他克莫司纳米微球的制备及其体外释药性能

Preparation and release characteristics in vitro of tacrolimus nanospheres

目的采用甲氧基聚乙二醇-聚乳酸聚合物(PEG-PLA)制备他克莫司微球(PPT),研究其体外释药特性。方法考察PPT的载药量、包封率、粒径大小、粒径分布和药物体外释放实验。结果PPT的制备工艺稳定、重复性好,微球外形圆整,表面光滑,分布均匀,平均粒径为(545.1±0.9)nm,平均载药量为(18.90±3.22)%,平均包封率为(25.0±1.6)%,35d的药物累积释放率为67.21%。结论他克莫司微球缓释时间长达35d,能够满足临床治疗的要求。

Objective To prepare tacrolimus nanospheres and study their physical state and release characteristics in vitro. Methods Tacrolimus nanospheres were prepared by emulsion-solvent evaporation method with PEG-PLA. The nanospheres were characterized in terms of morphology, size, encapsulation efficiency, the rate of drug loading and in vitro drug release. The physical state of PPT was determined by scanning electron microscopy （SEM） and dynamic light scatter （ DLS）. Results The preparing technology was feasible. The formed nanospheres were spherical with smooth surfaces. The distribution of particle size was uniform and average particle size was （545.1 ±0.9）nm. The rate of drug loading was （18.90 ±3.22） % and the encapsulation efficiency was （25.0 ±1.6 ） %. In vitro release study revealed that the 35-day accumulated release percentage reached 67.21%. Conclusion The sustained release tacrolimus nanoshperes prepared by emulsion-solvent evaporation method can satisfy the clinical demand.