title: Efficient delivery and distribution in skin of chlorogenic acid and resveratrol induced by microemulsion using sucrose laurate.
abstract: To achieve efficient skin delivery of polyphenols, we prepared a novel oil-in-water (o/w)-type microemulsion (MESL) using sucrose laurate as a surfactant and ethanol, isopropyl myristate and water as other components. We examined its usefulness by in vitro studies on skin delivery of chlorogenic acid and resveratrol as hydrophilic and hydrophobic polyphenols using Yucatan micropig skin, and also examined the difference in the distribution of these polyphenols in skin. MESL significantly improved skin incorporation of these polyphenols at all time points examined (6, 20, 40 h) in the epidermis and at 20 and 40 h in the dermis, compared with the microemulsion using Tween 80 as a surfactant component (MEK), although the solubilization capacity of MESL was lower than that of MEK. Using MESL, the incorporation amount in the dermis of each polyphenol increased with time, while the amount in the epidermis was almost constant during the time examined. Incorporation efficiencies into skin of chlorogenic acid and resveratrol induced by MESL at 40 h after application were about 6-fold and 19-fold higher in the epidermis and 3.5-fold and 15-fold higher in the dermis, respectively, than those by MEK. The increase was more prominent for resveratrol. Hydrophilic chlorogenic acid was distributed slightly more in the epidermis, while hydrophobic and smaller-molecular-weight resveratrol was mainly distributed in the dermis. These findings suggest that MESL could be a promising vehicle for the efficient skin delivery of chlorogenic acid and resveratrol, especially for resveratrol to the dermis.
authors.affiliation: Department of Pharmaceutical Technology, Kobe Pharmaceutical University.
authors.forename: Reiko
authors.initials: R
authors.lastname: Yutani
authors.forename: Taketomo
authors.initials: T
authors.lastname: Kikuchi
authors.forename: Reiko
authors.initials: R
authors.lastname: Teraoka
authors.forename: Shuji
authors.initials: S
authors.lastname: Kitagawa
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002726:Chlorogenic Acid / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004655:Emulsions / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000431:Ethanol / Q000737:chemistry; D009226:Myristates / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D000077185:Resveratrol; D012869:Skin Absorption; D013267:Stilbenes / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013395:Sucrose / Q000031:analogs & derivatives* / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry; D013552:Swine; D014867:Water / Q000737:chemistry
chemical_list: D004655:Emulsions; D009226:Myristates; D011136:Polysorbates; D013267:Stilbenes; D013501:Surface-Active Agents; D014867:Water; C018152:sucrose monolaurate; C008205:isopropyl myristate; D002726:Chlorogenic Acid; D000431:Ethanol; D013395:Sucrose; D000077185:Resveratrol