a Department of Pharmaceutics , The Applied Research Center of Medicinal Plants "ARCMP", National Organization for Drug Control and Research "NODCAR" , El-Haram, Giza , Egypt.
b Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Cairo University , Kasr El-Aini St, Cairo , Egypt , and.
J Liposome Res. 2018 Jun;28(2):126-136. doi: 10.1080/08982104.2017.1281951. Epub 2017 Feb 6.
The aim of this study was to investigate microemulsion (ME) based topical delivery system for fenoprofen calcium (FPCa) to eliminate its oral gastrointestinal adverse effects. ME was prepared by the water titration method using oleic acid as oil phase, tween 80 as a surfactant and propylene glycol as a cosurfactant. Oleic acid was selected as oil phase due to its good solubilizing capacity. ME existence region was determined using pseudo-ternary phase diagrams for preparing different formulations. Six different formulations were selected with various values of oil (25-68%), water (2-3%), and the mixture of surfactant and cosurfactant (1:1) (24-67%). The selected ME formulae were characterized for optical birefringence, transmission electron microscopy (TEM), pH, % transmittance, electronic conductivity, drug content, droplet size, rheological properties and stability evaluation. In vitro release study of FPCa from ME s through the synthetic membrane and hairless rat skin were evaluated. The optimized formula ME5 consisting of 5% w/w FPCa, 60% w/w oleic acid as oil phase, 3% w/w aqueous phase, and 32% w/w of surfactant phase containing Tween 80 and propylene glycol (1: 1) showed the highest transdermal flux and highest skin permeation rate. Finally, the % inhibition of carrageenan-induced rat paw edema of the optimized formula ME5 was highly significant (p < 0.001) as compared to plain gel of FPCa. In conclusion, ME is a promising technique for topical delivery of FPCa.
本研究旨在探讨微乳（ME）作为芬诺洛芬钙（FPCa）的局部给药系统，以消除其口服胃肠道不良反应。采用水滴定法制备 ME，以油酸为油相，吐温 80 为表面活性剂，丙二醇为助表面活性剂。选择油酸作为油相是因为其具有良好的增溶能力。使用伪三元相图确定 ME 的存在区域，以制备不同的配方。选择了六种不同的配方，油相（25-68%）、水相（2-3%）和表面活性剂与助表面活性剂（1:1）的混合物（24-67%）的比例各不相同。对所选 ME 配方进行了光学双折射、透射电子显微镜（TEM）、pH 值、透光率%、电子电导率、药物含量、粒径、流变学特性和稳定性评价。通过合成膜和无毛大鼠皮肤评估 FPCa 从 ME 中的体外释放。由 5%w/w FPCa、60%w/w 油酸作为油相、3%w/w 水相和 32%w/w 表面活性剂相（包含吐温 80 和丙二醇（1:1））组成的优化配方 ME5 显示出最高的透皮通量和最高的皮肤渗透速率。最后，与 FPCa 的普通凝胶相比，优化配方 ME5 对角叉菜胶诱导的大鼠足肿胀的抑制率具有高度显著性（p<0.001）。总之，ME 是 FPCa 局部给药的一种有前途的技术。
