载蟾毒灵聚氰基丙烯酸正丁酯纳米粒的制备及其评价

Preparation and evaluaiton of bufalin coated PBCA nanoparticles

目的以聚氰基丙烯酸正丁酯(PBCA)纳米粒为载体,制备包载中药单体蟾毒灵的纳米粒制剂。方法采用醇中聚合法制备了包载蟾毒灵的PBCA纳米粒,通过单因素试验及正交试验设计对制备工艺进行考察,并测定了纳米粒的粒径分布、形态、包封率、载药量及溶血性等理化性质。结果醇中聚合法制备的蟾毒灵PBCA纳米粒形态均匀,平均粒径为(151.2-6.1)nm,多分散系数为0.133±0.024,Zeta电位为(-7.09±0.58)mV,包封率为(70.812±6.139)%,载药量为(1.990±0.291)%;与蟾毒灵原料药相比,该制剂的溶血性更低,安全性有所提高。结论蟾毒灵PBCA纳米粒的制备方法,可有效缩短中药单体与酸性介质的接触时间,制得的纳米粒各项理化性质良好,可为易水解中药单体纳米粒载体的制备提供新思路。

Objective To prepare poly-n-butylcyanoacrylate （PBCA） nanoparticles entrapped a Chinese medicine monomer of bufalin. Methods Alcohol polymerization method was adopted to prepare bufalin PBCA nanoparticles and the preparation process was optimized by single factor experiment and orthogonal test design, while size distribution, morphology, encapsulation efficiency （EE）, drug loading and hemolytic of the prepared nanoparticles were systemly analyzed. Results The obtained nanoparticles were regular in shape with average particle size of （151.2 ± 6.1） nm, as well as a poly-dispersity index of 0.133 ± 0.024. The Zeta potential and EE of bufalin PBCA nanoparticles were （-7.09 ± 0.58） mV and （70.812 ± 6.139）%, respectively. Drug loading of PBCA nanoparticles is （1.990 ± 0.291）%. Moreover, less hemolysis and improved safety were appeared in the formulation group, comparing with the bulk drug group. Conclusion Alcohol polymerization method, a method to prepare PBCA nanoparticles which exhibites good physical and chemical properties, can effectively reduce the exposure time of the Chinese medicine monomer in the acidic media. It may provide a new idea for the preparation of nanocarrier of easily hydrolyzed monomer.