Luna-Canales Irene Carolina, Delgado-Buenrostro Norma Laura, Chirino Yolanda I, Nava-Arzaluz Guadalupe, Piñón-Segundo Elizabeth, Martínez-Cruz Graciela, Ganem-Rondero Adriana
Laboratorio de Investigación y Posgrado en Tecnología Farmacéutica (L-322, Campo 1), Universidad Nacional Autónoma de México, Cuautitlán Izcalli, Mexico.
Laboratorio 10, Unidad de Biomedicina, Universidad Nacional Autónoma de México, Tlalnepantla, Mexico.
Drug Dev Ind Pharm. 2023 Jan;49(1):42-51. doi: 10.1080/03639045.2023.2182121. Epub 2023 Mar 3.
Formulation of curcumin in a microemulsion with a high loading capacity and that favors its penetration into the skin.
Take advantage of the properties of microemulsions to promote the penetration of curcumin into the skin, with the aim of enhancing its therapeutic effects.
Curcumin was formulated in microemulsions based on oleic acid (oil phase), Tween® 80 (surfactant), and Transcutol HP (cosurfactant). The microemulsion formation area was mapped by constructing pseudo-ternary diagrams for surfactant:co-surfactant ratios 1:1, 1:2, and 2:1. Microemulsions were characterized through measurements of specific weight, refractive index, conductivity, viscosity, droplet size, and skin permeation studies.
Nine microemulsions were prepared and characterized, showing clear, stable formulations with globule size dependent on the proportion of the components. The microemulsion with the highest loading capacity (60 mg/mL), based on Tween 80, Transcutol HP, oleic acid, and water (40:40:10:10) was able to penetrate the viable epidermis, finding a total amount of curcumin in the receptor medium at 24 h of 10.17 ± 9.7 µg/cm. The distribution of curcumin in the skin, visualized by confocal laser scanning microscopy, showed that the maximum amount was located between 20 and 30 µm.
The inclusion of curcumin in a microemulsion allows its passage into and through the skin. The localization of curcumin, especially in the viable epidermis, would be important for those cases where local conditions are sought to be treated.
制备具有高载药量且有利于姜黄素渗透进入皮肤的微乳剂。
利用微乳剂的特性促进姜黄素渗透进入皮肤，以增强其治疗效果。
基于油酸（油相）、吐温80（表面活性剂）和二甲基亚砜（助表面活性剂）制备姜黄素微乳剂。通过构建表面活性剂与助表面活性剂比例为1:1、1:2和2:1的拟三元相图来确定微乳剂的形成区域。通过测定比重、折射率、电导率、粘度、液滴大小以及进行皮肤渗透研究来对微乳剂进行表征。
制备并表征了9种微乳剂，其制剂澄清、稳定，液滴大小取决于各组分的比例。基于吐温80、二甲基亚砜、油酸和水（40:40:10:10）的载药量最高（60mg/mL）的微乳剂能够穿透活表皮，在24小时时受体介质中姜黄素的总量为10.17±9.7μg/cm²。通过共聚焦激光扫描显微镜观察到的姜黄素在皮肤中的分布表明，最大量位于20至30μm之间。
将姜黄素包封于微乳剂中可使其进入并穿透皮肤。姜黄素的定位，尤其是在活表皮中的定位，对于寻求局部治疗的情况而言至关重要。
