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以胶粒动电位为指标,采用正交设计方法对聚氰基丙烯醚异丁酯毫微粒的制各条件进行了优化。根据阿克拉霉素A在聚氰基丙烯酸异丁酯毫微粒上的吸附机理,以载药量与载药毫微粒动电位为指标,采用均匀设计方法优化了制备肝靶向阿克拉霉素A聚氰基丙烯酸异丁酯毫微粒的工艺条件,在优化工艺条件下制得的载药毫檄粒粒径分布在40~120nm范围,胶粒动电位为-15.47mV,载药量为48.76%,药物载带率为98.83%。粒径分布与动电位值均满足肝靶向要求,载物量与药物载带率均高于同类材料报道值。HPLC法证明了吸附法工艺制得的载药毫微粒中药物的稳定性。体外释药试验结果表明,载药毫微粒中药物的释放具缓择性。与一步法制得的载药毫微粒比较表明,阿克拉霉素A聚氰基丙烯酸异丁酯毫微粒的载药机理主要是吸附。
Using the kinetic potential of colloidal particles as an index, the conditions for the preparation of isobutyl polycyanoacrylate nanoparticles were optimized by orthogonal design. According to the adsorption mechanism of aclacinomycin A on the isobutyl polycyanoacrylate nanoparticles, taking the drug loading and the electrokinetic potential of the drug loaded nanoparticles as an index, the uniform design method was used to optimize the preparation of liver targeting aclacinomycin A Polybutyl cyanoacrylate nanoparticles conditions, the optimum conditions in the preparation of the drug delivery milligram particle size distribution in the 40 ~ 120nm range, gel dynamic potential of -15.47mV, the drug loading of 48 .76%, drug carrier rate was 98.83%. The particle size distribution and the dynamic potential value all meet the requirements of liver targeting, and the loading capacity and drug loading rate are higher than the reported values of similar materials. HPLC method to prove the stability of drug-loaded nanoparticles prepared by the adsorption process. In vitro release test results show that the release of drug-loaded nanoparticles in a slow release. Compared with the one-step drug-loaded nanoparticles, the main mechanism of drug loading of acylacline A isobutyl polyacrylate nanoparticles is adsorption.