蚓激酶壳聚糖亚微粒的制备工艺研究

The preparation of lumbrokinase chitosan nanoparticles

目的:以蚓激酶为模型药物,研制壳聚糖亚微粒并优化其制备工艺。方法:以离子交联法制备壳聚糖亚微粒,以包封率为指标通过单因素筛选和正交试验优化其制备工艺,并观测其形态、粒径和Zeta电位。结果:三聚磷酸钠质量浓度为2g.L-1、壳聚糖为2g.L-1、蚓激酶1.5mg、搅拌时间10min时包封率最高,电子显微镜下可见较圆整的球形微粒,测得3批蚓激酶-壳聚糖-亚微粒(LK-CS-NP)的包封率为77.03%,载药量为5.39%,平均粒径为280.7nm,Zeta电位为+37.55mV。结论:蚓激酶壳聚糖亚微粒制备工艺简单、包封率高、亚微粒成形良好。

OBJECTIVE To prepare chitosan nanoparticles and to optimize its formulation with lumbrukinase as model drug. METHODS The chitosan nanoparticles were prepared by ion cross-linking methods, and its formulation was optimized by single factor screening and orthogonal test designing, and its entrapment ratio, form, size and zeta potential were determined. RESULTS Entrapment ratio reached its highest when sodium tripolyphosphate was 2 g·L^-1, chitosan was 2 g·L^-1, lumhrokinase was 1.5 mg,and stirring time was 10 min. Three lots of the nanoparticles were prepared,whose particles were seen round with elctron microscope, entrapment ratio was 77. 03 %, drug loading was 5.39%, average particle size was 280. 7 nm, and zeta potential was ＋ 37. 55 mV. CONCLUSION The formulation and technique of LK-CS-NP was easy, whose entrapment ratio was high and form was good.