蚓激酶脂质体的制备及质量评价

目的优选蚓激酶脂质体的制备工艺。方法采用薄膜超声分散法制备蚓激酶脂质体,以包封率为指标通过正交试验法优选制备处方和工艺,并考察制备脂质体的包封率、形态、粒径分布、Zeta电位及在体外释放规律。结果卵磷脂100mg、胆固醇20mg、蚓激酶1mg、PBS 15mL、pH6.6时包封率最高,电子显微镜下为囊状小球,测得3批蚓激酶脂质体的平均包封率为30.5%,平均粒径424 nm,Zeta电位为-49.68 mV,体外释放符合一级动力学释放规律。结论采用薄膜分散法制备蚓激酶脂质体工艺简单,包封率适宜,体外释放迅速。

Preparation and Quality Evaluation of Lumbrukinase Liposomes

Objective To optimize the preparation process for lumbrokinase liposomes.Methods The lumbrukinase liposomes were prepared by thin-film ultrasound dispersion method.The preparation process for lumbrukinase liposomes was optimized by orthogonal design with entrapment ratio as optimization index.During the preparation of lumbrukinase liposomes,we investigated the encapsulation efficiency,liposome shape,liposome diameter,Zata potential and in-vitro release.Results Entrapment ratio reached its highest value when lecithin was 100mg,cholesterol was 20mg,lumbrukinase was 1mg,PBS was 15mL and pH value was 6.6.The entrapped vesicles could be seen under electron microscope.For the 3 batches of liposomes,we obtained their average entrapment ratio being 30.5 %,average particle size at 424 nm,and Zeta potential at-49.68 mV.In-vitro release was fitted to first-order kinetic equation.Conclusion The preparation of lumbrukinase liposomes by thin-film ultrasound dispersion method is easy,with appropriate entrapment ratio and rapid in-vitro release.