title: Effect of N-methyl-2-pyrrolidone on skin permeation of estradiol.
abstract: N-Methyl-2-pyrrolidone (NMP) increased the skin permeation of estradiol (E2) in Yucatan micropig epidermis using a modified Franz-type diffusion cell. The addition of NMP significantly increased the fluxes of E2 from water and soybean oil. The flux and skin concentration of E2 were higher from soybean oil than from water and increased with increasing NMP concentrations in soybean oil. Correlation was observed with E2 flux and skin concentration (R(2) = 0.804) NMP enhanced E2 skin permeation because NMP made E2 skin concentration higher. Thus, NMP (10%) was added to the oily gel made by isocetyl isostearate and hydrogenated phospholipid. E2 permeation from the gel without NMP was the same as that from soybean oil suspension. The flux of E2 from the gel with NMP was 0.6 microg/h per cm(2) and might be sufficient for estrogen replacement therapy.
authors.affiliation: Department of Pharmaceutics and Biopharmaceutics, Showa Pharmaceutical University, Tokyo, Japan.
authors.forename: Atsuko
authors.initials: A
authors.lastname: Koizumi
authors.forename: Makiko
authors.initials: M
authors.lastname: Fujii
authors.forename: Masuo
authors.initials: M
authors.lastname: Kondoh
authors.forename: Yoshiteru
authors.initials: Y
authors.lastname: Watanabe
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D004958:Estradiol / Q000737:chemistry / Q000493:pharmacokinetics*; D066298:In Vitro Techniques; D011760:Pyrrolidinones / Q000737:chemistry / Q000493:pharmacokinetics*; D012869:Skin Absorption / Q000187:drug effects / Q000502:physiology*; D013552:Swine; D013556:Swine, Miniature
chemical_list: D011760:Pyrrolidinones; D004958:Estradiol; C038678:N-methylpyrrolidone