title: Transdermal drug transport and metabolism. I. Comparison of in vitro and in vivo results.
abstract: Using excised human skin and tissue grafted to athymic mice, the in vitro and in vivo delivery and metabolism of a salicylate diester were compared. Concentration profiles of this drug and its metabolites were obtained for the outer several hundred microns of the skin. These results show significant differences in the extent of enzymatic cleavage and distribution of metabolites between in vitro and in vivo studies. Furthermore, these data suggest that in vitro results may overestimate metabolism because of increased enzymatic activity and/or decreased capillary removal.
authors.affiliation: Pfizer Central Research, Groton, Connecticut 06340.
authors.forename: D B
authors.initials: DB
authors.lastname: Guzek
authors.forename: A H
authors.initials: AH
authors.lastname: Kennedy
authors.forename: S C
authors.initials: SC
authors.lastname: McNeill
authors.forename: E
authors.initials: E
authors.lastname: Wakshull
authors.forename: R O
authors.initials: RO
authors.lastname: Potts
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002264:Carboxylic Acids / Q000008:administration & dosage*; D004952:Esters / Q000008:administration & dosage* / Q000378:metabolism / Q000493:pharmacokinetics; D006801:Humans; D066298:In Vitro Techniques; D051379:Mice; D008819:Mice, Nude / Q000378:metabolism; D012459:Salicylates / Q000008:administration & dosage* / Q000378:metabolism / Q000493:pharmacokinetics; D020156:Salicylic Acid
chemical_list: D002264:Carboxylic Acids; D004952:Esters; D012459:Salicylates; D020156:Salicylic Acid