en
Scientific article
English

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

Published inJournal of pharmaceutical sciences, vol. 80, no. 8, p. 744-749
Publication date1991
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, Topical
  • Alcohols/chemistry/pharmacokinetics
  • Anti-Inflammatory Agents/chemistry
  • Chemistry, Physical
  • Humans
  • Hydrocortisone
  • Hydrogen Bonding
  • Molecular Weight
  • Octanols
  • Phenols/chemistry
  • Physicochemical Phenomena
  • Skin Absorption
  • Solubility
  • Solvents
  • Steroids/chemistry/pharmacokinetics
  • Structure-Activity Relationship
  • Surface Properties
Affiliation Not a UNIGE publication
Citation (ISO format)
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
Identifiers
ISSN of the journal0022-3549
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