Long-Tern Skin Permeation Kinetics of Estradiol: (II) Kinetics of Skin Uptake, Binding, and Metabolism

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Abstract
The in vitro skin permeation system developed in this laboratory was utilized to investigate the kinetics of uptake, binding, and metabolism of estradiol, the female hormone, by the hairless mouse skin. The kinetics of uptake of estradiol and its subsequent metabolism to estrone by the skin were examined by exposing one side of a freshly excised skin to an estradiol solution, while the other side of the skin was protected with an impermeable aluminum foil. The results concluded that the stratum corneum plays a rate-limiting role in the uptake and binding of estradiol and its metabolism to estrone by the skin. The mechanisms of the uptake and binding of estradiol to whole skin tissue (with stratum corneum) showed a sex dependence, with the rate higher in the female than in the male mouse. On the other hand, no sex-dependent difference was observed in the mechanism and rate of metabolism to estrone. After stripping off the rate-limiting stratum corneum, the mechanisms of the uptake, binding and metabolism of estradiol all became sex dependent with identical rates observed between male and female mice in the initial 14 hrs of the experiment; Between 14 to 21 hrs, the rates increased substantially with the female skin, but not with the male skin. The increase in the rate of uptake of estradiol by the female skin was related primarily to the increased rate of metabolism of estradiol to estrone.

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