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目的通过化学结合法将药物5-氟尿嘧啶(5-FU)与聚乙二醇-聚乳酸(mPEG-PLA)相连接,制备mPEG-PLA-5-FUA含药聚合物胶束,考察其体外释放性能。方法在5-FU的N-1位引入乙酸基,通过DCC缩合法,使5-氟尿嘧啶-1-基乙酸(5-FUA)与mPEG-PLA反应,制得含药聚合物mPEG-PLA-5-FUA,用红外吸收光谱(IR)、差热分析法(DTA)验证其结构;采用透析法制备聚合物胶束,分别用透射电镜观察聚合物胶束的形态,激光散射法测定聚合物胶束的粒径,紫外-可见分光光度法计算胶束载药量,芘探针荧光法测定临界胶束浓度(CMC)值,转篮法测定胶束释放度。结果经IR、DTA鉴定,成功合成了mPEG-PLA-5-FUA聚合物;其胶束平均粒径为42.1 nm,能明显看到胶束的球形核-壳结构;载药量为1.83%,CMC为2.68μg.mL-1,24 h释药量达28.7%。结论 mPEG-PLA-5-FUA载药聚合物胶束具有一定的缓释作用,有利于5-FU的抗肿瘤作用。
OBJECTIVE To prepare mPEG-PLA-5-FUA drug-containing polymer micelles by chemical combination of 5-fluorouracil (5-FU) and polyethylene glycol-polylactic acid (mPEG-PLA) performance. Methods Acetate groups were introduced into the N-1 position of 5-FU and 5-fluorouracil-1-yl acetic acid (5-FUA) was reacted with mPEG-PLA by DCC condensation to obtain mPEG-PLA-5 -FUA. The structure of the polymer micelles was confirmed by infrared absorption spectroscopy (IR) and differential thermal analysis (DTA). The micelles were prepared by dialysis. The morphologies of polymer micelles were observed by transmission electron microscopy. Beam diameter, UV-Vis spectrophotometry micellar drug loading, pyrene probe fluorescence determination of the critical micelle concentration (CMC) values, spinning basket method for the determination of micelles release. Results The mPEG-PLA-5-FUA polymer was successfully synthesized by IR and DTA. The average diameter of the micelles was 42.1 nm. The spherical core-shell structure of the micelles was clearly observed. The drug loading was 1.83% CMC was 2.68μg.mL-1,24 h release amount of 28.7%. Conclusion mPEG-PLA-5-FUA drug-loaded polymer micelles has a certain degree of sustained release, which is beneficial to the antitumor effect of 5-FU.