表面修饰唾液酸的唑来膦酸与多柔比星共载脂质体的制备
发布时间：2019-02-17 17:49
【摘要】：目的建立唑来膦酸与多柔比星包封率的测定方法,以包封率为指标优化唑来膦酸与多柔比星共载脂质体的处方及制备工艺,以期获得包封率高、稳定性好的制剂。方法将唑来膦酸配制成铵溶液作为水化介质,使用改良乙醇注入法制备唑来膦酸脂质体,在此基础上通过铵梯度法主动包载多柔比星以实现两种药物在脂质体中的共载。分别采用G-150葡聚糖凝胶微柱-高效液相色谱法与阳离子交换纤维微柱-紫外可见分光光度法测定唑来膦酸与多柔比星的包封率,通过对脂质体外水相中唑来膦酸的去除及对水化介质中阴离子浓度的考察,优化脂质体的处方与制备工艺。结果最优处方与工艺下制备的共载脂质体粒径约为110 nm,Zeta电位为-0.87 m V,其中唑来膦酸的包封率为6.5%,多柔比星的包封率大于90%。脂质体于4℃下避光放置60 d,粒径和包封率均无显著性变化,稳定性良好。结论唑来膦酸与多柔比星共载脂质体的包封率较高,稳定性较好。
[Abstract]:Objective to establish a method for the determination of the entrapment efficiency of zoledronic acid and doxorubicin, and to optimize the formulation and preparation process of liposomes co-loaded with zoledronic acid and doxorubicin with high entrapment efficiency and good stability. Methods Zoledronic acid was prepared into ammonium solution as hydration medium and liposomes were prepared by modified ethanol injection method. Doxorubicin was encapsulated by ammonium gradient method to realize the co-loading of two drugs in liposomes. The encapsulation efficiency of zoledronic acid and doxorubicin was determined by G-150 dextran gel microcolumn and cationic exchange fiber microcolumn UV-visible spectrophotometry, respectively. The formulation and preparation process of liposomes were optimized by the removal of zoledronic acid from the aqueous phase of liposomes and the investigation of anion concentration in hydrated media. Results the particle size of the cocarrier liposomes prepared by the optimal formulation and process was about -0.87mV with a potential of -0.87mV. The entrapment efficiency of zoledronic acid was 6.5, and that of doxorubicin was more than 90m. The particle size and entrapment efficiency of liposomes kept at 4 鈩，
本文编号：2425431
[Abstract]:Objective to establish a method for the determination of the entrapment efficiency of zoledronic acid and doxorubicin, and to optimize the formulation and preparation process of liposomes co-loaded with zoledronic acid and doxorubicin with high entrapment efficiency and good stability. Methods Zoledronic acid was prepared into ammonium solution as hydration medium and liposomes were prepared by modified ethanol injection method. Doxorubicin was encapsulated by ammonium gradient method to realize the co-loading of two drugs in liposomes. The encapsulation efficiency of zoledronic acid and doxorubicin was determined by G-150 dextran gel microcolumn and cationic exchange fiber microcolumn UV-visible spectrophotometry, respectively. The formulation and preparation process of liposomes were optimized by the removal of zoledronic acid from the aqueous phase of liposomes and the investigation of anion concentration in hydrated media. Results the particle size of the cocarrier liposomes prepared by the optimal formulation and process was about -0.87mV with a potential of -0.87mV. The entrapment efficiency of zoledronic acid was 6.5, and that of doxorubicin was more than 90m. The particle size and entrapment efficiency of liposomes kept at 4 鈩，
本文编号：2425431
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