盐酸阿霉素-黄芪甲苷脂质体制备工艺研究  

Study on the Preparation Technology of Doxorubicin Hydrochloride-astragaloside IV Liposome

作　　者：王成祥[1] 岳贵娟 秦楠坤 张婉乔 于梦琦 王莉婷 徐广 马群[1] WANG Chengxiang;YUE Guijuan;QIN Nankun;ZHANG Wanqiao;YU Mengqi;WANG Liting;XU Guang;MA Qun(Beijing University of Chinese Medic ine,Beijing 102488,China)

机构地区：[1]北京中医药大学,北京102488

出　　处：《辽宁中医药大学学报》2021年第6期32-37,共6页Journal of Liaoning University of Traditional Chinese Medicine

摘　　要：目的优选盐酸阿霉素-黄芪甲苷脂质体(LPs-DOX/AS)的制备工艺条件。方法通过单因素试验考察了脂质体制备方法、游离药物去除方式、孵育温度对脂质体制备的影响;以盐酸阿霉素、黄芪甲苷的包封率与载药量为考察指标,采用L9(34)正交试验,考察了磷脂浓度、磷脂与胆固醇的比例、药脂比对LPs-DOX/AS制备工艺的影响,并对所制得脂质体的粒径大小、微观形态和药物包封率及载药量等进行表征。结果 LPs-DOX/AS最佳制备工艺条件:磷脂浓度为8 mg/mL,磷脂与胆固醇比为10∶1,药脂比为1∶5。所制备的脂质体粒径为(102.6±0.2)nm,大小分散均匀;盐酸阿霉素的包封率和载药量分别为(98.57±0.49)%、(4.62±0.02)%,黄芪甲苷的包封率和载药量分别为(99.37±0.08)%、(14.45±0.04)%。结论优选工艺所制备的LPs-DOX/AS包封率和载药量较高,大小分散均匀,为LPs-DOX/AS的进一步研究奠定了基础。Objective To optimize the preparation conditions of doxorubicin-astragaloside IV liposomes(LPs-DOX/AS). Methods The effects of liposome preparation method,free drug removal method,and incubation temperature on liposome preparation were investigated through a single factor test. The effects of the influences such as the concentration of phospholipid,the ratio of phospholipid to cholesterol and the ratio of drug to lipid on preparation process of LPs-DOX/AS were studied by using L9(34)orthogonal test with standard of encapsulation rate and drug loading of doxorubicin hydrochloride and astragaloside IV as research indicators. The particle size,microscopic morphology,drug encapsulation rate and drug loading of the prepared liposomes were characterized. Results The optimal preparation conditions of LPs-DOX/AS was selected as follows:phospholipid concentration was 8 mg/mL,phospholipid to cholesterol ratio was 10∶1,and drug-lipid ratio was 1∶5. The particle size of the prepared liposome was(102.6±0.2)nm,the size was uniformly dispersed. The encapsulation rate and drug loading of doxorubicin were(98.57±0.49)% and(4.62±0.02)%,and the encapsulation rate and drug loading of astragaloside IV were(99.37±0.08)% and(14.45±0.04)%. Conclusion The LPs-DOX/AS prepared by the optimized process has high encapsulation efficiency and drug loading,and the size is uniformly dispersed,which provides a foundation for further research of LPs-DOX/AS.

关 键 词：阿霉素 黄芪甲苷 脂质体 正交设计 制备工艺 

分 类 号：R284[医药卫生—中药学]