title: Penetration of Ufenamate into Intact, Stripped, or Delipidized Skin Using Different Vehicles.
abstract: The purpose of this study was to clarify the effect of skin condition on skin penetration of the very high lipophilic drug, ufenamate (UF). UF was applied to stripped or delipidized skin using liquid paraffin (LP) or purified water containing polysorbate 80 at a dose of 2 µL/cm(2). We found that UF penetration into intact and stripped skin using a water vehicle was respectively 5 and 10 times higher than that using LP. UF is freely soluble in oil and insoluble in water; thus, activity in water is higher than that in LP. Therefore, it is useful to use a water-based vehicle for both intact sites and those with defective stratum corneum (SC). Conversely, we found that delipidization of SC decreased the penetration of UF significantly with both LP and water, and the amount measured in the epidermis was 1 µg/cm(2) with both vehicles. This indicates that UF is not suitable for so-called "dry skin." This study revealed clinically relevant differences in the penetration of UF into intact, stripped, or delipidized skin conditions.
authors.affiliation: Department of Pharmaceutics and Biopharmaceutics, Showa Pharmaceutical University.
authors.forename: Hayato
authors.initials: H
authors.lastname: Iino
authors.forename: Makiko
authors.initials: M
authors.lastname: Fujii
authors.forename: Manami
authors.initials: M
authors.lastname: Fujino
authors.forename: Naoya
authors.initials: N
authors.lastname: Koizumi
authors.forename: Yoshiteru
authors.initials: Y
authors.lastname: Watanabe
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D005439:Flufenamic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry; D008899:Mineral Oil / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D012867:Skin / Q000737:chemistry / Q000378:metabolism*; D012869:Skin Absorption; D013501:Surface-Active Agents / Q000737:chemistry; D013552:Swine; D013556:Swine, Miniature; D014867:Water / Q000737:chemistry
chemical_list: D000893:Anti-Inflammatory Agents; D008055:Lipids; D011136:Polysorbates; D013501:Surface-Active Agents; D014867:Water; D005439:Flufenamic Acid; D008899:Mineral Oil; C047051:ufenamate