吡喹酮固体脂质纳米粒的研制

Preparation of solid lipid nanoparticles containing praziquantel

目的采用超声分散法制备吡喹酮固体脂质纳米粒,并考察制备过程中的主要影响因素。方法首先通过试验确定制备工艺参数,然后考察各处方因素对粒径大小和稳定性的影响,最后以包封率为评价指标,采用正交实验设计法确定最优处方。结果透射电镜测得纳米粒为类圆球状,粒径分布较均匀。动态光散射法测得样品的粒径为(100±21)nm,包封率为(79.3±0.69)%,平均zeta电位值为-66.3 mV。结论以山嵛酸甘油酯和乙酸丁酯为脂质材料,豆磷脂、泊洛沙姆188和硬脂酸钠为复配乳化剂,采用超声分散法可以简便、快速制得吡喹酮固体脂质纳米粒。

Objective To prepare solid lipid nanoparticles containing praziquantel （PZQ-SI,N） by ultrasonic technique, and investigate the main factors in the process of preparing PZQ-SI,N. Methods At first the parameters of technology were determined by experiments, then the affecting factors of the size and stability of PZQ-SLN were researched. On the basis of the single factor exploration, the satisfactory formulation was selected by orthogonal design with high entrapment efficiency as standard. Results The morphological investigation by transmission electron microscopy showed that the nanoparticles had round and uniform shapes. The mean diameters was （100± 21） nm, accordingly the drug entrapment efficiencies was （79. 3 ± 0.69） %, and the zeta potential was - 66.3 mV. Conclusions The solid lipid nanoparticles loaded with praziquantel can be readily and quickly prepared by ultrasonic technique, with Compritol 888 ATO and butyl acetate as matrix material, soybean lecithin, poloxamer 188 and sodium stearate as co-emulsifier.