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

BACKGROUND: 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 efficien...

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Autores principales: Liu, Xingyan, Liu, Hong, Liu, Jianqiang, He, Zhiwei, Ding, Congcong, Huang, Guoliang, Zhou, Weihua, Zhou, Leshan
Formato: Texto
Lenguaje:English
Publicado: Dove Medical Press 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3075898/
https://www.ncbi.nlm.nih.gov/pubmed/21499422
http://dx.doi.org/10.2147/IJN.S16044
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author Liu, Xingyan
Liu, Hong
Liu, Jianqiang
He, Zhiwei
Ding, Congcong
Huang, Guoliang
Zhou, Weihua
Zhou, Leshan
author_facet Liu, Xingyan
Liu, Hong
Liu, Jianqiang
He, Zhiwei
Ding, Congcong
Huang, Guoliang
Zhou, Weihua
Zhou, Leshan
author_sort Liu, Xingyan
collection PubMed
description BACKGROUND: 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 ± 1.23 nm and an average entrapment efficiency of 86.42% ± 1.50%. In vitro transdermal testing of the ligustrazine ethosome patches showed that the cumulative 24-hour amount of ligustrazine was up to 183 ± 18 μg/cm(2). 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.
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spelling pubmed-30758982011-04-15 Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo Liu, Xingyan Liu, Hong Liu, Jianqiang He, Zhiwei Ding, Congcong Huang, Guoliang Zhou, Weihua Zhou, Leshan Int J Nanomedicine Original Research BACKGROUND: 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 ± 1.23 nm and an average entrapment efficiency of 86.42% ± 1.50%. In vitro transdermal testing of the ligustrazine ethosome patches showed that the cumulative 24-hour amount of ligustrazine was up to 183 ± 18 μg/cm(2). 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. Dove Medical Press 2011 2011-01-27 /pmc/articles/PMC3075898/ /pubmed/21499422 http://dx.doi.org/10.2147/IJN.S16044 Text en © 2011 Liu et al, publisher and licensee Dove Medical Press Ltd. This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.
spellingShingle Original Research
Liu, Xingyan
Liu, Hong
Liu, Jianqiang
He, Zhiwei
Ding, Congcong
Huang, Guoliang
Zhou, Weihua
Zhou, Leshan
Preparation of a ligustrazine ethosome patch and its evaluation in vitro and in vivo
title 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_short 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
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3075898/
https://www.ncbi.nlm.nih.gov/pubmed/21499422
http://dx.doi.org/10.2147/IJN.S16044
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