Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 13, Pages 3948-3954Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm060230+
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This work was devoted to the search for new artificial membranes allowing a rapid evaluation of passive human skin permeation of compounds with a parallel artificial membrane permeability assay ( PAMPA). Effective permeability coefficients ( P-e) determined for a set of compounds using the PAMPA technique with isopropyl myristate ( IPM) and silicone oil, alone or in mixture, were compared to the corresponding human skin permeability coefficient values ( K-p). A good correlation between Pe and Kp was found for compounds tested through a membrane consisting of 70% silicone and 30% IPM. Moreover, positive correlation between the membrane retention of compounds and stratum corneum/water partition coefficients ( P-SC) was established. These results showed that this new artificial membrane, defined as PAMPA-skin, is able to mimic the main barrier properties of human stratum corneum and can be used for the fast prediction of passive human skin permeability coefficients.
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