Evaluation of percutaneous absorption of esculetin: effect of chemical enhancers

Planta Med. 2013 Jan;79(2):131-6. doi: 10.1055/s-0032-1328058. Epub 2012 Dec 18.

Abstract

Percutaneous transdermal absorption of esculetin (6,7-dihydroxycoumarin), an oxidative damage inhibitor, was evaluated by means of in vitro permeation studies in which vertical Franz-type diffusion cells and pig ear skin were employed. To determine the absorption of esculetin, we validated a simple, accurate, precise, and rapid HPLC-UV method. Additionally, the effects of several percutaneous enhancers were studied. Pretreatment of porcine skin was performed with ethanol (control vehicle), decenoic acid, oleic acid, R-(+)-limonene, and laurocapram (Azone®) (5% in ethanol, w/w, respectively). Pretreatment of skin with oleic acid or laurocapram led to statistically significant differences in the transdermal flux of esculetin with respect to controls. Of the two enhancers, laurocapram showed the greatest capacity to enhance the flux of esculetin across pig skin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antioxidants / administration & dosage
  • Antioxidants / analysis
  • Antioxidants / pharmacokinetics*
  • Azepines / pharmacology*
  • Calibration
  • Chromatography, High Pressure Liquid / methods
  • Cyclohexenes / pharmacology
  • Decanoic Acids / pharmacology
  • Drug Delivery Systems
  • Drug Stability
  • Ear, External
  • Limonene
  • Oleic Acid / pharmacology*
  • Permeability
  • Reproducibility of Results
  • Sensitivity and Specificity
  • Skin / drug effects
  • Skin / metabolism
  • Skin Absorption / drug effects*
  • Swine
  • Terpenes / pharmacology
  • Time Factors
  • Umbelliferones / administration & dosage
  • Umbelliferones / analysis
  • Umbelliferones / pharmacokinetics*

Substances

  • Antioxidants
  • Azepines
  • Cyclohexenes
  • Decanoic Acids
  • Terpenes
  • Umbelliferones
  • laurocapram
  • Oleic Acid
  • decanoic acid
  • Limonene
  • esculetin