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关节腔注射塞来昔布微球对大鼠类风湿性关节炎的治疗作用

Therapeutic effect of celecoxib-loaded microspheres on rheumatoid arthritis in rats after intra-articular injection

  • 摘要: 考察关节腔注射塞来昔布(CEL)聚乳酸-羟基乙酸共聚物(PLGA)微球对大鼠类风湿性关节炎的治疗作用。以PLGA为载体,采用O/W乳化溶剂挥发法制备塞来昔布微球(CEL-MS)。采用完全弗氏佐剂诱导佐剂型关节炎(AA)大鼠模型,以大鼠足跖肿胀度、关节炎指数、脾脏指数和关节滑膜组织病理学检查作为治疗效果的指标,考察关节腔注射CEL-MS对大鼠类风湿性关节炎的治疗作用。结果显示,微球的形态圆整、表面光滑,平均粒径为(2.1 ± 0.3)μm、载药量为(20.8 ± 0.6)%。体内药效实验结果显示,与灌胃给予塞来昔布混悬液和关节腔注射塞来昔布混悬液相比,在关节炎大鼠关节腔中注射CEL-MS可显著降低关节肿胀和关节炎指数,有效抑制滑膜炎症。以上结果表明,关节腔注射CEL-MS对大鼠类风湿性关节炎具有良好的治疗作用。

     

    Abstract: This study sought to assess the therapeutic effect of celecoxib (CEL)-loaded polylactic acid-glycolic acid copolymer (PLGA) microspheres on rheumatoid arthritis in rats after intra-articular injection.The celecoxib-loaded microspheres (CEL-MS) were prepared by the O/W solvent volatilization method with PLGA as carrier.In order to investigate the therapeutic effect of CEL-MS on rheumatoid arthritis in rats after intra-articular injection, a rat model of adjuvant arthritis (AA) was constructed by complete Freund''s adjuvant, and the evaluation indicators of the therapeutic effect were rat paw swelling, arthritis index,spleen index and joint synovial histopathological examination. The results showed that the microspheres had a smooth spherical morphology with a particle size of (2.1 ± 0.3) μm and a drug loading efficiency of (20.8 ± 0.6)%.The results of the in vivo efficacy test showed that intra-articular injection of CEL-MS compared to the CEL suspension oral and the celecoxib suspension intra-articular injection in adjuvant arthritis rat model can significantly reduce joint swelling and arthritis index, thus effectively inhibiting synovial inflammation.The above results indicate that intra-articular injection of CEL-MS has a good therapeutic effect on rheumatoid arthritis in rats.

     

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