眼用左氧氟沙星聚氰基丙烯酸正丁酯毫微粒制备及药剂学特征研究

Preparation of Levofloxaci-polybutylcyanoacrylate-nanoparticles

目的:制备左氧氟沙星聚氰基丙烯酸正丁酯毫微粒(LF-PBCA-NP)。方法:以氰基丙烯酸正丁酯为聚合材料,应用L9(34)正交试验、均匀设计法精选,优化制备工艺。结果:制备PBCA-NP的优化条件为反应液pH2.5,Pluronic F68的含量为1.5%,Dextron70的含量为1%,优化条件下制备LF-PBCA-NP平均粒径为51nm,包封率95.7%,载药量50.3%。结论:经过优化筛选出了LF-PBCA-NP的最佳制备工艺;LF-PBCA-NP有望成为一种新的药物靶向载体系统。

Objective： To prepare Levofloxaci-polybutylcyanoacrylate-nanoparticles （LF-PBCA- NP）. Methods ： LF-PBCA-NP was prepared by emulsing polymerization method with polybutyleyanoacrylate as carriermaterial; the procedure was optimized by L9 （3^4） of orthogonal-design experiments and umiformdesign testwith the ebedding ratio and drug loading as the test standard. Results： The pH 2 . 5, 1.5% Pluronic F68 and 1. 0% dextrin 70 was the optimum condition for the preparation of PBCA-NP. Under this optimum condition, the mean diameter of the nanoparticles was 51 nm, the mean ebedding ratio was 95.7%, the mean drug loading was 50.3%. Conclusion： The obtained condition is the best preparation procedure of LF-PBCA- NP. It is expected to become a new drug targeting carrier system.