An ionic liquid-in-water microemulsion as a potential carrier for topical delivery of poorly water soluble drug: Development, ex-vivo and in-vivo evaluation

详细信息    查看全文

• 作者：Shishu Goindi ; ^{shishugoindi@yahoo.co.in" class="auth_mail" title="E-mail the corresponding author} ; Ramanpreet Kaur ; Randeep Kaur
• 关键词：Etodolac ; Ionic liquid ; Microemulsion ; Topical delivery ; Anti-inflammatory ; Anti-arthritic
• 刊名：International Journal of Pharmaceutics
• 出版年：2015
• 出版时间：30 November 2015
• 年：2015
• 卷：495
• 期：2
• 页码：913-923
• 全文大小：1822 K

文摘

In this paper, we report an ionic liquid-in-water (IL/w) microemulsion (ME) formulation which is able to solubilize etodolac (ETO), a poorly water soluble drug for topical delivery using BMIMPF₆ (1-butyl-3-methylimidazolium hexafluorophosphate) as IL, Tween 80 as surfactant and ethanol as co-surfactant. The prepared ME was characterized for physicochemical parameters, subjected to ex-vivo permeation studies as well as in-vivo pharmacodynamic evaluation. The ex-vivo drug permeation studies through rat skin was performed using Franz-diffusion cell and the IL/w based ME showed maximum mean cumulative percent permeation of 99.030 ± 0.921% in comparison to oil-in-water (o/w) ME (61.548 ± 1.875%) and oily solution (48.830 ± 2.488%) of ETO. In-vivo anti-arthritic and anti-inflammatory activities of the prepared formulations were evaluated using different rodent models and the results revealed that ETO loaded IL/w based ME was found to be more effective in controlling inflammation than oily solution, o/w ME and marketed formulation of ETO. Histopathological studies also demonstrated that IL/w based ME caused no anatomical and pathological changes in the skin.