Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion

Zhaowu Zeng1, Guanglin Zhou1, Xiaoli Wang2, Eric Zhijian Huang1, Xiaori Zhan1, Jun Liu1, Shuling Wang1, Anming Wang1, Haifeng Li1, Xiaolin Pei1, Tian Xie11Research Center for Biomedicine and Health, Hangzhou Normal University, Hangzhou, Zhejiang, China; 2Yichun University of Jiangxi Province, Yichun...

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Autores principales:	Zhaowu Zeng, Guanglin Zhou, Xiaoli Wang, et al
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2010
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/65616d710fd649e582b56064b3368c30
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spelling	oai:doaj.org-article:65616d710fd649e582b56064b3368c302021-12-02T08:08:31ZPreparation, characterization and relative bioavailability of oral elemene o/w microemulsion1176-91141178-2013https://doaj.org/article/65616d710fd649e582b56064b3368c302010-08-01T00:00:00Zhttp://www.dovepress.com/preparation-characterization-and-relative-bioavailability-of-oral-elem-a5007https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Zhaowu Zeng1, Guanglin Zhou1, Xiaoli Wang2, Eric Zhijian Huang1, Xiaori Zhan1, Jun Liu1, Shuling Wang1, Anming Wang1, Haifeng Li1, Xiaolin Pei1, Tian Xie11Research Center for Biomedicine and Health, Hangzhou Normal University, Hangzhou, Zhejiang, China; 2Yichun University of Jiangxi Province, Yichun, Jiangxi, ChinaAbstract: The objective was to develop an elemene oil/water (o/w) microemulsion and evaluate its characteristics and oral relative bioavailability in rats. Elemene was used as the oil phase and drug, polysorbate 80 as a surfactant along with ethanol, propylene glycol, and glycerol as the cosurfactants. The microemulsion was prepared by mixing method, or ultrasonication method in an ultrasonic bath. Its three-dimensional response surface diagram was drawn by Mathcad software. The microemulsion was characterized by visual observation, cross-polarized microscopy, size, zeta potential, acidity, viscosity, and surface tension measurement. The drug content and entrapment efficiency were determined by ultra fast liquid chromatography (UFLC) and liquid surface method. Blood was drawn from rats at different time points after oral administration of an elemene microemulsion or a commercial elemene emulsion for measurement of the drug in plasma by UFLC to establish the pharmacokinetic parameters and relative bioavailability. The elemene microemulsion as a clarified and isotropic system containing 1% elemene (w/v), 5% ethanol (v/v), 15% propylene glycol (v/v), 15% glycerol (v/v), and 5% polysorbate 80 (w/v), was characterized as (57.7 &plusmn; 2.8) nm in size, 0.485 &plusmn; 0.032 in polydispersity index, (3.2 &plusmn; 0.4) mv in zeta potential, (5.19 &plusmn; 0.08) in pH, 6 mpa&bull;s in viscosity, (31.8 &plusmn; 0.3) mN&bull;m-1 in surface tension, (8.273 &plusmn; 0.018) mg&bull;mL-1 in content of &szlig;-elemene, and (99.81 &plusmn; 0.24)% in average entrapment efficiency. The area under the concentration-time curves from 0 h to 24 h (AUC0&rarr;24h) of the elemene microemulsion and commercial elemene emulsion were integrated to be 3.092 mg&bull;h&bull;L-1 and 1.896 mg&bull;h&bull;L-1 respectively, yielding a relative bioavailability of 163.1%. The present study demonstrates the elemene microemulsion as a new formulation with ease of preparation, high entrapment efficiency, excellent clarity, good stability, and improved bioavailability.Keywords: elemene, microemulsion, relative bioavailability Zhaowu ZengGuanglin ZhouXiaoli Wanget alDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2010, Iss default, Pp 567-572 (2010)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Zhaowu Zeng Guanglin Zhou Xiaoli Wang et al Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion
description	Zhaowu Zeng1, Guanglin Zhou1, Xiaoli Wang2, Eric Zhijian Huang1, Xiaori Zhan1, Jun Liu1, Shuling Wang1, Anming Wang1, Haifeng Li1, Xiaolin Pei1, Tian Xie11Research Center for Biomedicine and Health, Hangzhou Normal University, Hangzhou, Zhejiang, China; 2Yichun University of Jiangxi Province, Yichun, Jiangxi, ChinaAbstract: The objective was to develop an elemene oil/water (o/w) microemulsion and evaluate its characteristics and oral relative bioavailability in rats. Elemene was used as the oil phase and drug, polysorbate 80 as a surfactant along with ethanol, propylene glycol, and glycerol as the cosurfactants. The microemulsion was prepared by mixing method, or ultrasonication method in an ultrasonic bath. Its three-dimensional response surface diagram was drawn by Mathcad software. The microemulsion was characterized by visual observation, cross-polarized microscopy, size, zeta potential, acidity, viscosity, and surface tension measurement. The drug content and entrapment efficiency were determined by ultra fast liquid chromatography (UFLC) and liquid surface method. Blood was drawn from rats at different time points after oral administration of an elemene microemulsion or a commercial elemene emulsion for measurement of the drug in plasma by UFLC to establish the pharmacokinetic parameters and relative bioavailability. The elemene microemulsion as a clarified and isotropic system containing 1% elemene (w/v), 5% ethanol (v/v), 15% propylene glycol (v/v), 15% glycerol (v/v), and 5% polysorbate 80 (w/v), was characterized as (57.7 &plusmn; 2.8) nm in size, 0.485 &plusmn; 0.032 in polydispersity index, (3.2 &plusmn; 0.4) mv in zeta potential, (5.19 &plusmn; 0.08) in pH, 6 mpa&bull;s in viscosity, (31.8 &plusmn; 0.3) mN&bull;m-1 in surface tension, (8.273 &plusmn; 0.018) mg&bull;mL-1 in content of &szlig;-elemene, and (99.81 &plusmn; 0.24)% in average entrapment efficiency. The area under the concentration-time curves from 0 h to 24 h (AUC0&rarr;24h) of the elemene microemulsion and commercial elemene emulsion were integrated to be 3.092 mg&bull;h&bull;L-1 and 1.896 mg&bull;h&bull;L-1 respectively, yielding a relative bioavailability of 163.1%. The present study demonstrates the elemene microemulsion as a new formulation with ease of preparation, high entrapment efficiency, excellent clarity, good stability, and improved bioavailability.Keywords: elemene, microemulsion, relative bioavailability
format	article
author	Zhaowu Zeng Guanglin Zhou Xiaoli Wang et al
author_facet	Zhaowu Zeng Guanglin Zhou Xiaoli Wang et al
author_sort	Zhaowu Zeng
title	Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion
title_short	Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion
title_full	Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion
title_fullStr	Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion
title_full_unstemmed	Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion
title_sort	preparation, characterization and relative bioavailability of oral elemene o/w microemulsion
publisher	Dove Medical Press
publishDate	2010
url	https://doaj.org/article/65616d710fd649e582b56064b3368c30
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_version_	1718398604109938688

Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion

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