Facile Fabrication of Thermo-Responsive and Reduction-Sensitive Polymeric Micelles for Anticancer Drug Delivery

Authors

  • Xulin Jiang,

    Corresponding author
    1. Key Laboratory of Biomedical Polymers of Ministry of Education, and Department of Chemistry, Wuhan University, Luojia Hill, Wuhan 430072, China
    • Key Laboratory of Biomedical Polymers of Ministry of Education, and Department of Chemistry, Wuhan University, Luojia Hill, Wuhan 430072, China.
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  • Lihua Li,

    1. Key Laboratory of Biomedical Polymers of Ministry of Education, and Department of Chemistry, Wuhan University, Luojia Hill, Wuhan 430072, China
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  • Jia Liu,

    1. Key Laboratory of Biomedical Polymers of Ministry of Education, and Department of Chemistry, Wuhan University, Luojia Hill, Wuhan 430072, China
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  • Wim E. Hennink,

    1. Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Science, Utrecht University, P.O. Box 80082, 3508 TB, Utrecht, The Netherlands
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  • Renxi Zhuo

    1. Key Laboratory of Biomedical Polymers of Ministry of Education, and Department of Chemistry, Wuhan University, Luojia Hill, Wuhan 430072, China
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Abstract

The development of thermo-responsive and reduction-sensitive polymeric micelles based on an amphiphilic block copolymer poly[(PEG-MEMA)-co-(Boc-Cyst-MMAm)]-block-PEG (denoted PEG-P-SS-HP) for the intracellular delivery of anticancer drugs is reported. PTX, as model drug, was loaded into the PEG-P-SS-HP micelles with an encapsulation efficiency >90%, resulting in a high drug loading content (up to 35 wt%). The PTX-loaded PEG-P-SS-HP micelles show slow drug release in PBS and rapid release after incubation with DTT. The PTX-loaded micelles display a better cytotoxic effect than the free drug, whereas empty micelles are found to be non-toxic. The thermo-responsive and reduction-sensitive polymeric micelles described may serve as promising carriers for cytostatic drugs.

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