【摘要】 目的:制备粉防己碱-阿霉素复合脂质体并对其工艺及质量进行研究与评价,为临床上逆转肿瘤的多药耐药提供新的思路。方法:采用3种不同脂质体制备方法,并以包封率为指标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梯度法制备复合脂质体的最佳处方最佳处方为:药脂比1∶20,磷脂-胆固醇比例3∶1,外水相pH值为7.6,硫酸铵浓度为250mmol/L。以该处方制备的脂质体DOX的平均包封率为90.77%,TET的平均包封率为80.12%。结论:该处方制备的粉防己碱-阿霉素复合脂质体包封率及外观良好,在低温充氮条件下较稳定,为进一步实验奠定了基础。更多还原

【Abstract】 Objective:To prepare doxorubicin-tetrandrine complex liposomes for technology study and quality control.In order to provide a new idea to reverse the tumor multidrug resistance in clinic.Methods:The formulations of doxorubicin-tetrandrine complex liposomes were optimized by three different kinds of methods.And the optimum formula was selected according to the entrapment efficiency.Re- sults:The complex liposomes were prepared by(NH4)2SO4-gradient method combined with pH gradient method according to optimum recipe.The optimum recipe of DOX-TET liposome was founded as DOX-TET/EPC of 1∶10,EPC/Ch of 3∶1,pH value of 7.6,incubation temperature of 50℃,(NH4)2SO4 concentration of 250 mmol/L.Under the formulation,DOX and TET were encapsulated 90.77%and 80.12%,respectively.Conclusion:The doxorubicin-tetrandrine complex liposomes have high entrapment efficiency with fine looking, which provides basis for the further studies.更多还原