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

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.