雷公藤甲素甘油醇质体与凝胶贴膏经皮给药改善大鼠佐剂型关节炎症状的比较研究  

Comparison of therapeutic effect of triptolide-loaded glycerol-mediated ethosomes and gel plasteron adjuvant arthritis via percutaneous administration

作　　者：朱春赟 张永太[1] 郭腾[1] 顾一帆 倪佳依 冯年平[1] ZHU Chunyun;ZHANG Yongtai;GUO Teng;GU Yifan;NI Jiayi;FENG Nianping(School of Pharmacy,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China)

机构地区：[1]上海中医药大学中药学院,上海201203

出　　处：《上海中医药杂志》2020年第11期78-84,共7页Shanghai Journal of Traditional Chinese Medicine

基　　金：上海市教委科研预算内项目(2013JW12,2020LK018)。

摘　　要：目的采用大鼠佐剂型关节炎模型,比较载雷公藤甲素甘油醇质体新型经皮给药系统与雷公藤甲素凝胶贴膏剂对大鼠佐剂型关节炎的作用。方法采用注入法制备甘油醇质体,测定其粒径分布与包封率;采用聚丙烯酸钠交联法制备雷公藤甲素凝胶贴膏剂;建立大鼠佐剂型关节炎模型,比较雷公藤甲素甘油醇质体与凝胶贴膏对佐剂型关节炎改善作用的优劣。结果所制备的雷公藤甲素甘油醇质体平均粒径为(153.10±2.69)nm,电动电位为(-45.73±0.60)mV,包封率为(75.97±0.94)%。透射电镜下观察磷脂囊泡近圆形,表面光滑,分布均匀。局部用药后,与阳性药组(雷公藤多苷口服给药)相比,醇质体组对大鼠的体质量影响较小;醇质体组大鼠的关节炎指数、足跖容积,以及血浆中TNF-α、IL-6与IL-1β的水平均显著低于模型组(P<0.01);与凝胶贴膏组相比,醇质体组经皮给药对TNF-α、IL-6表达的抑制作用更强(P<0.05)。结论采用甘油醇质体作为经皮给药载体,可有效改善药物的经皮递送,从而增强雷公藤甲素改善大鼠佐剂型关节炎症状的作用。Objective To compare the effects of triptolide-loaded glycerol-mediated ethosomes(TP-ES)and gel plaster on the rat adjuvant arthritis model. Methods TP-ES was prepared by injection method,and its particle size distribution and encapsulation efficiency were measured.The cross-linked sodium polyacrylate was used as the carrier for preparing the TP-loaded gel plaster. Rat adjuvant arthritis model was established,and gel plaster was used as a control to evaluate the therapeutic effect of TP-ES on adjuvant arthritis. Results The average particle size of the prepared TP-ES was 153.10±2.69 nm,the zeta potential was-45.73±0.60 mV,and the encapsulation efficiency was 75.97±0.94%. Under the transmission electron microscope,the phospholipid vesicles are nearly round with smooth surfaces and even distribution. After topical administration,compared with the positive group(tripterygium glycoside with intragastric administration),the TP-ES group had less effect on the body weight of the rats,indicating that the toxic and side effects were reduced. The rats arthritis index and toe volume, as well as the levels of TNF-α, IL-6 and IL-1β in the blood of TP-ES group, were significantly lower than those of the model group. Compared with the gel plaster group, the TP-ES group showed stronger inhibition of the expression of TNF-α and IL-6(P<0.05). Conclusion By using glycerol-mediated ethosomes as the transdermal drug delivery carrier can effectively improve the transdermal delivery of drugs, thereby enhancing the therapeutic effect.

关 键 词：类风湿关节炎 雷公藤甲素 脂质体 甘油醇质体 凝胶贴膏 经皮给药系统 

分 类 号：R285.5[医药卫生—中药学]