Anti-tumor efficiency of NGR-modified PEG-PLGA micelles containing paclitaxel: in vitro and in vivo

doi:10.5246/jcps.2012.01.005

Abstract

Abstract: In the present study, we prepared novel NGR-modified PEG-PLGA polymeric micelles containing paclitaxel (NGR-PM-PTX) in order to evaluate their potential targeting to aminopeptidase N receptors expressed on tumor endothelial cells and the tumor cell surface and its anti-tumor activity in vitro and in vivo. NGR-PM-PTX was prepared by thin-film hydration method. The in vitro targeting characteristics of NGR-modified PM on HUVEC (human umbilical vein endothelial cells), HT1080 (human ﬁbrosarcoma cells) and MCF-7 (human breast adenocarcinoma cells) were then investigated. The anti-tumor activity of NGR-PM-PTX was evaluated in HT1080 tumor-bearing mice in vivo. The targeting activity of the NGR-modified PM was demonstrated by flow cytometry and confocal microscopy in vitro. NGR-PM-PTX also produced marked anti-tumor activity to HT1080 tumor-bearing mice in vivo.

Key words: Aminopeptidase N, Asn-Gly-Arg, Paclitaxel, Targeting, Polymeric micelles

CLC Number:

R945

Supporting:

Bing-Xiang Zhao, Yue Huang, Li-Min Luo, Xin Zhao, Xin Wang, Su Chen, Ke-Fu Yu, Xuan Zhang^*, Qiang Zhang . Anti-tumor efficiency of NGR-modified PEG-PLGA micelles containing paclitaxel: in vitro and in vivo [J]. , DOI: 10.5246/jcps.2012.01.005.

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