氯碘羟喹纳米粒的制备及其功能性评价
Preparation and the biological function evaluation of Clioquinol nanopartices
作者：武航海;
Author：
收稿日期： 年卷（期）页码：2015,30(04):-408-411
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：氯碘羟喹;载药纳米粒;药物增溶;生物利用度;急性毒性;聚乙二醇;聚乳酸羟基乙酸共聚物;缓释给药系统
Key words：
基金项目：
中文摘要
目的以聚乙二醇(PEG)-聚乳酸羟基乙酸共聚物(PLGA)为载体,制备氯碘羟喹(CQ)的纳米给药系统。方法通过PEG引发的开环聚合物制备两亲性聚合物PEG-PLGA,采用乳化溶剂蒸发法制备CQ-PEG-PLGA纳米粒给药系统,并计算其载药量和包封率。采用透射电镜和粒度分析仪表征载药纳米粒的粒度和形态。以Hela细胞为模型,结合MTT法评价纳米粒给药系统的细胞毒性。SD大鼠予尾静脉注射给药后,检测其药动学行为。结果载药纳米粒的粒径约200 nm,CQ的负载量和包封率均随着投药量的提高而增大,体外细胞培养表明其能有效降低CQ的细胞毒性,能延长药物在SD大鼠体内的滞留时间并提高生物利用度。结论所制备的纳米粒给药系统可以有效改善CQ的水溶性、降低细胞的毒性、延长药物在体内的滞留时间并提高生物利用度,有望开发为抗老年痴呆的缓释给药系统。
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