左氧氟沙星磁性明胶微球制备及其缓释性能

摘要

The preparation and sustained release properties of the levofloxacin magnetic gelatin mi-crospheres have been studied by using the emulsion crosslinking.The effects of the factors such as the ratio of levofloxacin to gelatin,water/oil ratio,concentration of gelatin and glutaraldehyde were dis-cussed.The optimal synthesis process was optimized by orthogonal experiment,and the release charac-teristics of levofloxacin magnetic gelatin microspheres were determined by dynamic dialysis method.The morphology and particle size of microspheres and the details of Fe3 O4 and levofloxacin embedding in ge-latin were investigated.The results show that the optimum preparation conditions of levofloxacin mag-netic gelatin microspheres are as follows:gelatin concentration is 1 5%,the ratio of levofloxacin to gelat-in is 1∶2,water/oil ratio is 1∶5,and the amount of glutaraldehyde is 3.6 mL.At the same time,the encapsulation efficiency and drug loading are 8.89% and 51.36%,respectively.The in vitro accumula-tived release amount of microspheres are 64% in artificial intestinal juice and 72% in artificial gastric j uice for 5 h,respectively,indicating that the drug microspheres has a good sustained release perform-ance,and the release process follows the first order kinetic equation.The magnetic gelatin micro-spheres has good sphericity and uniformity,and Fe3 O4 and levofloxacin are embedded in the gelatin.%采用乳化交联法研究了左氧氟沙星磁性明胶微球的制备及其缓释性能.选取左氧氟沙星与明胶的比例、水油比、明胶浓度、戊二醛用量四个因素进行正交实验,优化最佳合成工艺.采用动态透析法测定载药微球的体外释放特性,同时对载药微球的形态、粒径、磁性及包覆情况进行表征.结果表明,载药微球最佳制备工艺为：明胶浓度15%,左氧氟沙星明胶比1∶2,水油比1∶5,戊二醛用量3.6 mL；包封率为8.89%,载药量为51.36%；微球5 h体外累积释药百分率人工肠液中达到64%,人工胃液中达到72%,具有较好的缓释性能,体外释放符合一级动力学方程；磁性明胶微球成球性良好,分布均匀,Fe3 O4及左氧氟沙星被明胶包覆.