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Linear combination methods for prediction of drug skin permeation

Stefan Scheler ; Sandoz GmbH , Biopharmaceuticals, Pharmaceutical & Device Development, Biochemiestrasse 10, 6336 Langkampfen, Austria
Alfred Fahr ; Friedrich Schiller University of Jena, Department of Pharmaceutical Technology, Lessingstr. 8, 07743 Jena, Germany
Xiangli Liu ; Bradford School of Pharmacy, U niversity of Bradford, BD7 1DP, UK

Puni tekst: engleski pdf 1.316 Kb

str. 199-220

preuzimanja: 1.433



Many in-vitro methods for prediction of skin permeability have been reported in literature. Cerasome electrokinetic chromatography is one of the most sophisticated approaches representing a maximum level of similarity to the lipid phase of the stratum corneum. One goal of this study was to investigate the affinity pattern of Cerasome and to compare it with the permeability profile of human skin. Another purpose was to study the applicability of Hansen solubility parameters for modelling skin permeation and to investigate the predictive and explanatory potential of this method. Visualisation in Hansen diagrams revealed very similar profiles of Cerasome electrokinetic chromatography retention factors and skin permeability coefficients. In both cases, the characteristic pattern with two clusters of highly retained or highly permeable substances could be shown to be mainly caused by two groups of compounds, one of them with high affinity to ceramides, fatty acids and lecithin and the other being more affine to cholesterol. If based on a sufficiently comprehensive experimental dataset, model-independent predictions of skin permeability data using three-component Hansen solubility parameters are able to achieve similar accuracy as calculations made with an Abraham linear free energy relationship model in which the compounds are characterized by seven physicochemical descriptors.

Ključne riječi

Cerasome 9005; Liposome electrokinetic chromatography; Linear free energy relationship analysis; Solubility parameter; Stratum corneum

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