摘要
目的:制备并表征局部用咪喹莫特泡囊凝胶剂,考察药物皮内滞留效应。方法:制备并表征咪喹莫特泡囊凝胶剂,离体鼠皮透皮实验考察药物皮内滞留量和透过量,切片观察药物皮内分布。结果:泡囊的平均粒径197.2 nm,Zeta电位-42.97 m V,包封率27.44%;泡囊凝胶剂体外释放t1/2与泡囊相似,但为凝胶剂的4.94倍和市售乳膏的3.83倍,12 h透过药量均比凝胶剂和市售乳膏小一半,单位面积皮内药物滞留量约为它们的2倍,切片显示药库效应显著。结论:泡囊凝胶剂具缓释作用和药库效应,可增加皮内滞留,减少角质层拦截和透过皮肤的药量,将有利于皮肤病的治疗,并可降低局部刺激性和全身毒性的风险。
Objective： To prepare and characterize imiquimod niosomal gel for topical application, and in- vestigate the intracutaneous retention effect. Methods： Imiquimod niomosal gel was prepared and characterized. The amount of imiquimod permeated and within the skin was investigated by transdermal studies on the ex-vivo rat skin. Intradermal drug distribution in the skin section was observed with confocal laser scanning microscopy. Results： The average particle size, zeta-potential and entrapment efficiency of the imiquimod niosomes were 197.2 nm, - 42.97 mV and 27.44% , respectively. The tl/2 value of drug release from the niosomal gel in vitro was similar to that from the niosomes （P 〉 0.5） , but was 4.94 and 3.83 folds as that from the gel and commercial cream, respectively （P 〈 0.01 ）. The amount of drug permeated from niosomal gel into the skin in 12 h was 50% less than that from the gel and commercial cream, while the amount of drug retention in the skin was about 2 times more than that of the gel and commercial cream. The significant reservoir effect was also demonstrated by the section observation. Conclusion： Imiquimod niosomal gel shows a sustained release property and a reservoir effect for the drug, making high retention of drug in the skin, and reducing the drug in stratum interception and skin transmission. Therefore, it would be helpful for therapy of dermatosis, and reduce the topical irritation and the systemic toxicity.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2015年第1期97-101,共5页
Chinese Journal of New Drugs
基金
国家自然科学基金(81273462)
关键词
泡囊凝胶剂
咪喹莫特
体外释放
皮内滞留
药库效应
niosomal gel
imiquimod
drug release in vitro
intraeutaneous accumulation
reservoir effect
