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Synthesis and characterization of a well-defined amphiphilic block copolymer and its paclitaxel prodrug from methoxy poly(ethylene glycol) and oligomer of glycolic acid

Authors

  • Li Zhang,

    1. Key Laboratory of Advanced Functional Polymeric Materials of College of Hunan Province, and Key Laboratory of Polymeric Materials & Application Technology of Hunan Province, Xiangtan University, Xiangtan, Hunan 411105, People's Republic of China
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  • Jinyan Fu,

    1. Key Laboratory of Advanced Functional Polymeric Materials of College of Hunan Province, and Key Laboratory of Polymeric Materials & Application Technology of Hunan Province, Xiangtan University, Xiangtan, Hunan 411105, People's Republic of China
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  • Zhixiang Xia,

    1. Key Laboratory of Advanced Functional Polymeric Materials of College of Hunan Province, and Key Laboratory of Polymeric Materials & Application Technology of Hunan Province, Xiangtan University, Xiangtan, Hunan 411105, People's Republic of China
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  • Ping Wu,

    1. Key Laboratory of Environmentally Friendly Chemistry and Applications of Ministry of Education, Xiangtan University, Xiangtan, Hunan 411105, People's Republic of China
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  • Xuefei Zhang

    Corresponding author
    1. Key Laboratory of Advanced Functional Polymeric Materials of College of Hunan Province, and Key Laboratory of Polymeric Materials & Application Technology of Hunan Province, Xiangtan University, Xiangtan, Hunan 411105, People's Republic of China
    2. Key Laboratory of Environmentally Friendly Chemistry and Applications of Ministry of Education, Xiangtan University, Xiangtan, Hunan 411105, People's Republic of China
    • Key Laboratory of Advanced Functional Polymeric Materials of College of Hunan Province, and Key Laboratory of Polymeric Materials & Application Technology of Hunan Province, Xiangtan University, Xiangtan, Hunan 411105, People's Republic of China
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Abstract

A well-defined amphiphilic block copolymer was synthesized by the coupling of 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 deprotection. The block copolymer had a polydispersity index (PDI) of 1.01, as determined by gel permeation chromatography. It was further coupled to paclitaxel to form a prodrug of paclitaxel. The paclitaxel content in the prodrug was about 10%, and its PDI was 1.02. The antitumor activity of the conjugate against human lung carcinoma A549 cells was evaluated by mitochondrial dehydrogenase (MTT) assay. The results show that paclitaxel could be released from the conjugate without losing cytotoxicity. Therefore, the well-defined amphiphilic block copolymer from MPEG and oligomer of glycolic acid could potentially provide novel opportunities to obtain reproducible pharmacokinetic behavior in the design of a drug-delivery system. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2011

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