Permeabilities of alkyl p-aminobenzoates through living skin equivalent and cadaver skin.
The in vitro permeabilities of alkyl p-aminobenzoates through living skin equivalent (LSE) and cadaver skin were compared. Methyl, ethyl, and butyl p-aminobenzoates were used as model compounds. The permeabilities of these compounds through LSE and cadaver skin from an aqueous drug suspension were determined with a flow-through diffusion cell. The permeability coefficients of these esters in LSE were an order of magnitude higher than in cadaver skin. This was primarily because of low resistances offered by the outermost layer (i.e., stratum corneum) of LSE. In the case of cadaver skin, the permeability coefficient increased as the carbon chain length increased, whereas no appreciable change in the permeability coefficients of these esters in LSE was observed. These results clearly suggest that the LSE membrane offered very little resistance as opposed to cadaver skin. Therefore, the LSE membrane may not quantitatively represent a good human skin model for evaluating skin permeation of a drug from topical or transdermal formulations.
Roy
S D
SD
Syntex Research, Palo Alto, CA 94304.
Fujiki
J
J
Fleitman
J S
JS
D000478:Alkylation; D062365:Aminobenzoates / Q000737:chemistry / Q000493:pharmacokinetics*; D002102:Cadaver; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005069:Evaluation Studies as Topic; D006801:Humans; D066298:In Vitro Techniques; D008954:Models, Biological; D009795:Octanes / Q000737:chemistry; D010539:Permeability; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption / Q000502:physiology*; D012995:Solubility; D014867:Water / Q000737:chemistry
D062365:Aminobenzoates; D009795:Octanes; D014867:Water