Literature DB >> 15576187

Synthesis and characterization of the paclitaxel/MPEG-PLA block copolymer conjugate.

Xuefei Zhang1, Yuxin Li, Xuesi Chen, Xiuhong Wang, Xiaoyi Xu, Qizhi Liang, Junli Hu, Xiabin Jing.   

Abstract

A paclitaxel/MPEG-PLA block copolymer conjugate was prepared in three steps: (1) hydroxyl-terminated diblock copolymer of monomethoxy-poly(ethylene glycol)-b-poly(lactide) (MPEG-PLA) was synthesized by ring-opening polymerization of L-lactide using MPEG as a maroinitiator; (2) it was converted to carboxyl-terminated MPEG-PLA by reacting with mono-t-butyl ester of diglycolic acid and subsequent deprotecting the t-butyl group with TFA; (3) the latter was reacted with paclitaxel in the presence of dicyclohexylcarbodiimide and dimethylaminopyridine. Structures of the polymers synthesized were confirmed by (1)H NMR, and their molecular weights were determined by gel permeation chromatography. The antitumor activity of the conjugate against human liver cancer H7402 cells was evaluated by MTT method. The results showed that paclitaxel can be released from the conjugate without losing cytotoxicity.

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Year:  2005        PMID: 15576187     DOI: 10.1016/j.biomaterials.2004.06.024

Source DB:  PubMed          Journal:  Biomaterials        ISSN: 0142-9612            Impact factor:   12.479


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