吲哚美辛载药纳米胶束治疗大鼠实验性关节炎

Effect of indomethacin-loaded micelles on rheumatoid arthritis in rats

目的探索负载吲哚美辛的载药共聚物纳米胶束治疗类风湿性关节炎的作用。方法以大鼠叉菜胶型关节炎为模型,经关节腔内给药,评价载药纳米胶束的治疗效果。结果载药纳米胶束能够显著抑制足爪肿胀,且用胶束治疗的大鼠没有胃溃疡的产生。结论2种体内实验结果表明,吲哚美辛载药纳米胶束通过关节内注射能够达到持续治疗效能。局部注射给药还可避免口服给药所引起的严重的胃部刺激。

Objective To investigate the effect of indomethacin （IND）-loaded micelles on rheumatoid arthritis and its mechanism. Methods Freund＇ s-induced adjuvant arthritis and carrageenan-induced acute arthritis in SD rats were employed to evaluate the therapeutic effect of IND-loaded polymeric micelles after intraarticuar drug administration. Fifty-six SD rats were randomly divided to receive IND-loaded micelles at a dose of 4.5, 1.5, 0. 5 mg/kg respectively, IND injection, oral administration of IND, blank PNIPAm/EAB-PPP-1 micelles at the 8^th day once a day for a week after subcutaneous injection of 0. 1 ml Freund＇ s into voix pedis of the right hind foot. The normal control rats took normal saline instead of Freund＇ s. There were 8 rats in each group. Results IND-loaded micelles could inhibit the swollen joint. No rats of intraarticular drug administration developed ulceration. Conclusion The sustained therapeutic efficacy could be achieved through intraarticular injection of IND-loaded micelles. Local delivery of IND can avoid severe gastrointestinal stimulation that frequently results from oral administration of IND.