Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Yumeng Wei,1,* Jianmin Guo,2,* Xiaoli Zheng,2,* Jun Wu,3 Yang Zhou,1 Yu Yu,4 Yun Ye,1 Liangke Zhang,4 Ling Zhao11School of Pharmacy, 2Institute of Basic Medical Sciences, Luzhou Medical College, Luzhou City, Sichuan Province, P...

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Autores principales:	Wei Y, Guo J, Zheng X, Wu J, Zhou Y, Yu Y, Ye Y, Zhang L, Zhao L
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/a5532e1d19c0443b9d6d1dcd846a5ee1
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spelling	oai:doaj.org-article:a5532e1d19c0443b9d6d1dcd846a5ee12021-12-02T06:46:23ZPreparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes1178-2013https://doaj.org/article/a5532e1d19c0443b9d6d1dcd846a5ee12014-08-01T00:00:00Zhttp://www.dovepress.com/preparation-pharmacokinetics-and-biodistribution-of-baicalin-loaded-li-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Yumeng Wei,1,* Jianmin Guo,2,* Xiaoli Zheng,2,* Jun Wu,3 Yang Zhou,1 Yu Yu,4 Yun Ye,1 Liangke Zhang,4 Ling Zhao11School of Pharmacy, 2Institute of Basic Medical Sciences, Luzhou Medical College, Luzhou City, Sichuan Province, People’s Republic of China; 3Department of Clinical Pharmacy and Outcomes Sciences, College of Pharmacy, University of South Carolina, Greenville, SC, USA; 4School of Pharmacy, Chongqing Medical University, Chongqing, People’s Republic of China*These authors contributed equally to this workAbstract: Baicalin (BA) is a major constituent of Scutellaria baicalensis Georgi, a medicinal herb. Previous pharmacokinetic studies of BA showed its low oral bioavailability. The aim of the present study was to develop a novel BA-loaded liposome (BA-LP) to enhance oral bioavailability. BA-LP, composed of BA, Tween® 80, Phospholipon® 90H, and citric acid at weight ratio of 96/50/96/50, respectively, was prepared by the effervescent dispersion technique and characterized in terms of morphology, size, zeta potential, encapsulation efficiency, and the in vitro release. Pharmacokinetics and biodistribution studies were carried out in rats after oral administration of BA-LP and a carboxymethyl cellulose suspension containing BA (BA-CMC) as a control. BA-LP exhibited a spherical shape by transmission electron microscopy observation. BA-LP had a mean particle size of 373±15.5 nm, zeta potential of -20.1±0.22 mV, and encapsulation efficiency of 82.7%±0.59%. The BA-LP showed a sustained-release behavior, and the in vitro drug-release kinetic model fit well with the Weibull distribution equation: lnln (1/(1-Q)) =0.609 lnt -1.230 (r=0.995). The oral bioavailability and the peak concentration of the BA-LP was threefold and 2.82-fold that of BA-CMC, respectively. The in vivo distribution results indicated that drug concentrations were significantly increased in the liver, kidney, and lung in the case of BA-LP, which were 5.59-fold, 2.33-fold, and 1.25-fold higher than those of BA-CMC, respectively. In conclusion, the study suggested that BA-LP might be a potential oral drug delivery system to improve bioavailability of BA. Keywords: nanoliposomes, bioavailability, nanoliposomes, in vitro release, bioavailability, in vivo evaluationWei YGuo JZheng XWu JZhou YYu YYe YZhang LZhao LDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 3623-3630 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Wei Y Guo J Zheng X Wu J Zhou Y Yu Y Ye Y Zhang L Zhao L Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes
description	Yumeng Wei,1,* Jianmin Guo,2,* Xiaoli Zheng,2,* Jun Wu,3 Yang Zhou,1 Yu Yu,4 Yun Ye,1 Liangke Zhang,4 Ling Zhao11School of Pharmacy, 2Institute of Basic Medical Sciences, Luzhou Medical College, Luzhou City, Sichuan Province, People’s Republic of China; 3Department of Clinical Pharmacy and Outcomes Sciences, College of Pharmacy, University of South Carolina, Greenville, SC, USA; 4School of Pharmacy, Chongqing Medical University, Chongqing, People’s Republic of China*These authors contributed equally to this workAbstract: Baicalin (BA) is a major constituent of Scutellaria baicalensis Georgi, a medicinal herb. Previous pharmacokinetic studies of BA showed its low oral bioavailability. The aim of the present study was to develop a novel BA-loaded liposome (BA-LP) to enhance oral bioavailability. BA-LP, composed of BA, Tween® 80, Phospholipon® 90H, and citric acid at weight ratio of 96/50/96/50, respectively, was prepared by the effervescent dispersion technique and characterized in terms of morphology, size, zeta potential, encapsulation efficiency, and the in vitro release. Pharmacokinetics and biodistribution studies were carried out in rats after oral administration of BA-LP and a carboxymethyl cellulose suspension containing BA (BA-CMC) as a control. BA-LP exhibited a spherical shape by transmission electron microscopy observation. BA-LP had a mean particle size of 373±15.5 nm, zeta potential of -20.1±0.22 mV, and encapsulation efficiency of 82.7%±0.59%. The BA-LP showed a sustained-release behavior, and the in vitro drug-release kinetic model fit well with the Weibull distribution equation: lnln (1/(1-Q)) =0.609 lnt -1.230 (r=0.995). The oral bioavailability and the peak concentration of the BA-LP was threefold and 2.82-fold that of BA-CMC, respectively. The in vivo distribution results indicated that drug concentrations were significantly increased in the liver, kidney, and lung in the case of BA-LP, which were 5.59-fold, 2.33-fold, and 1.25-fold higher than those of BA-CMC, respectively. In conclusion, the study suggested that BA-LP might be a potential oral drug delivery system to improve bioavailability of BA. Keywords: nanoliposomes, bioavailability, nanoliposomes, in vitro release, bioavailability, in vivo evaluation
format	article
author	Wei Y Guo J Zheng X Wu J Zhou Y Yu Y Ye Y Zhang L Zhao L
author_facet	Wei Y Guo J Zheng X Wu J Zhou Y Yu Y Ye Y Zhang L Zhao L
author_sort	Wei Y
title	Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes
title_short	Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes
title_full	Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes
title_fullStr	Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes
title_full_unstemmed	Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes
title_sort	preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/a5532e1d19c0443b9d6d1dcd846a5ee1
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Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

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