盐酸维拉帕米脂质体的制备及其影响因素

 目的 制备盐酸维拉帕米脂质体，并对处方和制备过程中的影响因素进行考察。 方法 分别以被动载药法和硫酸铵梯度法制备盐酸维拉帕米脂质体，对处方进行优化，并考察硫酸铵梯度法的影响因素。测定其粒径、 Zeta 电位和稳定性。 结果 硫酸铵梯度法所得包封率远大于被动载药法，且受硫酸铵浓度、载药温度和载药时间的影响。按优化的处方和工艺制备的盐酸维拉帕米脂质体，包封率大于 95 % ，平均粒径 136 nm ，粒径分布均匀， Zeta 电位为 - 13.4 mV ，稳定性良好。 结论 采用硫酸铵梯度法可成功制备盐酸维拉帕米脂质体，通过对处方和工艺进行优化，可以达到很高的包封率和良好的稳定性。

Preparation of Liposomes Containing Verapamil Hydrochloride and Its Influencing Factors

OBJECTIVE To prepare verapamil hydrochloride (VH) liposomes and investigate the formulation and influencing factors in the preparing process. METHODS VH liposomes were prepared by passive loading and ammonium sulfate gradients methods, respectively. The formulation was polished, and the influencing factors of ammonium sulfate gradients method were investigated. The particle size distribution and Zeta potential were determined, and the stability of liposomes was studied. RESULTS ■The entrapment efficiency obtained from ammonium sulfate gradients was much higher than that of passive loading methods, and was influenced by the concentration of ammonium sulfate, the loading temperature and the loading time. VH liposomes prepared by the optimized formulation and process showed an entrapment efficiency above 95%, an average diameter of 136 nm, a Zeta potential of -13.4 mV and a good stability. CONCLUSION VH liposomes were successfully prepared by ammonium sulfate gradients. High entrapment efficiency and good stability were obtained by the optimization of formulation and preparing process.