Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation

Ling Zhao,1,2 Yumeng Wei,1,2 Yu Huang,1 Bing He,2 Yang Zhou,1 Junjiang Fu31Department of Pharmaceutical Sciences, School of Pharmacy, Luzhou Medical College, Luzhou City, Sichuan Province, People's Republic of China; 2Drug and Functional Food Research Center, Luzhou Medical College, Luzhou C...

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Autores principales:	Zhao L, Wei Y, Huang Y, He B, Zhou Y, Fu J
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/33bed8a506284951b4154048e7221b41
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spelling	oai:doaj.org-article:33bed8a506284951b4154048e7221b412021-12-02T05:14:22ZNanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation1176-91141178-2013https://doaj.org/article/33bed8a506284951b4154048e7221b412013-10-01T00:00:00Zhttp://www.dovepress.com/nanoemulsion-improves-the-oral-bioavailability-of-baicalin-in-rats-in--a14548https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Ling Zhao,1,2 Yumeng Wei,1,2 Yu Huang,1 Bing He,2 Yang Zhou,1 Junjiang Fu31Department of Pharmaceutical Sciences, School of Pharmacy, Luzhou Medical College, Luzhou City, Sichuan Province, People's Republic of China; 2Drug and Functional Food Research Center, Luzhou Medical College, Luzhou City, Sichuan Province, People's Republic of China; 3The Research Center for Preclinical Medicine, Luzhou Medical College, Luzhou City, Sichuan Province, People's Republic of ChinaAbstract: Baicalin is one of the main bioactive flavone glucuronides derived as a medicinal herb from the dried roots of Scutellaria baicalensis Georgi, and it is widely used for the treatment of fever, inflammation, and other conditions. Due to baicalin's poor solubility in water, its absolute bioavailability after oral administration is only 2.2%. The objective of this study was to develop a novel baicalin-loaded nanoemulsion to improve the oral bioavailability of baicalin. Based on the result of pseudoternary phase diagram, the nanoemulsion formulation consisting of soy-lecithin, tween-80, polyethylene glycol 400, isopropyl myristate, and water (1:2:1.5:3.75:8.25, w/w) was selected for further study. Baicalin-loaded nanoemulsions (BAN-1 and BAN-2) were prepared by internal or external drug addition and in vivo and in vitro evaluations were performed. The results showed that the mean droplet size, polydispersity index, and drug content of BAN-1 and BAN-2 were 91.2 ± 2.36 nm and 89.7 ± 3.05 nm, 0.313 ± 0.002 and 0.265 ± 0.001, and 98.56% ± 0.79% and 99.40% ± 0.51%, respectively. Transmission electron microscopy revealed spherical globules and confirmed droplet size analysis. After dilution 30-fold with water, the solubilization capacity of BAN-1 and BAN-2 did not change. In vitro release results showed sustained-release characteristics. BAN-1 formulation was stable for at least 6 months and was more stable than BAN-2. In rats, the area under the plasma drug concentration-time curve value of BAN-1 was 1.8-fold and 7-fold greater than those of BAN-2 and free baicalin suspension after oral administration at a dose of 100 mg/kg. In conclusion, these results demonstrated that the baicalin-loaded nanoemulsion formulation, in particular BAN-1, was very effective for improving the oral bioavailability of baicalin and exhibited great potential for future clinical application.Keywords: nanoemulsion, baicalin, oral bioavailability, pharmacokineticsZhao LWei YHuang YHe BZhou YFu JDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss Issue 1, Pp 3769-3779 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Zhao L Wei Y Huang Y He B Zhou Y Fu J Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation
description	Ling Zhao,1,2 Yumeng Wei,1,2 Yu Huang,1 Bing He,2 Yang Zhou,1 Junjiang Fu31Department of Pharmaceutical Sciences, School of Pharmacy, Luzhou Medical College, Luzhou City, Sichuan Province, People's Republic of China; 2Drug and Functional Food Research Center, Luzhou Medical College, Luzhou City, Sichuan Province, People's Republic of China; 3The Research Center for Preclinical Medicine, Luzhou Medical College, Luzhou City, Sichuan Province, People's Republic of ChinaAbstract: Baicalin is one of the main bioactive flavone glucuronides derived as a medicinal herb from the dried roots of Scutellaria baicalensis Georgi, and it is widely used for the treatment of fever, inflammation, and other conditions. Due to baicalin's poor solubility in water, its absolute bioavailability after oral administration is only 2.2%. The objective of this study was to develop a novel baicalin-loaded nanoemulsion to improve the oral bioavailability of baicalin. Based on the result of pseudoternary phase diagram, the nanoemulsion formulation consisting of soy-lecithin, tween-80, polyethylene glycol 400, isopropyl myristate, and water (1:2:1.5:3.75:8.25, w/w) was selected for further study. Baicalin-loaded nanoemulsions (BAN-1 and BAN-2) were prepared by internal or external drug addition and in vivo and in vitro evaluations were performed. The results showed that the mean droplet size, polydispersity index, and drug content of BAN-1 and BAN-2 were 91.2 ± 2.36 nm and 89.7 ± 3.05 nm, 0.313 ± 0.002 and 0.265 ± 0.001, and 98.56% ± 0.79% and 99.40% ± 0.51%, respectively. Transmission electron microscopy revealed spherical globules and confirmed droplet size analysis. After dilution 30-fold with water, the solubilization capacity of BAN-1 and BAN-2 did not change. In vitro release results showed sustained-release characteristics. BAN-1 formulation was stable for at least 6 months and was more stable than BAN-2. In rats, the area under the plasma drug concentration-time curve value of BAN-1 was 1.8-fold and 7-fold greater than those of BAN-2 and free baicalin suspension after oral administration at a dose of 100 mg/kg. In conclusion, these results demonstrated that the baicalin-loaded nanoemulsion formulation, in particular BAN-1, was very effective for improving the oral bioavailability of baicalin and exhibited great potential for future clinical application.Keywords: nanoemulsion, baicalin, oral bioavailability, pharmacokinetics
format	article
author	Zhao L Wei Y Huang Y He B Zhou Y Fu J
author_facet	Zhao L Wei Y Huang Y He B Zhou Y Fu J
author_sort	Zhao L
title	Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation
title_short	Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation
title_full	Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation
title_fullStr	Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation
title_full_unstemmed	Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation
title_sort	nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/33bed8a506284951b4154048e7221b41
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Nanoemulsion improves the oral bioavailability of baicalin in rats: in vitro and in vivo evaluation

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