Folate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy

Lili Wang, Min Li, Na ZhangSchool of Pharmaceutical Science, Shandong University, Jinan, Shandong, ChinaAbstract: The purpose of this study was to develop two novel drug delivery systems based on biodegradable docetaxel-lipid-based-nanosuspensions. The first one was poly(ethylene glycol)-modified do...

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Autores principales:	Wang L, Li M, Zhang N
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/3676f8b928ea495eb7b89a5e306a9a2d
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spelling	oai:doaj.org-article:3676f8b928ea495eb7b89a5e306a9a2d2021-12-02T05:32:49ZFolate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy1176-91141178-2013https://doaj.org/article/3676f8b928ea495eb7b89a5e306a9a2d2012-06-01T00:00:00Zhttp://www.dovepress.com/folate-targeted-docetaxel-lipid-based-nanosuspensions-for-active-targe-a10266https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Lili Wang, Min Li, Na ZhangSchool of Pharmaceutical Science, Shandong University, Jinan, Shandong, ChinaAbstract: The purpose of this study was to develop two novel drug delivery systems based on biodegradable docetaxel-lipid-based-nanosuspensions. The first one was poly(ethylene glycol)-modified docetaxel-lipid-based-nanosuspensions (pLNS). It was developed to increase the cycle time of the drug within the body and enhance the accumulation of the drug at the tumor site. The second one was targeted docetaxel-lipid-based-nanosuspensions (tLNS) using folate as the target ligand. The tLNS could target the tumor cells that overexpressed folate receptor (FR). The morphology, particle size, and zeta potential of pLNS and tLNS were characterized, respectively. The in vitro cytotoxicity evaluation of Duopafei&reg;, pLNS, and tLNS were performed in human hepatocellular liver carcinoma HepG2 (FR-) and B16 (FR+) cells, respectively. The in vivo antitumor efficacy and pharmacokinetics, as well as the drug tissue distribution, were evaluated in Kunming mice bearing B16 cells. The particle size of pLNS was 204.2 &plusmn; 6.18 nm and tLNS had a mean particle size of 220.6 &plusmn; 9.54 nm. Cytotoxicity of tLNS against B16 (FR+) cell lines was superior to pLNS (P &lt; 0.05), while there was no significant difference in the half maximum inhibitory concentration values for HepG2 (FR-) cells between pLNS and tLNS. The results of the in vivo antitumor efficacy evaluation showed that tLNS exhibited higher antitumor efficacy by reducing tumor volume (P &lt; 0.01) compared with Duopafei and pLNS, respectively. The results of the in vivo biodistribution study indicate that the better antitumor efficacy of tLNS was attributed to the increased accumulation of the drug in the tumor.Keywords: lipid-based-nanosuspensions, docetaxel, cancer therapy, folate, target drug deliveryWang LLi MZhang NDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 3281-3294 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Wang L Li M Zhang N Folate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy
description	Lili Wang, Min Li, Na ZhangSchool of Pharmaceutical Science, Shandong University, Jinan, Shandong, ChinaAbstract: The purpose of this study was to develop two novel drug delivery systems based on biodegradable docetaxel-lipid-based-nanosuspensions. The first one was poly(ethylene glycol)-modified docetaxel-lipid-based-nanosuspensions (pLNS). It was developed to increase the cycle time of the drug within the body and enhance the accumulation of the drug at the tumor site. The second one was targeted docetaxel-lipid-based-nanosuspensions (tLNS) using folate as the target ligand. The tLNS could target the tumor cells that overexpressed folate receptor (FR). The morphology, particle size, and zeta potential of pLNS and tLNS were characterized, respectively. The in vitro cytotoxicity evaluation of Duopafei&reg;, pLNS, and tLNS were performed in human hepatocellular liver carcinoma HepG2 (FR-) and B16 (FR+) cells, respectively. The in vivo antitumor efficacy and pharmacokinetics, as well as the drug tissue distribution, were evaluated in Kunming mice bearing B16 cells. The particle size of pLNS was 204.2 &plusmn; 6.18 nm and tLNS had a mean particle size of 220.6 &plusmn; 9.54 nm. Cytotoxicity of tLNS against B16 (FR+) cell lines was superior to pLNS (P &lt; 0.05), while there was no significant difference in the half maximum inhibitory concentration values for HepG2 (FR-) cells between pLNS and tLNS. The results of the in vivo antitumor efficacy evaluation showed that tLNS exhibited higher antitumor efficacy by reducing tumor volume (P &lt; 0.01) compared with Duopafei and pLNS, respectively. The results of the in vivo biodistribution study indicate that the better antitumor efficacy of tLNS was attributed to the increased accumulation of the drug in the tumor.Keywords: lipid-based-nanosuspensions, docetaxel, cancer therapy, folate, target drug delivery
format	article
author	Wang L Li M Zhang N
author_facet	Wang L Li M Zhang N
author_sort	Wang L
title	Folate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy
title_short	Folate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy
title_full	Folate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy
title_fullStr	Folate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy
title_full_unstemmed	Folate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy
title_sort	folate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/3676f8b928ea495eb7b89a5e306a9a2d
work_keys_str_mv	AT wangl folatetargeteddocetaxellipidbasednanosuspensionsforactivetargetedcancertherapy AT lim folatetargeteddocetaxellipidbasednanosuspensionsforactivetargetedcancertherapy AT zhangn folatetargeteddocetaxellipidbasednanosuspensionsforactivetargetedcancertherapy
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Folate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy

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