粉防己碱阿霉素脂质体的制备与体外释放度的研究

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1:20,磷脂与胆固醇质量的比例为3:1、外水相pH值为7.6,孵育温度50℃、硫酸铵浓度为250 mmol/L.释放度试验显示脂质体中阿霉素和粉防己碱分别在24 h和16 h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.

Preparation of tetrandrine-doxorubicin complex liposomes and its release property in vitro

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 (NH_4)_2SO_4 -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 (NH_4)_2SO_4 was 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