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目的制备环孢素脂质体并进行质量评价。方法用薄膜-超声分散法制备环孢素脂质体,以包封率为评价指标,正交设计法优化处方和工艺,用HPLC法测定环孢素的含量,并观察其形态、粒径和稳定性。结果用混合磷脂制备环孢素脂质体的最优处方是磷脂和胆固醇的质量比为4∶1,磷脂在水化介质中的浓度为3%,药物和磷脂的质量比为1∶40,水化介质为pH=7.4的磷酸盐缓冲液;最佳的工艺条件为水化温度45℃,水化时间30min,搅拌时间10min,超声时间2h。按该处方工艺制备的脂质体包封率为97.84%,98.2%的粒径为(32.65±5.46)nm。在4℃冰箱存放5个月后形态和粒径无明显变化,渗漏率为4.55%。结论制备的环孢素脂质体包封率高、粒径小、稳定性好。
Objective To prepare cyclosporine liposomes for quality evaluation. Methods Cyclosporine liposomes were prepared by membrane-ultrasonic dispersion method. The encapsulation efficiency was used as the evaluation index. The orthogonal design method was used to optimize the formulation and technology. The content of cyclosporine was determined by HPLC. The morphology, stability. Results The optimum formulation for preparing cyclosporine liposomes with mixed phospholipids was that the mass ratio of phospholipid to cholesterol was 4: 1, the concentration of phospholipid in hydration medium was 3%, the mass ratio of drug to phospholipid was 1:40, The hydration medium was pH = 7.4 phosphate buffer; the optimum conditions were: hydration temperature 45 ℃, hydration time 30min, stirring time 10min, ultrasonic time 2h. The encapsulation efficiency of the liposome prepared by the prescription process was 97.84%, and the particle size of 98.2% was (32.65 ± 5.46) nm. There was no obvious change in morphology and particle size after 5 months in 4 ℃ refrigerator, the leakage rate was 4.55%. Conclusion Cyclosporine liposomes have high encapsulation efficiency, small particle size and good stability.