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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。
Objective To study the in vitro release behavior of sirolimus sustained-release microspheres and its inhibitory effect on lymphocyte proliferation. Methods The sirolimus sustained-release microspheres were prepared by emulsion-solvent evaporation method. The microspheres morphology was observed by transmission electron microscopy. The drug loading, encapsulation efficiency and drug release rate in vitro were determined. The inhibitory rate of sustained release microspheres on human lymphocytes was detected by MTT assay. Results The average particle size of the sustained release microspheres of sirolimus was (186.73 ± 12.62) nm, the drug loading was (28.74 ± 2.63)% and the entrapment efficiency was (73.53 ± 7.12)%. In vitro stable release, release within 24 h 47.3%, 168 h cumulative release rate of about 93.15%. The inhibitory rates of sirolimus sustained-release microspheres on lymphocyte proliferation were 18.28%, 33.96%, 50.24%, 73.91% and 83.02% after cultured for 12, 24, 48, 72 and 96 h respectively. Conclusion The sustained release microspheres of sirolimus have a good in vitro sustained release effect and inhibit the proliferation of lymphocytes.