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Title

Quantitative structure-permeation relationships for solute transport across silicone membranes

Authors
Geinoz, S.
Rey, S.
Boss, G.
Bunge, A. L.
Reist, Marianne
Testa, Bernard
Published in Pharmaceutical Research. 2002, vol. 19, no. 11, p. 1622-1629
Abstract PURPOSE: The purpose of this work was to assess the molecular properties that influence solute permeation across siliconemembranes and to compare the results with transport across human skin. METHODS: The permeability coefficients (log Kp) of a series of model solutes across silicone membranes were determined from the analysis of simple transport experiments using a pseudosteady-state mathematical model of the diffusion process. Subsequently, structure permeation relationships were constructed and examined, focusing in particular on the difference between solute octanol/water and 1,2 dichloroethane/water partition coefficients (deltalog P(oct-dce)), which re ported upon H-bond donor activity, and the computationally derived molecular hydrogen-bonding potential. RESULTS: The hydrogen-bond donor acidity and the lipophilicity of the compounds examined greatly influenced their permeation across sil cone membranes. Furthermore, for a limited dataset, a significant correlation was identified between solute permeation across silicone membranes and that through human epidermis. CONCLUSION: The key molecular properties that control solute perme ation across silicone membranes have been identified. For the set of substituted phenols and other unrelated compounds examined here a similar structure-permeation relationship has been derived for their transport through human epidermis, suggesting application of the results to the prediction of flux across biological barriers.
Keywords Biological Transport/drug effects/physiologyDiffusion Chambers, Culture/methodsMembranes, ArtificialModels, TheoreticalPermeability/drug effectsPharmaceutical Preparations/chemistry/*metabolismQuantitative Structure-Activity RelationshipSilicones/chemistry/*pharmacokinetics
Stable URL http://archive-ouverte.unige.ch/unige:10577
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PMID: 12458667
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