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HCPT前药
COLLOIDS AND SURFACES B-BIOINTERFACES · 2019 · IF 3.973

Synthesis, self-assembly and drug release behaviors of a bottlebrush polymer-HCPT prodrug for tumor chemotherapy

Fangyuan Lv,Dapeng Liu,Hailin Cong,Youqing Shen,Bing Yu

A bottlebrush polymer-cytotoxin prodrug, where a potent anticancer drug 10-hydroxycamptothecin (HCPT) and water-soluble methoxypolyethylene glycols (mPEG) were attached into the polyester backbone, was synthesized via thiol-ene reaction. The synthesized bottlebrush polymer-HCPT conjugate with drug loading content as high as ca. 20.4 wt% was characterized by NMR, IR, UV and fluorescence techniques. The prepared bottlebrush polymer-HCPT prodrug could self-assemble into nanosized micelles ( ca. 153 nm), which were uniform and stable in aqueous solution. Moreover, when exposed to esterase, the formed prodrug micelles as stimuli-responsive nanomaterials could release HCPT. In the cellar uptake and cytotoxicity experiments, the formed prodrug micelles exhibited effective internalization into tumor cells and excellent anticancer efficacies.

研究领域: 生物材料学 · 药学 · 肿瘤学
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