Permeation and distribution of ferulic acid and its α-cyclodextrin complex from different formulations in hairless rat skin

AAPS PharmSciTech. 2011 Jun;12(2):514-20. doi: 10.1208/s12249-011-9609-y. Epub 2011 Apr 14.

Abstract

Ferulic acid (FA) is a natural product that occurs in seeds of many plants where it is generally located in the bran. This compound is a multifunctional ingredient endowed with antioxidative, radical scavenging, sunscreening and antibacterial actions. The aim of this study was to analyse the ferulic acid cutaneous permeation and distribution, through and into the skin layers, from different cosmetic vehicles, an O/W emulsion (pH 6.0) and two gel-type formulations at different pH levels (6.0 and 7.4), containing FA alone or an inclusion complex with α-cyclodextrin (CD-FA). In vitro permeation studies were performed in vertical diffusion cells using hairless rat excised skin. At appropriate intervals of time, the amount of permeated sunscreen/radical scavenger was evaluated by high-performance liquid chromatography (HPLC). At the end of experiments, treated skin samples were sectioned with a cryomicrotome and the FA content of the individual slices was analysed by HPLC. FA-containing formulations, O/W emulsion, gels A and B, originated FA fluxes of 8.48 ± 2.31, 8.38 ± 0.89 and 5.72 ± 0.50 μg/cm(2) h, respectively, thus suggesting the pH influence on FA percutaneous permeation. The use of the inclusion complex, CD-FA, determined in all cases a decrease of FA transdermal permeation while no influence of pH was observed. Gel-type formulations containing FA ensured higher sunscreen storage in the superficial layers if compared with O/W emulsion. When FA was included in α-cyclodextrin, FA amount retained into skin layers decreased markedly.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Topical
  • Animals
  • Chemistry, Pharmaceutical / standards
  • Coumaric Acids / administration & dosage
  • Coumaric Acids / pharmacokinetics*
  • Coumaric Acids / standards
  • Male
  • Permeability
  • Rats
  • Rats, Hairless
  • Skin Absorption / drug effects
  • Skin Absorption / physiology*
  • alpha-Cyclodextrins / administration & dosage
  • alpha-Cyclodextrins / pharmacokinetics*
  • alpha-Cyclodextrins / standards

Substances

  • Coumaric Acids
  • alpha-Cyclodextrins
  • ferulic acid
  • alpha-cyclodextrin