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目的使用3-羟基丁酸-co-3-羟基戊酸共聚物制备西罗莫司缓释微球,为预防和治疗角膜移植术后免疫排斥反应奠定基础。方法采用乳化-溶剂挥发法制备微球,正交实验法优化,测得载药量、包封率等指标,结合光镜观察其形态特征,得出最佳制备条件后,模拟眼内前房环境检测其体外释药性能。结果微球制备工艺稳定,重复性好。微球成球率高,形态圆整,表面光滑,载药量为(37.34±1.25)%,包封率为(99.63±0.93)%,能够在体外稳定缓释,500 h累积释药率为71%。结论西罗莫司缓释微球表征良好,载药量、包封率较高,有望发挥稳定释药的临床作用。
Objective To prepare sirolimus sustained-release microspheres using 3-hydroxybutyrate-co-3-hydroxyvaleric acid copolymer and to lay the foundation for the prevention and treatment of immunological rejection after keratoplasty. Methods The microspheres were prepared by emulsion - solvent evaporation method. The orthogonal test was used to optimize the drug loading and entrapment efficiency. Morphological characteristics of the microspheres were observed by light microscopy. After the optimal preparation conditions were obtained, Environmental testing of its in vitro release properties. Results Microspheres preparation process is stable and reproducible. The results showed that the microspheres had a high percentage of ball formation, round shape and smooth surface. The drug loading was (37.34 ± 1.25)% and the entrapment efficiency was (99.63 ± 0.93)%. 71%. Conclusion The sustained-release microspheres of sirolimus have good characterization, high loading capacity and high entrapment efficiency, which is expected to exert the clinical effect of stable drug release.