Partitioning, diffusivity and clearance of skin permeants in mammalian dermis.

Partitioning, diffusivity and clearance of skin permeants in mammalian dermis. Research Abstract Details 

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Partitioning, diffusivity and clearance of skin permeants in mammalian dermis. Abstract Text:

Kosmas Kretsos,Matthew A Miller,Grettel Zamora-Estrada,Gerald B Kasting,Kosmas Kretsos,Matthew A Miller,Grettel Zamora-Estrada,Gerald B Kasting,Kosmas Kretsos,Matthew A Miller,Grettel Zamora-Estrada,Gerald B Kasting,

The partition coefficients (K(de)) and diffusivities (D(de)) of compounds in mammalian dermis were examined through an analysis of in vitro permeation data obtained from the literature combined with experimental results with the test permeant, (3)H-testosterone. The literature data involved 26 compounds ranging in molecular weight from 18 to 476Da and four species-human, guinea pig, rat and mouse. Testosterone was studied by permeation and desorption measurements employing excised human dermis in the presence and absence of external serum albumin. Mathematical models for both K(de) and D(de) were developed. The K(de) model involved ionization, binding to extravascular serum proteins and partitioning into a small lipid compartment. The D(de) model employed a free diffusivity with a liquid-like size dependence multiplied by a binding factor derived from K(de). An additional analysis considered in vivo dermal concentration profiles of topically applied permeants. Literature data for 5 of 6 permeants were shown to be well described by a previously published model for capillary clearance in the dermis, which leads to an exponential decay of concentration with depth. Computed decay lengths (1/e values) ranged from 210 to 920mum, and the corresponding clearance rate constants k(de) ranged from 0.9x10(-4) to 14x10(-4)s(-1) (n=8). Departures from the exponential decay profile are discussed in terms of non-uniform capillary clearance and incomplete attainment of a steady-state.

Partitioning, diffusivity and clearance of skin permeants in mammalian dermis. Publishing Authors By Initials

K Kretsos,MA Miller,G Zamora-Estrada,GB Kasting,K Kretsos,MA Miller,G Zamora-Estrada,GB Kasting,K Kretsos,MA Miller,G Zamora-Estrada,GB Kasting,

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Partitioning, diffusivity and clearance of skin permeants in mammalian dermis. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: International journal of pharmaceutics

VOLUME: 346

Page Numbers: 64-79

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ISSN: 0378-5173

DAY: 23

MONTH: 06

YEAR: 2007

Partitioning, diffusivity and clearance of skin permeants in mammalian dermis. Information

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LANGUAGE: eng

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AFFILIATION: College of Pharmacy, University of Cincinnati Academic Health Center, P.O. Box 670004, Cincinnati, OH 45267-0004, USA.

Country: Netherlands

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MEDLINETA: Int J Pharm

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