Nogueira Marianne A P C, Cardoso Camila O, Albuquerque Lucas F F, Cunha-Filho Marcilio, Gratieri Tais, Gelfuso Guilherme M
Laboratory of Food, Drug and Cosmetics (LTMAC), School of Health Sciences, University of Brasília, Campus Universitário Darcy Ribeiro, S/N. 70910-900, Asa Norte, Brasília, DF, Brazil.
AAPS PharmSciTech. 2025 May 30;26(5):148. doi: 10.1208/s12249-025-03146-z.
Given the anti-inflammatory properties of Resveratrol, this paper proposes developing a grape seed oil-in-water microemulsion (ME) for topical administration to treat inflammatory skin pathological conditions. Thermal analyses confirmed compatibility between Resveratrol, grape seed oil, Tween 80, and Span 80 used in the formulations. Two compositions (ME1 and ME2) were selected from a pseudo-ternary diagram prepared by components titration. ME1 (50% water, 35% surfactant, 15% oil) and ME2 (60% water, 30% surfactant, 10% oil) showed mean droplet sizes of 23.1 ± 0.7 nm and 24.9 ± 1.7 nm (PdI = 0.34 and 0.47), zeta potential between -11.7 ± 0.5 and -13.6 ± 0.9 mV, and pH values of 6.2 ± 0.5 and 7.1 ± 1.1, respectively. Rheological analyses revealed Newtonian behavior and low viscosity, with physical stability for 60 days at room temperature. In vitro drug permeation studies using porcine skin demonstrated that ME increased Resveratrol penetration into deeper skin layers by fourfold (p < 0.001) compared to the control solution (ME1: 2.9 ± 0.1 μg/cm, ME2: 2.4 ± 0.1 μg/cm), while reducing retention in the stratum corneum. HET-CAM experiments indicated safety for topical application. In conclusion, the ME was a promising alternative for future clinical investigations to treat inflammatory skin conditions.
鉴于白藜芦醇的抗炎特性，本文提出开发一种用于局部给药的水包葡萄籽油微乳剂（ME），以治疗炎症性皮肤病理状况。热分析证实了配方中使用的白藜芦醇、葡萄籽油、吐温80和司盘80之间的相容性。从通过组分滴定制备的拟三元相图中选择了两种组合物（ME1和ME2）。ME1（50%水、35%表面活性剂、15%油）和ME2（60%水、30%表面活性剂、10%油）的平均液滴尺寸分别为23.1±0.7nm和24.9±1.7nm（多分散指数PdI=0.34和0.47），ζ电位在-11.7±0.5至-13.6±0.9mV之间，pH值分别为6.2±0.5和7.1±1.1。流变学分析显示出牛顿流体行为和低粘度，在室温下具有60天的物理稳定性。使用猪皮进行的体外药物渗透研究表明，与对照溶液相比，ME使白藜芦醇渗透到更深皮肤层的能力提高了四倍（p<0.001）（ME1：2.9±0.1μg/cm，ME2：2.4±0.1μg/cm），同时减少了在角质层中的滞留。鸡胚绒毛尿囊膜（HET-CAM）实验表明局部应用是安全的。总之，ME是未来治疗炎症性皮肤病临床研究的一个有前景的替代方案。
