齐墩果酸脂质体的制备工艺优化  

Optimization of Preparation Process for Oleanolic Acid Liposomes

作　　者：李昀泽 李佳霖 粟康 鲁思文 邓书平[1] 郝爱军 LI Yunze;LI Jialin;SU Kang;LU Siwen;DENG Shuping;HAO Aijun(School of Chemistry and Environmental Engineering,Yingkou Instituete of Technology,Yingkou 115014,China)

机构地区：[1]营口理工学院化学与环境工程学院,辽宁营口115014

出　　处：《山东化工》2024年第22期14-16,20,共4页Shandong Chemical Industry

基　　金：辽宁省省教育厅科学研究项目(LZKJ1205);营口市企业博士双创计划项目(2022年);营口理工学院大学生创新创业训练项目(202314435005)。

摘　　要：齐墩果酸具有抑制血小板聚集、抗肿瘤、促进肝细胞再生、降血糖、血脂、镇静等多方面药理作用。但临床上齐墩果酸难溶于水,口服生物半衰期较短,绝对生物利用度较低,限制了临床应用。为了改善这些缺点,研究了薄膜分散法制备齐墩果酸脂质体的最佳工艺。通过单因素实验和正交优化实验优化了齐墩果酸脂质体的制备工艺。得到最佳制备工艺为磷脂质量分数3.0%,脂药质量比为30∶1,磷脂与胆固醇的质量比例为2∶1,超声时间为20 min。最优实验条件下,制备的齐墩果酸脂质体包封率为98.8%。粒径为(325±50)nm, zeta电位为-3.09 mv。Oleanolic acid has various pharmacological effects such as inhibiting platelet aggregation,anti-tumor,promoting liver cell regeneration,lowering blood sugar,blood lipids,and sedation.However,oleanolic acid is insoluble in water,has a short oral half-life,and low absolute bioavailability,which limits its clinical application.In order to improve these drawbacks,this article studied the optimal process for preparing oleanolic acid liposomes using thin film dispersion method.This article optimized the preparation process of oleanolic acid liposomes through single factor experiments and orthogonal optimization experiments.The optimal preparation process was obtained as follows:a phospholipid concentration of 3.0%,a lipid to drug ratio of 30∶1,a phospholipid to cholesterol ratio of 2∶1,and an ultrasound time of 20 min.Under the optimal experimental conditions,the encapsulation efficiency of the prepared oleanolic acid liposomes was 98.8%.The particle size is(325±50)nm,with the zeta potential of-3.09 mv.

关 键 词：齐墩果酸 脂质体 薄膜分散法 正交优化实验 

分 类 号：TQ461[化学工程—制药化工] R943[医药卫生—药剂学]