Chen Huabing, Chang Xueling, Du Danrong, Li Jin, Xu Huibi, Yang Xiangliang
College of Life Science and Technology, Huazhong University of Science and Technology, 430074 Wuhan, China.
Int J Pharm. 2006 Jun 6;315(1-2):52-8. doi: 10.1016/j.ijpharm.2006.02.015. Epub 2006 Apr 5.
The purpose of this study was to construct microemulsion-base hydrogel formulation for topical delivery of ibuprofen. Ethyl oleate (EO) was screened as the oil phase of microemulsions, due to a good solubilizing capacity of the microemulison systems and excellent skin permeation rate of ibuprofen. The pseudo-ternary phase diagrams for microemulsion regions were constructed using ethyl oleate as the oil, Tween 80 as the surfactant, propylene glycol as the cosurfactant. Various microemulsion formulations were prepared and the abilities of various microemulsions to deliver ibuprofen through the skin were evaluated in vitro using Franz diffusion cells fitted with porcine skins. The in vitro permeation data showed that microemulsions increased the permeation rate of ibuprofen 5.72-30.0 times over the saturated solution. The optimum formulation consisted of 3% ibuprofen, 6% EO, 30% Tween 80/PG (2:1) and water, showed a high permeation rate of 38.06 microg cm(-2) h(-1). Xanthan gum as a gel matrix was used to construct the microemulsion-based hydrogel for improving the viscosity of microemulsion for topical administration. The studied microemulsion-based hydrogel showed a good stability. These results indicate that the studied microemulsion-based hydrogel may be a promising vehicle for topical delivery of ibuprofen.
本研究的目的是构建用于布洛芬局部给药的微乳基水凝胶制剂。由于微乳体系具有良好的增溶能力以及布洛芬优异的皮肤渗透速率,油酸乙酯(EO)被筛选为微乳的油相。以油酸乙酯为油相、吐温80为表面活性剂、丙二醇为助表面活性剂构建了微乳区域的拟三元相图。制备了各种微乳制剂,并使用配备猪皮的Franz扩散池体外评估了各种微乳将布洛芬透过皮肤递送的能力。体外渗透数据表明,微乳使布洛芬的渗透速率比饱和溶液提高了5.72 - 30.0倍。最佳制剂由3%布洛芬、6% EO、30%吐温80/丙二醇(2:1)和水组成,显示出38.06 μg cm⁻² h⁻¹的高渗透速率。黄原胶作为凝胶基质用于构建微乳基水凝胶,以提高微乳用于局部给药时的粘度。所研究的微乳基水凝胶显示出良好的稳定性。这些结果表明,所研究的微乳基水凝胶可能是一种有前景的布洛芬局部给药载体。