通过RAFT聚合法制备含有二硫键的谷胱甘肽（GSH）响应型两亲性嵌段共聚物P（RhB-SS-MA）-PEG-PPBA，其在水性介质中自组装形成"核-壳"结构的纳米胶束，抗癌药物阿霉素（DOX）包裹在胶束的疏水性核中形成DOX@P（RhB-SS-MA）-PEG-PPBA纳米药物载体。利用¹HNMR、TEM、芘荧光探针、UV-Vis等对聚合物及纳米胶束的结构、形貌、GSH刺激响应性等进行表征和分析，并对载药胶束的细胞内药物递送性能进行研究。结果表明，聚合物胶束外观形貌呈球形，平均粒径约50 nm，临界胶束浓度较低；载药胶束能有效地将DOX递送至B16F10鼠源黑色素瘤细胞的细胞核，且对模拟的肿瘤组织高水平GSH具有较高敏感性，在pH 7.4、10 mmol/L GSH环境下，24 h内DOX的累积释放率达到73.6%。

A glutathione (GSH)-responsive amphiphilic block copolymer P(RhB-SS-MA)-PEG-PPBA is prepared via RAFT polymerization method, which self-assembles in aqueous medium to form "core-shell" nano micelles.Adriamycin (DOX), a kind of anticancer drug, is wrapped in the hydrophobic core of the micellar to form DOX@P(RhB-SS-MA)-PEG-PPBA nano-drug carrier.¹H-NMR, TEM, pyrene fluorescent probe and UV-Vis are utilized to characterize and analyze the structure, morphology and GSH stimulation response of both the polymer and the nano micelles.The intracellular drug delivery performance of the drug-carrying micelles is also studied.Results show that the polymer micelles present a low critical micelle concentration and spherical morphology with an average particle size of about 50 nm.The drug-carrying micelles can effectively deliver DOX to the nucleus of B16F10 murine melanoma cells and are highly sensitive to the high level of GSH of the simulated tumor microenvironment.The cumulative release rate of DOX reaches 73.6% within 24 hours under an environment with a pH of 7.4 and 10 mmol·L^-1 of GSH.

张海亮(1986-),男,硕士,讲师,研究方向为刺激响应型高分子材料,402204961@qq.com