多柔比星聚合物胶束制备、表征及其体外释药研究.pdfVIP

.526. 中国抗生素杂志2015年7月第40卷第7期 文章编号: 1001-8689(2015)07-0526-05 多柔比星聚合物胶束制备、表征及其体外释药研究 典灵辉郭向华程主己伦林晓严雄于恩江毛志慧 (广东医学院药学院，东莞 523808) 摘要:目的 制备多柔比里，的soluplus聚合物胶束，并对其进行体外评价。方法 采用薄膜分散法-pH诱导法相结合制备多 柔比星聚合物胶束:采用粒径测定仪、透射电镜、 X-射线衍射(XRD)、差示扫描量热法(DSC)及红外光谱(FTIR)对其进行表征: 采用HPLC法测定胶束的包封率和载药量;采用动态膜透析法考察载药胶束的体外释药特性。结果 本研究制备的胶束呈球形 或类球形，平均粒径为(67.57 士2.9)nm，平均包封率为(77.81 ::1:: 4.03)%，平均载药量(10.15 ::1:: 1.56)%; XRD和DSC结果表明多柔 比星以无定型状态或分子状态包载在聚合物胶束中; FTIR结果表明多柔比星分子中挂基和聚合物的叛基之间形成了氢键:体外 释放结果表明多柔比星的soluplus聚合物胶束具有缓释作用。结论 该胶束制备工艺简单，其粒径、包封率、载药量可控，具有 缓释作用。 关键词z 多柔比星; Soluplus; 聚合物胶束:体外评价 中图分类号: R979.1 文献标志码:A Preparation, characterization and drug release property of doxorubicin-loaded polymeric micelles Dian Ling-hui , Guo Xiang-hua , Cheng Ji-lun , Lin Xiao , Yan Xiong , Yu En-jiang and Mao Zhi-hui (School ofPharmaceutical Sciences, Guangdong Medical College, Dongguan 523808) Abstract Objective To prepare doxorubicin-loaded soluplus polymeric micelles (ADM-PMs) and evaluate their quality. Methods The ADM-PMs were prepared by film dispersion method using an amphiphilic copolymer soluplus. The ADM-PMs were characterized by dynamic light scattering, transmission electron microscopy (TEM) , X-ray di曲action (XRD) , differential scanning calorime町(DSC)， and fourier transform-infrared spectra (FTIR). The release cu凹e was determined by dialysis. Entrapment efficiency and drug loading were determined by HPLC. Results The ADM-PMs observed by TEM were spherical with a mean particle size of (67.57士2.9)nm， the encapsulation efficiency and drug loading of ADM-PMs were (77.81士4.03)% and (10.15土1.56)%. XRD and DSC determined that doxorub