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Percutaneous penetration of drugs: a quantitative structure-permeability relationship study

el Tayar, Nabil
Tsai, Ruey-Shiuan
Testa, Bernard
Hansch, C.
Leo, A.
Published in Journal of pharmaceutical sciences. 1991, vol. 80, no. 8, p. 744-749
Abstract Human skin permeation data taken from the literature were analyzed for quantitative relationships with physicochemical properties and structural descriptors. No correlations exist with molecular weights and solvent-accessible surface areas. In most cases, skin permeation was inversely correlated with the parameter delta log Poct-hep (i.e., log Poctanol minus log Pheptane), which is mainly a measure of the H-bond donor acidity of the solutes. Lipophilicity itself, as expressed by log Poctanol, also contributes positively to skin permeation in some cases. The results of this quantitative structure-permeability relationship study are interpreted in terms of a unified mechanistic model whereby drugs can permeate via an intercellular route (correlation with both delta log Poct-hep and log Poct) and/or a transcellular route (correlation with log Poct only).
Keywords Administration, TopicalAlcohols/chemistry/pharmacokineticsAnti-Inflammatory Agents/chemistryChemistry, PhysicalHumansHydrocortisoneHydrogen BondingMolecular WeightOctanolsPhenols/chemistryPhysicochemical PhenomenaSkin AbsorptionSolubilitySolventsSteroids/chemistry/pharmacokineticsStructure-Activity RelationshipSurface Properties
PMID: 1791533
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EL TAYAR, Nabil et al. Percutaneous penetration of drugs: a quantitative structure-permeability relationship study. In: Journal of pharmaceutical sciences, 1991, vol. 80, n° 8, p. 744-749. doi: 10.1002/jps.2600800807

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Deposited on : 2010-08-06

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