槐定碱脂质体的制备及理化性质研究

Study on preparation of sophoridine liposomes and its physicochemical properties

目的:考察槐定碱脂质体处方工艺,并研究其理化性质。方法:以包封率为主要指标,采用逆相蒸发法制备槐定碱脂质体,用正交试验筛选优化最佳处方工艺,并考察脂质体的形态、粒径、Zeta电位、包封率、体外释放度及稳定性等理化性质。结果:槐定碱脂质体在电镜下呈类圆形,平均粒径为(232±11)nm,药物包封率为(50.8±1.6)%,Zeta电位为-32.6mV,体外45h累积释放率为89%,在冷藏条件下较稳定。结论:槐定碱脂质体包封率为(50.8±1.6)%,带负电,粒径分布均匀,为槐定碱制备成靶向制剂提供了参考。

OBJECTIVE To investigate the formulation of sophoridine liposomes, and determine its physicochemical properties. METHODS Sophoridine liposomes were prepared through a reverse evaporation technique and the formulation was optimized with entrapment efficiency as the optimized index by an orthogonal design. Then the liposomes were characterized in terms of shape, particle size, zeta potential, entrapment efficiency, in vitro release and its stability. RESULTS Sophoridine liposome prepared by reverse evaperation was uniform and round, its mean particle size was （232 ±11 ）nm, the entrapment effi ciency was （50. 75± 1.63）%, Zeta potential was - 32.6 mV, the release kinetics of sophoridine from liposome was conformed to bioexponential equation and the stability temperature of sophoridine liposome was 4℃. CONCLUSION The entrapment efficiency of sophoridine liposome is （50. 75 ± 1. 63）%, and with negative charge, its particle size distribution is uniform, and providing reference for sophoridine targeted preparation research.