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Self-assembly of a biodegradable branched PE-PCL-b-PEC amphiphilic polymer: synthesis, characterization and targeted delivery of doxorubicin to cancer cells

机译:可生物降解的分支PE-PCL-b-PEC两亲聚合物的自组装:阿霉素对癌细胞的合成,表征和靶向递送

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A novel biodegradable branched block copolymer was synthesized by the ring-opening polymerization of ethylene carbonate using pre-synthesized four-armed pentaerythretol poly(epsilon-caprolactone) (PE-PCL) as a macro initiator. Folic acid was conjugated with the end-group of the block copolymer and self-assembled in water to form polymer micelles (PMs). The very low critical micelle concentration of the block copolymer suggests its potential application in advanced drug delivery systems. The PMs are spherical in shape and have an average size of 80 nm, which is suitable for the delivery of drugs. The hydrophobicity of pentaerythretol poly(epsilon-caprolactone) and its branched structure can accommodate high amounts of doxorubicin. Compared with a blank sample, PMs containing encapsulated doxorubicin show a much higher cytotoxicity towards HeLa cells. A high rate of release of doxorubicin in vitro at pH 5.0 shows that the system is responsive to pH. Confocal laser scanning microscopy showed that the doxorubicin-loaded PMs were internalized into the HeLa cells.
机译:通过预合成的四臂季戊四醇聚ε-己内酯(PE-PCL)作为大分子引发剂,通过碳酸亚乙酯的开环聚合反应合成了一种新型的可生物降解的支链嵌段共聚物。叶酸与嵌段共聚物的末端基团共轭,并在水中自组装形成聚合物胶束(PMs)。嵌段共聚物的临界胶束浓度非常低,表明其在先进的药物输送系统中的潜在应用。 PM为球形,平均尺寸为80nm,适合于药物递送。季戊四醇聚(ε-己内酯)的疏水性及其分支结构可容纳大量的阿霉素。与空白样品相比,含有封装的阿霉素的PMs对HeLa细胞具有更高的细胞毒性。 pH 5.0时,阿霉素的体外高释放速率表明该系统对pH敏感。共聚焦激光扫描显微镜显示,装载阿霉素的PM被内化到HeLa细胞中。

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