Alkylglycerol Derivatives, a New Class of Skin Penetration Modulators

Molecules. 2017 Jan 22;22(1):185. doi: 10.3390/molecules22010185.

Abstract

The absorption modulating activity of two alkylglycerol derivatives (batyl and chimyl alcohol) on skin barrier properties was evaluated. Biophysical tests such as transepidermal water loss (TEWL) and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy, as well as in vitro skin permeation studies, were performed in order to determine the effect of these compounds as chemical absorption modulators. Four drugs were used as models: three NSAIDS (diclofenac, naproxen, and piroxicam) and glycyrrhizic acid. The results showed that treatment of the skin with alkylglycerols caused (i) a reduction on the amount of drug permeated; (ii) a reduction in TEWL; and (iii) changes in the ATR-FTIR peaks of stratum corneum lipids, indicative of a more ordered structure. All of these findings confirm that alkyl glycerols have an absorption retarding effect on the drugs tested. Such effects are expected to give rise to important applications in the pharmaceutical and cosmetic sectors, in cases where it is desirable for the drug to remain in the superficial layers of the skin to achieve a local effect.

Keywords: absorption modulators; absorption retarders; alkylglycerols; attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy; skin permeation; transepidermal water loss (TEWL).

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Diclofenac / administration & dosage
  • Diclofenac / metabolism
  • Drug Carriers / pharmacology*
  • Glyceryl Ethers / pharmacology*
  • Glycyrrhizic Acid / administration & dosage
  • Glycyrrhizic Acid / metabolism
  • Naproxen / administration & dosage
  • Naproxen / metabolism
  • Permeability / drug effects*
  • Piroxicam / administration & dosage
  • Piroxicam / metabolism
  • Skin / drug effects
  • Skin / metabolism*
  • Skin Absorption / drug effects*
  • Spectroscopy, Fourier Transform Infrared
  • Swine

Substances

  • Drug Carriers
  • Glyceryl Ethers
  • Piroxicam
  • Diclofenac
  • batyl alcohol
  • Naproxen
  • Glycyrrhizic Acid
  • chimyl alcohol