Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation

Kaili Hu,1 Shan Cao,1,2 Fuqiang Hu,3 Jianfang Feng11Murad Research Center for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 2Pharmacy Department, Baoshan Central Hospital, Shanghai, 3School of Pharmacy, Zhejiang University, Hangzhou, ChinaAbstract: The a...

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Autores principales:	Hu K, Cao S, Hu F, Feng J
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/ec1142d8674949e2bc3414576af899ef
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spelling	oai:doaj.org-article:ec1142d8674949e2bc3414576af899ef2021-12-02T02:10:29ZEnhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation1176-91141178-2013https://doaj.org/article/ec1142d8674949e2bc3414576af899ef2012-07-01T00:00:00Zhttp://www.dovepress.com/enhanced-oral-bioavailability-of-docetaxel-by-lecithin-nanoparticles-p-a10341https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Kaili Hu,1 Shan Cao,1,2 Fuqiang Hu,3 Jianfang Feng11Murad Research Center for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 2Pharmacy Department, Baoshan Central Hospital, Shanghai, 3School of Pharmacy, Zhejiang University, Hangzhou, ChinaAbstract: The aim of this research work was to investigate the potential of lecithin nanoparticles (LNs) in improving the oral bioavailability of docetaxel. Docetaxel-loaded LNs (DTX-LNs) were prepared from oil-in-water emulsions and characterized in terms of morphology, size, zeta potential, and encapsulation efficiency. The in vitro release of docetaxel from the nanoparticles was studied by using dialysis bag method. Caco-2 cell monolayer was used for the in vitro permeation study of DTX-LNs. Bioavailability studies were conducted in rats and different pharmacokinetic parameters were evaluated after oral administration of DTX-LNs. The results showed that DTX-LNs had a mean diameter of 360 &plusmn; 8 nm and exhibited spherical shape with smooth surface under transmission electron microscopy. The DTX-LNs showed a sustained-release profile, with about 80% of docetaxel released within 72 hours. The apical to basolateral transport of docetaxel across the Caco-2 cell monolayer from the DTX-LNs was 2.14 times compared to that of the docetaxel solution (0.15 &times; 10-5 &plusmn; 0.016 &times; 10-5 cm/second versus 0.07 &times; 10-5 &plusmn; 0.003 &times; 10-5 cm/second). The oral bioavailability of the DTX-LNs was 3.65 times that of docetaxel solution (8.75% versus 2.40%). These results indicate that DTX-LNs were valuable as an oral drug delivery system to enhance the absorption of docetaxel.Keywords: lecithin nanoparticles, oral delivery, docetaxel, bioavailabilityHu KCao SHu FFeng JDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 3537-3545 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Hu K Cao S Hu F Feng J Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation
description	Kaili Hu,1 Shan Cao,1,2 Fuqiang Hu,3 Jianfang Feng11Murad Research Center for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 2Pharmacy Department, Baoshan Central Hospital, Shanghai, 3School of Pharmacy, Zhejiang University, Hangzhou, ChinaAbstract: The aim of this research work was to investigate the potential of lecithin nanoparticles (LNs) in improving the oral bioavailability of docetaxel. Docetaxel-loaded LNs (DTX-LNs) were prepared from oil-in-water emulsions and characterized in terms of morphology, size, zeta potential, and encapsulation efficiency. The in vitro release of docetaxel from the nanoparticles was studied by using dialysis bag method. Caco-2 cell monolayer was used for the in vitro permeation study of DTX-LNs. Bioavailability studies were conducted in rats and different pharmacokinetic parameters were evaluated after oral administration of DTX-LNs. The results showed that DTX-LNs had a mean diameter of 360 &plusmn; 8 nm and exhibited spherical shape with smooth surface under transmission electron microscopy. The DTX-LNs showed a sustained-release profile, with about 80% of docetaxel released within 72 hours. The apical to basolateral transport of docetaxel across the Caco-2 cell monolayer from the DTX-LNs was 2.14 times compared to that of the docetaxel solution (0.15 &times; 10-5 &plusmn; 0.016 &times; 10-5 cm/second versus 0.07 &times; 10-5 &plusmn; 0.003 &times; 10-5 cm/second). The oral bioavailability of the DTX-LNs was 3.65 times that of docetaxel solution (8.75% versus 2.40%). These results indicate that DTX-LNs were valuable as an oral drug delivery system to enhance the absorption of docetaxel.Keywords: lecithin nanoparticles, oral delivery, docetaxel, bioavailability
format	article
author	Hu K Cao S Hu F Feng J
author_facet	Hu K Cao S Hu F Feng J
author_sort	Hu K
title	Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation
title_short	Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation
title_full	Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation
title_fullStr	Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation
title_full_unstemmed	Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation
title_sort	enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/ec1142d8674949e2bc3414576af899ef
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_version_	1718402684969549824

Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation

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