Influence of membrane-solvent-solute interactions on solute permeation in skin

Int J Pharm. 2007 Aug 1;340(1-2):65-70. doi: 10.1016/j.ijpharm.2007.03.030. Epub 2007 Mar 30.

Abstract

The relative importance of solubility parameters and other solvent properties on membrane diffusion processes has not been fully elucidated in the literature. Previously, we have studied the effect of different vehicles on the permeation of caffeine, benzoic acid (BA) and salicylic acid (SA) through silicone membranes. The present paper investigates diffusion of the selected permeants from different saturated solutions through human epidermis. The permeation of caffeine was strongly affected by the vehicle chosen and the maximum enhancement observed for the permeation of caffeine was 288-fold. A maximum of 12-fold enhancement in the flux was observed for the permeation of SA and a maximum of 10-fold enhancement was observed for the permeation of BA. The diffusion profiles obtained for SA in the different solvents were very similar when compared with those obtained for BA but the permeation rates were higher for BA than for SA. This similarity results from the similar chemical structure and lipophilicity.

Publication types

  • Comparative Study

MeSH terms

  • Analysis of Variance
  • Benzoic Acid / chemistry
  • Benzoic Acid / metabolism*
  • Caffeine / chemistry
  • Caffeine / metabolism*
  • Cell Membrane Permeability / drug effects*
  • Diffusion
  • Diffusion Chambers, Culture
  • Epidermis / drug effects*
  • Epidermis / metabolism
  • Humans
  • Membranes, Artificial
  • Models, Biological
  • Molecular Structure
  • Salicylic Acid / chemistry
  • Salicylic Acid / metabolism*
  • Silicones / chemistry
  • Skin Absorption / drug effects*
  • Solubility
  • Solvents / pharmacology*
  • Time Factors

Substances

  • Membranes, Artificial
  • Silicones
  • Solvents
  • Caffeine
  • Benzoic Acid
  • Salicylic Acid