Pandey Sujata, Baki Gabriella
Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 3000 Arlington Ave, Toledo, OH 43614, USA.
Gels. 2025 Jan 5;11(1):41. doi: 10.3390/gels11010041.
Microemulsions have been commonly used with various permeation enhancers to improve permeability through the skin. The purpose of this study was to compare the release and permeation ability of two commonly used permeation enhancers-diethylene glycol monoethyl ether (DGME) and oleyl alcohol-by the changes in oil composition, the addition of a gelling agent, and water content using ibuprofen as a model drug. Four microemulsions were formulated, selection was based on ternary phase diagrams, and physicochemical properties were evaluated. The release and permeation of the microemulsion formulations were performed in vitro by Franz cell studies on a regenerated cellulose membrane and a Strat-M membrane, respectively, and the amount of ibuprofen permeated and released was analyzed by high-performance liquid chromatography (HPLC). All four microemulsions were compatible with the skin pH, and the average pH ranged from 4.9 to 5.6. The average droplet size of the microemulsions ranged from 119.8 to 153.3 nm. Drug release was significantly the highest from the gel-based microemulsions (59% and 64%, < 0.05). However, there was a fourfold difference in drug permeation from these gels-a significantly higher permeation from the microemulsion-gel containing oleic acid and oleyl alcohol compared to the DGME formulation. These results indicated that the microemulsion-gel with oleyl alcohol as the permeation enhancer could be a preferable formulation approach for the topical administration of ibuprofen. These results highlight the need for optimization of the microemulsion formulation to confirm the permeation-enhancing effects of chosen permeation enhancers despite being a well-known permeation enhancer.
微乳剂已普遍与各种渗透促进剂一起使用，以提高经皮渗透性。本研究的目的是通过改变油相组成、添加胶凝剂和含水量，以布洛芬为模型药物，比较两种常用渗透促进剂——二甘醇单乙醚（DGME）和油醇——的释放和渗透能力。制备了四种微乳剂，根据三元相图进行选择，并对其理化性质进行了评估。通过Franz扩散池分别在再生纤维素膜和Strat-M膜上进行微乳剂配方的体外释放和渗透实验，采用高效液相色谱（HPLC）分析布洛芬的渗透量和释放量。所有四种微乳剂均与皮肤pH值相容，平均pH值范围为4.9至5.6。微乳剂的平均液滴尺寸范围为119.8至153.3nm。基于凝胶的微乳剂的药物释放量显著最高（59%和64%，P<0.05）。然而，这些凝胶的药物渗透存在四倍差异——与DGME配方相比，含有油酸和油醇的微乳剂-凝胶的渗透显著更高。这些结果表明，以油醇作为渗透促进剂的微乳剂-凝胶可能是布洛芬局部给药的优选配方方法。这些结果突出了优化微乳剂配方的必要性，以确认所选渗透促进剂的渗透增强效果，尽管它是一种众所周知的渗透促进剂。
