【摘要】 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。更多还原

【Abstract】 potential was used as a criterion for optimizing formula and technology for poly-isobutylcyanoacrylate nanoparticles(IBC-NP )prepared by orthogonal design.ξ potential was-59.40 mV of the IBC-NP that was prepared in optimized condition;This value was significantlyhigher than that reported by others. According to the mechanism of aclacinomycin A(ACM)ad-sorbed onto IBC-NP,the drug loading and ξ potential were used as criteria for optimizing formulaand technology for aclacinomycin A polyisobutyl-cyanoacrylate nanoparticles(ACM-IBC-NP) pre-pared by uniform design. The ACM-IBC-NP can be prepared in this condition in which drug load-ing was 48.76%,drug embedding ratio was 98.83%,ξpotential was-15.47 mV,average diame-ter of nanoparticles was 78.26 nm,and dispersity of nanoparticles was 0 25.The value of drugloading and drug embedding ratio was the highest in reported articles on IBC-NP. The average di-ameter and potential all conformed to the requirements of liver targeting,The stability of ACM inACM-IBC-NP was proved by HPLC. The characteristics of sustained release of ACM in ACM-IBC-NP were also shown by drug release test in vitro,The main mechanism of ACM Ioaded byIBC- NP was adsorption.更多还原