Dermal absorption of chemicals is an area of increasing interest to the pharmaceutical and cosmetic industries, as well as in dermal exposure and risk assessment processes. In this paper the capability of biopartitioning micellar chromatography (BMC) as an in vitro technique to describe compound percutaneous absorption is evaluated. A multivariate study (principal component analysis, partial least squares) is performed in order to evaluate the importance of some physicochemical variables on the skin permeability constant values. From these results, a quantitative retention-activity relationship model for predicting the skin permeability constants that uses the BMC retention data and melting point as descriptor variables was obtained from a heterogeneous set of 43 compounds. The main advantage of the proposed methodology is that it allows the obtention of permeability constants of ionic compound and it can be very useful to predict the effect of pH of vehicle on the skin permeability of xenobiotics.
The application of the short-end capillary injection to capillary electrophoresis frontal analysis (CE-FA) to study the interaction between basic, neutral and acid drugs towards human serum albumin (HSA) at near-physiological conditions is presented. The compounds selected display a wide range of binding affinities and the results obtained were in good agreement with those reported in the literature. An equation for the estimation of the number of primary binding sites and their corresponding affinity constants is developed isolating the experimentally measured variables in just one axis. The proposed CE-FA method to screen drug interactions with HSA under physiological conditions is simple, rapid and cost-effective what may facilitate its implementation in the drug discovery process.
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