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首页> 外文期刊>Journal of drug delivery science and technology >Synthesis of CO2-philic amphiphilic block copolymers by RAFT polymerization and its application on forming drug-loaded micelles using ScCO2 evaporation method
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Synthesis of CO2-philic amphiphilic block copolymers by RAFT polymerization and its application on forming drug-loaded micelles using ScCO2 evaporation method

机译：用SCCO2蒸发法合成RAFT聚合的CO2-含二亲子嵌段共聚物及其在形成药物负载胶束的应用

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摘要

Well-defined drug-loaded micelles are emerging as key nanoplatforms for cancer theranostic and biomedical application. As the basic building block, the CO2-philic polymer has been demonstrated as a high-efficient candidate for the construction of drug-loaded micelles by using supercritical carbon dioxide (ScCO2). Herein, the CO2-philic polymer-poly vinyl acetate (PVAc) is successful via RAFT polymerization technology synthesized in this study. Moreover, the amphiphilic block copolymers, poly(vinyl acetate)-b-poly(ethylene glycol) methyl ether methacrylate (PVAc-b-PEGMA), is successfully synthesized and used for the preparation of paclitaxel-loaded micelles by solvent evaporation method. The parameters of the prepared micelles by using two solvents are compared. When ScCO2 is used as the solvent, the average diameter, encapsulation efficiency (EE), drug loading efficiency (LC) is 476 nm, 38.1 +/- 0.6%, 12.7 +/- 0.2%, respectively. While ethanol is used as the solvent, the above three parameters are 48 nm, 30.6 +/- 0.5%, and 10.2 +/- 0.2%. In addition, in vitro drug release study reveals that the total drug release amount close to 80% from the prepared micelles within 120 h and the release rate is slow and continuous. These results indicate that the solvent evaporation method using the copolymers and ScCO2 as the dispersed phase is a promising procedure for high-efficient fabrication of drug-loaded micelles.
机译：定义明确的药物负载胶束被涌现为癌症治疗和生物医学应用的关键纳米型纳米级。作为基本构建块，通过使用超临界二氧化碳（SCCO2），已经证明了CO2- - 铁聚合物作为制造药物装载胶束的高效候选者。在此，CO 2-铁聚合物 - 聚乙烯酯（PVAC）是通过本研究合成的筏聚合技术成功的。此外，成功地合成了两亲嵌段共聚物，聚（乙酸乙烯酯）-B-聚（乙二醇）甲基醚甲基丙烯酸甲酯（PVAC-B-PEGMA）并通过溶剂蒸发方法制备紫杉醇负载胶束。比较使用两种溶剂的制备胶束的参数。当SCCO2用作溶剂时，平均直径，包封效率（EE），药物负载效率（LC）分别为476nm，38.1 +/- 0.6％，12.7 +/- 0.2％。虽然乙醇用作溶剂，但上述三个参数为48nm，30.6 +/- 0.5％，10.2 +/- 0.2％。此外，体外药物释放研究表明，从120小时内的制备胶束的总药物释放量接近80％，释放速​​率缓慢且连续。这些结果表明，使用共聚物和SCCO2作为分散相的溶剂蒸发方法是用于高效制备药物负载胶束的有希望的方法。

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