine ethosome were 1% (w/v) phospholipid, 0.4% (w/v) cholesterol, and 45% (v/v) ethanol.Results: Ligustrazine ethosomes were obtained with an average particle size of 78.71 &plusmn; 1.23 nm and an average entrapment efficiency of 86.42% &plusmn; 1.50%. In vitro transdermal testing of the ligustrazine ethosome patches showed that the cumulative 24-hour amount of ligustrazine was up to 183 &plusmn; 18 &micro;g/cm2. The pharmacokinetic results revealed that the relative bioavailability was 209.45%.Conclusion: Compared with conventional ligustrazine administration, ligustrazine ethosome patches could promote better drug absorption and increase bioavailability. This study demonstrates that the transdermal action of the ligustrazine ethosome patch was comparatively good.Keywords: ligustrazine, ethosomes, patch
format	article
author	Xingyan Liu1 Hong Liu Jianqiang Liu Zhiwei He et al
author_facet	Xingyan Liu1 Hong Liu Jianqiang Liu Zhiwei He et al
author_sort	Xingyan Liu1 Hong Liu
title	Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo
title_short	Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo
title_full	Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo
title_fullStr	Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo
title_full_unstemmed	Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo
title_sort	preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/7defe5bf98ae47f096781b13825c86fe
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Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo

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