University Camerino, School of Pharmacy, Camerino, Italy.
Drug Dev Ind Pharm. 2012 Sep;38(9):1128-33. doi: 10.3109/03639045.2011.641564. Epub 2011 Dec 22.
A microemulsion for the cutaneous release of quercetin was prepared. An aqueous phase, containing 40% Transcutol® P as solubilizing agent and permeation enhancer, was emulsified with Labrafil® as oil phase and Labrasol®/Capryol™ 90 as Solvent/Co-solvent. Quercetin was dissolved in the microemulsion at the concentration of 1%. Ternary phase diagrams were generated to determine the optimal concentration of each excipient composing the microemulsion. The physicochemical properties of the microemulsion, such as pH, viscosity, refractive index, and particle size distribution were determined. The microemulsion was stable for 12 months at the storing conditions of 25.0 ± 1.0°C. The in vitro quercetin permeability into and through the abdominal hairless pig skin was determined by vertical Franz's cells. Quercetin showed hardly any permeability through the skin when dissolved in water- and Transcutol® P-free media, whereas a remarkable increase in cutaneous permeability was observed when quercetin was formulated in the microemulsion or when simply dissolved in Transcutol® P. These two last formulations are those showing the lower skin retention.
已制备用于透皮释放槲皮素的微乳。水相含有 40%的 Transcutol® P 作为增溶和渗透促进剂，与 Labrafil® 油相和 Labrasol®/Capryol™ 90 溶剂/共溶剂乳化。将槲皮素溶解在微乳中，浓度为 1%。生成三元相图以确定构成微乳的每种赋形剂的最佳浓度。测定了微乳的物理化学性质，如 pH 值、粘度、折射率和粒径分布。微乳在 25.0±1.0°C 的储存条件下稳定 12 个月。通过垂直 Franz 细胞测定了微乳中槲皮素经腹部无毛猪皮的体外透皮渗透。当溶解在不含水和 Transcutol® P 的介质中时，槲皮素几乎没有透皮渗透，而当槲皮素在微乳中形成配方或简单地溶解在 Transcutol® P 中时，皮肤渗透性显著增加。后两种配方的皮肤保留率较低。
