苄达赖氨酸脂质体的制备

Preparation of Bendazac Lysine Liposome

以苄达赖氨酸、大豆卵磷脂、胆固醇为原料制备了苄达赖氨酸脂质体。以包封率为主要指标,选取药脂比、超声时间、水相pH值和孵育温度4个因素进行正交实验优化制备工艺,用紫外分光光度计测定包封率,用粒度和Zeta电位分析仪测定所制备脂质体的粒径分布及Zeta电位。确定最佳制备工艺条件为:药脂比1∶5(g∶g)、超声时间15min、水相pH值5、孵育温度60℃,在该条件下所制得的3批苄达赖氨酸脂质体的平均包封率为81.54%,平均粒径为(99.85±9.60)nm,平均Zeta电位为(-30.6±1.8)mV,体外释放实验证明释放速度慢于市售制剂。表明所制备的苄达赖氨酸脂质体包封率高、稳定性好。

Bendazac lysine liposome was prepared using bendazac lysine, soybean lecithin, and cholesterol as raw materials. With the encapsulation rate as the main index,the preparation process were optimized by an or- thogonal experiment with four factors,i, e. ,ratio of drug to lipid,ultrasonic time,pH value of water phase and incubation temperature. The encapsulation rate of the liposome was detected by UV spectrophotometry, and the particle size distribution and Zeta potential were determined by a particle size and Zeta potential analyzer.The optimal preparation conditions were as follows： ratio of drug to lipid of 1 ： 5（g ： g） ,ultrasonic time of 15 min, pH value of water phase of 5,and incubation temperature of 60 ℃. Under the optimal conditions, the average encapsulation rate of three batches bendazac lysine liposomes was 81.54% ,the average particle size was （99.85 ±9.60） nm and the average Zeta.potential was （-30.6±1.8） inV. Release experiment in vitro showed the release rate was slower than that of commercial preparations. The liposome has high encapsulation rate and good stability.