目的以阿霉素和粉防己碱为模型药物制备脂质体并进行工艺研究,同时对该脂质体进行体外释放度的研究。方法采用3种不同脂质体制备方法,并以包封率为指标采用正交设计法进行处方筛选和工艺优化。结果确定了硫酸铵梯度法结合pH梯度法制备脂质体的最佳制备处方为:药脂比为∶20,磷脂与胆固醇质量的比例为3∶、外水相pH值为7.6,孵育温度50℃、硫酸铵浓度为250mmol/L。释放度试验显示脂质体中阿霉素和粉防己碱分别在24h和6h内完全释放。结论制备的粉防己碱阿霉素脂质体包封率及外观良好,具有一定的缓释效果。

Objective Selecting doxorubicin and tetrandrine as model drug to prepare complex liposomes, study the methods of preparation, and research its release property in vitro. Methods The formulation of tetrandrine-doxorubicin complex liposomes was optimized by three different kinds of methods. And the optimum formula was selected through the orthogonal test according to the entrapment efficiency. Results Tetrandrine-doxorubicin complex liposomes were prepared by (NH₄)₂SO₄-gradient method combined with pH gradient method. One optimum recipe was founded that tetrandrine-doxorubicin complex liposomes/egg phosphatidyl choline was 1∶20, egg phosphatidyl choline/cholesterol was 3∶1, pH value was 7.6, incubation temperature was 50 ℃, concentration of (NH₄)₂SO₄was 250 mmol/L. The doxorubicin completely released within 24 h, and the tetrandrine released within 16 h. Conclusion Tetrandrine-doxorubicin complex liposomes have high entrapment efficiency with fine-looking, which is better for the further studies