环孢素A脂质体制备及其体外释药方法学考察  

Studies on Preparation and Releasing of Cyclosporin A Liposome in Vitro

作　　者：许洁[1,2] 杨志强[1] 潘萍[1] 张学农[1] 吴函珊 

机构地区：[1]苏州大学药学院,江苏苏州215123 [2]07届药学本科毕业实习生

出　　处：《抗感染药学》2008年第4期222-227,共6页Anti-infection Pharmacy

基　　金："江苏省科技厅社会发展项目资助(编号:BS200522);江苏省高新技术产业发展项目资助(编号:JHB05-46);江苏省卫生厅招标课题(编号:H200630);苏州大学医学发展基金资助(编号:EE132503)

摘　　要：目的:考察环孢素A(cyclosporin A,CsA)脂质体的制备方法、理化性质及其体外释放行为。方法:比较薄膜分散法、逆向蒸发法、乙醇注入法、乙醚注入法所得的环孢素A脂质体(CsA-Lip),并以包封率和载药量为综合指标,正交设计优化CsA-Lip处方工艺;分别采用动态透析法和超速离心法研究CsA-Lip的体外释放行为。结果:乙醇注入法制备CsA-Lip的平均粒径为(80.41±3.12)nm,包封率为(87.09±0.03)%,载药量为(4.98±0.45)%,24 h释放44%。结论:经优化制备的CsA脂质体具有较高的包封率和载药量,并具有缓释作用。Objective： To study the preparation methods of Cyclosporin A liposome（CsA-Lip） and its characteristics in vitro. Methods： Selecting a proper method from thin film vesicle, reverse-phase evaporation, ethanol-injection and ether-injection technique. The optimized formulation was screened by orthogonal experimental design with entrapment efficiency and loading quality of CsA-Lip as general indexes. The CsA release from drug-loaded liposome was investigated with bag filter and ultracentrifugation in vitro. Results： The particle size, the entrapment efficacy and drug loading of CsA-Lip prepared with ethanol-injection were （80.41 ± 3.12）nm, （87.09 ±0.03）% and （4.98 ± 0.45）% respectively. 44% of total drug was released during the first 24 h. Conclusion： Ethanol-injection was convenient to prepare CsA-Lip which was high in entrapment efficiency and loading and had the advantages of sustained release.

关 键 词：环孢素A 脂质体 体外释放 超速离心 

分 类 号：R94[医药卫生—药剂学]