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目的制备利福平聚乳酸-羟基乙酸共聚物(PLGA)微球-原位凝胶复合给药系统用于结核病局部给药,以达到局部滞留、缓慢释放的作用。方法采用液中干燥法制备微球,用海藻酸钠制成离子敏感型原位凝胶,考察微球以及复合给药系统的体外药物释放情况,初步考察复合给药系统在大鼠肺部的胶凝时间。结果微球平均粒径为149.569μm,包封率(n=3)为(69.43±3.53)%,载药量(n=3)为(26.43±3.10)%,体外释放实验表明,微球-原位凝胶复合给药系统有抑制药物突释的作用,且药物在30 d内释放25%,大鼠肺部胶凝实验表明,离子敏感型原位凝胶在大鼠肺部可滞留6 h。结论利福平PLGA微球-原位凝胶复合给药系统达到了局部滞留、缓慢释放药物的目的。
Objective To prepare paclitaxel polylactic acid - glycolic acid copolymer (PLGA) microspheres - in situ gel composite delivery system for local administration of tuberculosis in order to achieve local retention and slow release. Methods The microspheres were prepared by liquid-drying method. Ion-sensitive in situ gels were prepared by sodium alginate. The in vitro drug release of the microspheres and the compound drug delivery system was investigated. The effects of the compound drug delivery system in the lungs of rats Gel time. Results The average diameter of the microspheres was 149.569μm, the encapsulation efficiency was (69.43 ± 3.53)% and the drug loading (n = 3) was (26.43 ± 3.10)%. In-situ gel compound delivery system can inhibit the burst of drug, and the drug release 25% within 30 d, rat lung gel test showed that ion-sensitive in situ gel can be retained in rat lung 6 h Conclusion The rifampicin PLGA microspheres - in-situ gel composite delivery system achieved the local retention, the purpose of slow release of drugs.