Influence of membrane-solvent-solute interactions on solute permeation in skin.
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.
Dias
M
M
Department of Pharmaceutics, School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.
Hadgraft
J
J
Lane
M E
ME
D000704:Analysis of Variance; D019817:Benzoic Acid / Q000737:chemistry / Q000378:metabolism*; D002110:Caffeine / Q000737:chemistry / Q000378:metabolism*; D002463:Cell Membrane Permeability / Q000187:drug effects*; D004058:Diffusion; D015194:Diffusion Chambers, Culture; D004817:Epidermis / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D008567:Membranes, Artificial; D008954:Models, Biological; D015394:Molecular Structure; D020156:Salicylic Acid / Q000737:chemistry / Q000378:metabolism*; D012828:Silicones / Q000737:chemistry; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D012997:Solvents / Q000494:pharmacology*; D013997:Time Factors
D008567:Membranes, Artificial; D012828:Silicones; D012997:Solvents; D002110:Caffeine; D019817:Benzoic Acid; D020156:Salicylic Acid