背景:甲咪唑,口服抗甲状腺药物,最近因其局部应用于治疗黄褐斑时的皮肤增亮效果而受到关注。本研究旨在开发,优化,并表征了甲咪唑微乳作为一种新型的,局部黄褐斑治疗的安全方法。
方法:我们通过混合适量的表面活性剂(Tween80和Span20)制备了含有3%甲咪唑的微乳液制剂,丙二醇助表面活性剂,和油相(油酸-transcutolp,比例为1:10)。然后我们评估液滴大小,稳定性,粘度,和使用大鼠皮肤模型的皮肤渗透。
结果:微乳液的液滴尺寸范围为7.06至28.13nm,粘度在120和254厘泊之间。我们的分析确定了液滴大小,粘度,和膜释放作为重要的独立变量。我们确定了最佳配方通过大鼠皮肤的渗透性参数,包括稳态渗透率(Jss),渗透系数(p),滞后时间(Tlag),和表观扩散系数(Dapp)。
结论:我们发现微乳液的特性,物理化学性质,和体外释放取决于表面活性剂与辅助表面活性剂的比例,含水量,和含油量。我们开发了具有高表面活性剂与辅助表面活性剂比率和低水和油百分比的最佳配方。该配方显示出最终产品的商业化和制造潜力。
BACKGROUND: Methimazole, an oral antithyroid drug, has recently gained attention for its skin-brightening effects when applied topically to treat melasma. This study aims to develop, optimize, and characterize a methimazole
microemulsion as a novel, safe approach for local melasma treatment.
METHODS: We prepared
microemulsion formulations containing 3% methimazole by combining appropriate amounts of surfactants (Tween 80 and Span 20), propylene glycol cosurfactant, and an oil phase (oleic acid-transcutol p at a 1:10 ratio). We then assessed droplet size, stability, viscosity, and skin permeation using rat skin models.
RESULTS: The microemulsions\' droplet sizes ranged from 7.06 to 28.13 nm, with viscosities between 120 and 254 centipoises. Our analysis identified droplet size, viscosity, and membrane release as significant independent variables. We determined the permeability parameters of the optimal formulation through rat skin, including steady-state permeability rate (Jss), permeability coefficient (p), lag time (Tlag), and apparent diffusion coefficient (Dapp).
CONCLUSIONS: We found that the microemulsions\' characteristics, physicochemical properties, and in vitro release depended on the surfactant-to-cosurfactant ratio, water content, and oil content. We developed an optimal formulation with a high surfactant-to-cosurfactant ratio and low water and oil percentages. This formulation shows potential for commercialization and manufacturing of final products.