西罗莫司缓释微球的制备及其对淋巴细胞增殖的抑制作用研究

Preparation and inhibitory effect of sirolimus sustained-release microsphere on lymphocyte proliferation

目的研究西罗莫司缓释微球的体外释药行为及其对淋巴细胞增殖的抑制作用。方法用乳化-溶剂挥发法制备西罗莫司缓释微球,用透射电子显微镜观察微球形态,测定载药量、包封率、体外释药率。用噻唑蓝(MTT)法检测缓释微球对人淋巴细胞的抑制率。结果西罗莫司缓释微球平均粒径为(186.73±12.62)nm,载药量为(28.74±2.63)%,包封率为(73.53±7.12)%。在体外稳定缓释,24 h内释药量达到47.3%,168 h后累计释药率约为93.15%。培养12,24,48,72,96 h后,西罗莫司缓释微球对淋巴细胞增殖抑制率分别为18.28%,33.96%,50.24%,73.91%,83.02%。结论西罗莫司缓释微球具有良好的体外缓释效果和抑制淋巴细胞增殖的作用。

Sirolimus Methods To study the preparation and inhibitory effect of sustained -release microsphere on lymphocyte proliferation. The sirolimus sustained- release microspheres were prepared by the emulsion solvent evaporation. The morphology of microspheres were observed by transmission electron microscope. The inhibitory rate of sirolimus sustained - release microspheres on human lymphocyte were detected by MTT assay. Results The average particle size of the micro- spheres was （ 186. 73 ± 12.62 ） μm, drug loading was （28.74 ±2.63） %, encapsulation efficiency was （ 73.53 ± 7. 12 ） %. Sirolimus sustained - release microspheres can stably release in vitro, the cumulative release rate of 24 h was 47.3%, the cumulative release rate of 168 h was 93.15%. After the culture of 12, 24, 48, 72, 96 h, the inhibition rate of proliferation of the microspheres was 18.28%, 33.96%, 50. 24%, 73.91%, 83.02%. Conclusion Sirolimus sus- tained- release microspheres had good sustained -release effect in vitro and inhibition of lymphocyte proliferation, providing the basis for the new formulation of sirolimus.