Sharif Makhmalzadeh Behzad, Torabi Shiva, Azarpanah Armita
School of Pharmacy , Ahvaz Jundishapur University of Medical Sciences , Ahvaz , Iran .
Iran J Pharm Res. 2012 Winter;11(1):47-58.
The topical delivery of non-steroidal anti-inflammatory drugs (NSAIDS) such as Ibuprofen has been explored as a potential method of avoiding the first pass effects and the gastric irritation, which may occur when used orally. Ibuprofen is formulated into many topical preparations to reduce the adverse effects and simultaneously avoid the hepatic first-pass metabolism as well. However, it is difficult to obtain an effective concentration through topical delivery of Ibuprofen due to its low skin permeability. The aim of this study was to develop two types of nanoemulsions formulations and focused on the screening of Ibuprofen-loaded nanoemulsions and evaluating the influence of these types of nanoemulsions on the skin permeability of the drug. In both nanoemulsion formulations, oil was similar, but the surfactant and co-surfactant were different. The effect of independent variables on skin permeability parameters was evaluated using full factorial design. Results demonstrate that novel formulations were more effective as skin enhancer than traditional formulation. In case of the novel formulation, any increase in percentage of surfactant and co-surfactant had increasing effect on flux (Jss). On the other hand, the proportion of surfactant/co-surfactant (S/C) demonstrated reverse correlation with Jss. While, in traditional formulations, direct correlation was found between both variables, and Jss. Comparison between two types of nanoemulsion formulations revealed that, novel formulations were more effective as topical Ibuprofen carrier in contrast to traditional type due to lower amounts of surfactant and co-surfactant and less irritating effect.
布洛芬等非甾体抗炎药的局部给药已被探索为一种避免首过效应和口服时可能出现的胃部刺激的潜在方法。布洛芬被制成多种局部制剂,以减少不良反应并同时避免肝脏首过代谢。然而,由于布洛芬的皮肤渗透性低,通过局部给药难以获得有效浓度。本研究的目的是开发两种类型的纳米乳剂配方,并专注于筛选负载布洛芬的纳米乳剂以及评估这些类型的纳米乳剂对药物皮肤渗透性的影响。在两种纳米乳剂配方中,油相相似,但表面活性剂和助表面活性剂不同。使用全因子设计评估自变量对皮肤渗透性参数的影响。结果表明,新型配方作为皮肤增强剂比传统配方更有效。对于新型配方,表面活性剂和助表面活性剂百分比的任何增加都会对通量(Jss)产生增加的影响。另一方面,表面活性剂/助表面活性剂(S/C)的比例与Jss呈负相关。而在传统配方中,这两个变量与Jss之间存在正相关。两种类型的纳米乳剂配方之间的比较表明,与传统类型相比,新型配方作为局部布洛芬载体更有效,因为表面活性剂和助表面活性剂的用量较低且刺激性较小。