title: Skin accumulation and penetration of a hydrophilic compound by a novel gemini surfactant, sodium dilauramidoglutamide lysine.
abstract: We investigated a novel peptide-based gemini amphiphilic compound, sodium dilauramidoglutamide lysine (DLGL), as a chemical enhancer for the skin penetration of l-ascorbic acid 2-glucoside (AAG). A three-dimensional cultured human skin product, TESTSKIN™ LSE-high (LSE-high), was used as a skin model. The penetration flux of AAG with DLGL and that obtained with sodium lauramidoglutamide (LG) as a conventional surfactant across LSE-high were increased by 12.56 and 69.29 times compared to the control, respectively. The ratio of AAG amount with DLGL in the skin (21.78% total dose) was significantly increased (p<0.05) compared to the control (7.23%) and to the AAG amount with LG (8.13%). The AAG amounts in receptor were 1.06% (control), 3.19% (+DLGL) and 21.00% (+LG). Thus, DLGL preserved AAG in skin, resulting in enhanced AAG penetration flux. However, LG might create the pathways through the skin. We conclude that DLGL is a gemini surfactant that accumulates a hydrophilic compound in skin and enhances the penetration flux. DLGL may therefore be a novel addition agent for skin local therapy.
authors.affiliation: Kyushu Institute of Technology, Department of Biosciences and Bioinformatics, 680-4 Kawazu, Iizuka, Fukuoka 820-8502, Japan. hikima@bio.kyutech.ac.jp
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Hikima
authors.forename: Yoshinaga
authors.initials: Y
authors.lastname: Tamura
authors.forename: Yukio
authors.initials: Y
authors.lastname: Yamawaki
authors.forename: Masashi
authors.initials: M
authors.lastname: Yamamoto
authors.forename: Kakuji
authors.initials: K
authors.lastname: Tojo
mesh_terms: D001205:Ascorbic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D005079:Excipients / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D066298:In Vitro Techniques; D008954:Models, Biological; D015394:Molecular Structure; D009842:Oligopeptides / Q000737:chemistry* / Q000494:pharmacology; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption / Q000187:drug effects*; D013501:Surface-Active Agents / Q000737:chemistry* / Q000494:pharmacology; D013997:Time Factors; D014018:Tissue Distribution
chemical_list: D005079:Excipients; D009842:Oligopeptides; D013501:Surface-Active Agents; C065378:ascorbic acid 2-O-glucoside; D001205:Ascorbic Acid