主动载药法制备三氧化二砷脂质体  

Preparation of arsenic trioxide liposome by active drug-loading method

作　　者：王晓瑜[1,2] 马满玲[2] 

机构地区：[1]武警后勤学院附属医院药剂科,天津300061 [2]哈尔滨医科大学附属第一医院药学部,黑龙江哈尔滨150001

出　　处：《中草药》2014年第5期648-651,共4页Chinese Traditional and Herbal Drugs

基　　金：黑龙江省科学技术计划项目(GB05C401-04)

摘　　要：目的采用主动载药法制备三氧化二砷(As2O3)脂质体,并优化处方组成,考察主动载药法制备As2O3脂质体的可行性。方法采用正交设计法筛选处方,主动载药法制备As2O3脂质体;用葡聚糖凝胶G-50柱分离脂质体和游离药物,用原子荧光分光光度法测定包封率;用电镜观察脂质体的外观形态,并用激光粒径分析仪测定脂质体的粒径和Zeta电位;并进一步考察其优势。结果所得脂质体的包封率为(72.3±0.8)%;形态为粒径均匀的球形或类球形,粒径为(193±12)nm,Zeta电位为(36.1±3.0)mV;脂质体具有良好的安全性与较好的稳定性。结论优选得到的As2O3脂质体处方和制备工艺合理,并且所制备的As2O3脂质体具有良好的安全性。Objective To prepare arsenic trioxide （As2O3） liposome, to optimize the formulation ofAs203 liposomes, and to study the feasibility of As2O3 liposomes prepared by the active drug-loading. Methods Liposomes were prepared by the active drug-loading method. An orthogonal test was utilized to optimize the formulation and preparation of As2O3 liposomes. The unencapsulated As2O3 and liposomes were separated by Sephadex gel G-50 column, the entrapment efficiency （EE） was detected by atomic fluorescence spectrophotometry. The morphological examination of As2O3 liposomes was performed using transmission electron microscopy. The particle size and Zeta potential of the liposomes were measured. The advantage of As2O3 liposomes made by active drug-loading method was investigated. Results The EE of the liposomes was （72.3 ± 0.8）%, the morphology of liposomes was spherical or ellipsoidal shape with uniform particle size, the mean partical size was （193±12） nm, and Zeta potential was （36.1 ± 3.0） mV. Liposomes have good safety and better stability. Conclusion The selected formulation and preparation technique ofAs2O3 liposomes could be rational and stable, and the prepared As2O3 liposomes have Rood safety.

关 键 词：三氧化二砷 脂质体 正交设计 主动载药法 包封率 

分 类 号：R283.6[医药卫生—中药学]