微针条件下雷公藤甲素不同剂型对类风湿性关节炎大鼠皮肤损伤的研究

 目的 研究不同长度微电子机械系统（ MEMS）微针条件下，雷公藤甲素（TP）不同剂型对大鼠类风湿性关节炎（RA）模型皮肤损伤的影响。方法 制备TP丙二醇水溶液、脂质体、脂质体水凝胶贴剂3种剂型，采用Ⅱ型胶原诱导的大鼠RA模型，对大鼠左右侧皮肤分别作100和200 μm MEMS微针处理，用紫外分光光度法检测皮肤乳酸脱氢酶（LDH）活性。结果 给予MEMS微针处理后，大鼠皮肤LDH活性没有显著变化（P＞0.05）；TP不同剂型均使皮肤LDH活性明显升高（P＜0.05），其中溶液组升高最大（P＜0.001），脂质体组次之（P＜0.01），脂质体水凝胶贴剂组升高最小（P＜0.05），但是左右两侧皮肤比较无明显差异（P＞0.05）。结论 100和200 μm MEMS微针均可安全地用于RA大鼠的经皮给药促透；TP制备为脂质体水凝胶贴剂后可显著地减小对RA大鼠皮肤的损伤，是其透皮给药的理想剂型。

Effects of Different Triptolide Formulations Given by MEMS Micro-Needles on Skin Injury of Rheumatoid Arthritis Rats

OBJECTIVE To study the effects of different triptolide formulations given by micro electro mechanical systems(MEMS) micro-needles on skin injury of rheumatoid arthritis rats.METHODS Three formulations of triptolide were prepared including the aqueous solution of 20% propylene glycol,liposomes,and liposomes hydrogel patch.Rats with rheumatoid arthritis induced by collagen II were used,and 100 and 200 μm MEMS micro-needles treatment was performed on left and right sides of rat skin.The lactate dehydrogenase(LDH) activities were measured by ultraviolet spectro-photometric method.RESULTS After processed by MEMS micro-needle,the LDH activities of RA rat skin did not change obviously(P>0.05).All triptolide formulations increased LDH activities(P<0.05),and the increasement of solution group was largest(P<0.001),followed by lipsomes group(P<0.01) and liposomes hydrogel patch(P<0.05).Nevertheless,there was no significant difference between left and right sides of rat skin(P>0.05).CONCLUSION Both 100 and 200 μm MEMS micro-needles were safe for enhancement of transdermal delivery in rheumatoid arthritis rats.The skin injury was observably relieved when triptolide was prepared as liposomes hydrogel patch which is a perfect formulation for transdermal delivery of triptolide.