Skin Permeation Characteristics of Estradiol Patches and Their Comparative Efficacy Test in Ovariectomized Rabbits

에스트라디올 패취의 피부투과 특성 및 난소제거 토끼에서의 비교 효력시험

Transdermal patch formulations of estradiol to treat post-menopausal symptoms and prevent osteoporosis in women were developed and evaluated for the permeation characteristics through the excised hairless mouse abdorminal skin and the uterotropic effect on the ovariectomized rabbits. The design of patch formulations was optimized by varying several formulation parameters, such as type of enhancers, amount of enhancers, amount of drug loading and coating thickness. Compared to a commercially available transdermal product, several patch formulations showed the similar skin permeation profiles (following zero-order kinetics), but their skin permeation rates were lasted for the longer period (a week). In one-week uterotropic efficacy test in the ovariectimized rabbits, the selected patch formulations showed the positive effect in atrophy of the urogenital epithelium. The mean values of uterus weight in rabbits after application of patches containing estradiol were much higher than those in control group (containing no drug).