PDF(Pubmed)
Abstract：
This research aimed to develop miconazole-based microemulsions using oleic acid as a natural lipophilic phase and a stabilizer mixture comprising Tween 20 and PEG 400 to solubilize miconazole as an antifungal agent known for its activity in oral candidiasis and to improve its bioavailability. The formulation and preparation process was combined with a mathematical approach using a 23-full factorial plan. Fluid and gel-like microemulsions were obtained and analyzed considering pH, conductivity, and refractive index, followed by extensive analyses focused on droplet size, zeta potential, rheological behavior, and goniometry. In vitro release tests were performed to assess their biopharmaceutical characteristics. Independent variables coded X1-Oleic acid (%, w/w), X2-Tween 20 (%, w/w), and X3-PEG 400 (%, w/w) were analyzed in relationship with three main outputs like mean droplet size, work of adhesion, and diffusion coefficient by combining statistical tools with response surface methodology. The microemulsion containing miconazole base-2%, oleic acid-5%, Tween 20-40%, PEG 400-20%, and water-33% exhibited a mean droplet size of 119.6 nm, a work of adhesion of 71.98 mN/m, a diffusion coefficient of 2.11·10-5 cm2/s, and together with remarked attributes of two gel-like systems formulated with higher oil concentrations, modeled the final optimization step of microemulsions as potential systems for buccal delivery.
摘要：
这项研究旨在开发基于咪康唑的微乳剂，该乳剂使用油酸作为天然亲脂性相，并使用包含Tween20和PEG400的稳定剂混合物来溶解咪康唑作为抗真菌剂，并提高其生物利用度。配方和制备过程与使用23全因子计划的数学方法相结合。流体和凝胶状微乳液获得和分析考虑pH,电导率，和折射率，其次是对液滴大小的广泛分析，zeta电位,流变行为，和测角法.进行体外释放测试以评估其生物制药特性。独立变量编码X1-油酸(%，w/w),X2-吐温20(%,w/w),和X3-PEG400(%，w/w)与三个主要输出的关系进行了分析，如平均液滴尺寸，粘合功，通过将统计工具与响应面方法相结合，得到扩散系数。含咪康唑碱-2%的微乳液，油酸-5%，吐温20-40%，PEG400-20%，33%的水表现出119.6nm的平均液滴尺寸，71.98mN/m的附着力功，扩散系数为2.11·10-5cm2/s，以及用较高油浓度配制的两种凝胶样系统的显著属性，将微乳液的最终优化步骤建模为口腔输送的潜在系统。
