文献类型：期刊文献

英文题名：Controlled preparation and antitumor efficacy of vitamin E TPGS-functionalized PLGA nanoparticles for delivery of paclitaxel

作者：Wang, Guoying[1,2];Yu, Bo[3];Wu, Yuequn[2];Huang, Baolin[1,2];Yuan, Yuan[1,2];Liu, Chang Sheng[1,2]

机构：[1]E China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[2]E China Univ Sci & Technol, Minist Educ, Key Lab Ultrafine Mat, Shanghai 200237, Peoples R China;[3]Hangzhou PushiKang Biotechnol Co Ltd, Hangzhou 310021, Zhejiang, Peoples R China

年份：2013

卷号：446

期号：1-2

起止页码：24

外文期刊名：INTERNATIONAL JOURNAL OF PHARMACEUTICS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000316736500004)】；

基金：The authors wish to express their gratitude to the financial supports from National Basic Research Program of China (973 Program, No. 2012CB933600) and Shanghai Nanotechnology Special Foundation (No. 11nm0506300). The authors also appreciate Shanghai Animal Center for Animal Experiments.

语种：英文

外文关键词：Paclitaxel; TPGS-functionalized PLGA nanoparticles; Controllable preparation; Drug delivery; Antitumor efficacy

摘要：Vitamin E TPGS-functionalized polymeric nanoparticles have been developed as a promising drug delivery platform in recent years. Obtaining reproducible monodisperse TPGS/polymeric nanoparticles with high encapsulation efficiency (EE%) still remains a big challenge. In this study, an inverse-phase nanoprecipitation method was developed to synthesize TPGS-functionalized PLGA nanoparticles (TPNs) for controlled release of paclitaxel (PTX). To take advantages of lipids, a part of TPGS in the TPNs was replaced by lipids. The results showed that with weight ratio of TPGS-to-PLGA of 2-3 and a molar replacement of lecithin ratio of 30%, the PTX-loaded TPNs (PTPNs) and PTX-loaded lipid-containing TPNs (PLTPNs) exhibited controllable and nearly uniform size of 130-150 nm and EE% of over 80%. Compared to Taxol (R), both the PTPNs and PLTPNs significantly increased the intracellular uptake and exerted strong inhibitory effect on human lung cancer A549 model cells. Furthermore, a selective accumulation to tumor site and significant antitumor efficacy of TPNs in the A549 lung cancer xenografted nude mice were observed by intravenous administration, especially for the PTPNs group. Our data suggested that the inverse-phase nanoprecipitation method holds great potential for the fabrication of the paclitaxel-loaded TPNs and the TPNs prepared here is a promising controllable delivery system for paclitaxel. (C) 2013 Elsevier B. V. All rights reserved.