Synthesis and Characterization of a Well-defined Amphiphilic Block Copolymer and Its Paclitaxel Prodrug from MPEG and Oligomer of Glycolic Acid

Zhang Li; Fu Jinyan; Wu Ping; Xia Zhixiang; Zhang Xuefei

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Synthesis and Characterization of a Well-defined Amphiphilic Block Copolymer and Its Paclitaxel Prodrug from MPEG and Oligomer of Glycolic Acid

Zhang Li ,Fu Jinyan ,Wu Ping ,Xia Zhixiang ,Zhang Xuefei *

College of Chemistry, Xiangtan University

*Correspondence author

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Funding: Specialized Research Fund for the Doctoral Program of Higher Education（No.20070530007）

Opened online: 6 December 2010

Accepted by: none

Citation: Zhang Li ,Fu Jinyan ,Wu Ping .Synthesis and Characterization of a Well-defined Amphiphilic Block Copolymer and Its Paclitaxel Prodrug from MPEG and Oligomer of Glycolic Acid[OL]. [ 6 December 2010] http://en.paper.edu.cn/en_releasepaper/content/4393170

A well-defined amphiphilic block copolymer was synthesized by coupling carboxyl-terminated methoxy Poly (ethylene glycol) (MPEG) with a hydroxyl-terminated octamer of glycolic acid which was obtained by a stepwise synthetic procedure with the end-group protection and de-protection. The block copolymer had a polydispersity index (PDI) of 1.01 determined by GPC. It was further coupled to paclitaxel to form a prodrug of paclitaxel. The paclitaxel content in the prodrug was ca. 10% and its PDI was 1.02. The antitumor activity of the conjugate against human lung carcinoma A549 cells was evaluated by MTT assay. The results showed that paclitaxel can be released from the conjugate without losing cytotoxicity. Therefore, the well-defined amphiphilic block copolymer from MPEG and oligomer of glycolic acid would potentially provide novel opportunities to obtain reproducible pharmacokinetic behavior in design of drug delivery system.

Keywords:Polymer Chemistry; Amphiphiles; Biodegradable; Block copolymers; Conjugated polymers; Drug delivery systems

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