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

Paper ID Volume ID Publish Year Pages File Format Full-Text
12405 791 2005 8 PDF Available
Title
Synthesis and characterization of the paclitaxel/MPEG-PLA block copolymer conjugate
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 1H 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.

Keywords
Paclitaxel; Prodrug; Ring-opening polymerization; Diglycolic anhydride
First Page Preview
Synthesis and characterization of the paclitaxel/MPEG-PLA block copolymer conjugate
Publisher
Database: Elsevier - ScienceDirect
Journal: Biomaterials - Volume 26, Issue 14, May 2005, Pages 2121–2128
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering