Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, Georgia 30341, USA.
J Pharm Sci. 2013 Aug;102(8):2622-31. doi: 10.1002/jps.23627. Epub 2013 May 31.
The aim of this study was to develop a microemulsion formulation of adapalene for transfollicular delivery. A pseudoternary phase diagram was developed for microemulsion consisting of oleic acid as oil phase, tween 20 as surfactant, Transcutol® as cosurfactant, and deionized water. Differential tape stripping and confocal laser scanning microscopy were performed to determine the penetration of microemulsion through hair follicles. Transmission electron microscopy, dynamic light scattering, polarizing light microscopy, and differential scanning calorimetry were performed to characterize the microstructures of microemulsion. The pH and viscosity of the microemulsions were also determined. Permeation studies were carried out in vitro on porcine ear skin over a period of 24 h using Franz diffusion cells. The drug penetration in the hair follicles increased from 0.109 ± 0.03 to 0.292 ± 0.094 μg, as the microstructure of microemulsion shifted from oil-in-water to bi-continuous, with increase in water content of microemulsion. Confocal laser scanning microscopy images suggested that hair follicles provided the path for transfollicular permeation of adapalene microemulsion. These results suggest that microemulsion penetrated through hair follicles and are promising for transfollicular drug delivery.
本研究旨在开发一种用于经毛囊传递的阿达帕林微乳制剂。采用伪三元相图法，以油酸为油相、吐温 20 为表面活性剂、Transcutol®为助表面活性剂、去离子水为水相，制备微乳。采用微分条带剥离和共聚焦激光扫描显微镜（CLSM）测定微乳经毛囊的渗透情况。采用透射电子显微镜（TEM）、动态光散射（DLS）、偏光显微镜和差示扫描量热法（DSC）对微乳的微观结构进行表征。还测定了微乳的 pH 值和黏度。采用Franz 扩散池，在体外于猪耳皮肤进行 24 h 的渗透研究。随着微乳的微观结构由油包水型向双连续型转变，水含量增加，药物在毛囊中的渗透量从 0.109 ± 0.03 μg 增加至 0.292 ± 0.094 μg。CLSM 图像表明，毛囊为阿达帕林微乳经皮渗透提供了途径。这些结果表明，微乳可以透过毛囊，有望用于经毛囊递药。
