醋酸铜梯度法制备阿霉素脂质体  

Study on preparation of doxorubicin liposome by copper acetate gradient method

作　　者：马佳 赵艺 刘诗文 苏海莹 陈玉姣 徐晖[2] 王绍宁[1] MA Jia;ZHAO Yi;LIU Shiwen;SU Haiying;CHEN Yujiao;XU Hui;WANG Shaoning(School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China;School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《中国药剂学杂志（网络版）》2022年第6期205-212,共8页Chinese Journal of Pharmaceutics：Online Edition

基　　金：辽宁省教育厅项目(LJKZ0959);沈阳药科大学归国留学人员启动基金项目(GGJJ20211104);沈阳药科大学国家级大学生创新创业训练计划项目(202210163009)。

摘　　要：目的利用醋酸铜梯度制备阿霉素脂质体,并探讨其载药机制。方法以包封率为指标考察影响阿霉素载药的因素,通过紫外光谱的变化确证阿霉素—铜离子复合物的形成。结果采用醋酸铜梯度制备的阿霉素脂质体包封率可达87.43%±2.90%,显著高于硫酸铜梯度和氯化铜梯度;药脂比、载药温度及外水相pH值对脂质体的包封率影响较大。随着释放介质pH值的降低阿霉素从脂质体中的释放增加。结论醋酸铜梯度法适用于阿霉素脂质体的制备,阿霉素—铜离子复合物的形成及醋酸根离子的存在可能是提高阿霉素包封率的主要原因。Objective The doxorubicin liposome was prepared by copper acetate gradient and its drug delivery mechanism was discussed.Methods Encapsulation effeciency was used as the index to investigate the factors affecting the drug loading of doxorubicin,and the formation of doxorubicincopper ion complex was confirmed by the change of ultraviolet spectrum.Results The encapsulation efficiency of doxorubicin liposome prepared by copper acetate gradient(87.43±2.90)%was significantly higher than that of copper sulfate gradient and copper chloride gradient.Drug-lipid ratio,drug loading temperature and pH of external aqueous phase had great effects on liposo me encapsulation efficiency.The release of doxorubicin from liposomes increased as the decreased pH of the release medium.Conclusion The copper acetate gradient method is suitable for the preparation of doxorubicin liposomes.The formation of doxorubicin-copper ion complex and the existence of acetate ion may be the main reasons for improving the entrapment efficiency of doxorubicin.

关 键 词：药剂学 脂质体 醋酸铜梯度 阿霉素 

分 类 号：R94[医药卫生—药剂学]