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Related Experiment Videos

Predicting skin permeability.

R O Potts1, R H Guy

  • 1Cygnus Therapeutic Systems, Redwood City, California 94063.

Pharmaceutical Research
|May 1, 1992
PubMed
Summary
This summary is machine-generated.

This study models compound transport through mammalian epidermis using molecular size and lipophilicity. Results show stratum corneum lipids explain permeability, negating the need for a pore pathway for small molecules.

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Area of Science:

  • Dermatology
  • Pharmacokinetics
  • Biophysics

Background:

  • Mammalian epidermis acts as a barrier to compound transport.
  • Understanding percutaneous absorption is crucial for drug delivery and toxicology.
  • Physicochemical properties influence a compound's ability to penetrate the skin.

Purpose of the Study:

  • To develop a predictive model for percutaneous flux based on molecular properties.
  • To elucidate the role of stratum corneum lipids in molecular transport.
  • To investigate the necessity of an aqueous pathway for small molecule permeation.

Main Methods:

  • Analysis of published permeability coefficient (Kp) data for over 90 diverse compounds.
  • Application of a model correlating Kp with molecular volume (MV) or molecular weight (MW) and octanol/water partition coefficient (Koct).

Related Experiment Videos

  • Evaluation of the contribution of stratum corneum intercellular lipid properties to Kp.
  • Main Results:

    • Stratum corneum intercellular lipid properties sufficiently explain Kp dependence on MV/MW and Koct.
    • An aqueous-polar pathway is not required to explain Kp values for small, polar nonelectrolytes.
    • The high diffusivity of small molecules accounts for their seemingly high Kp values.

    Conclusions:

    • A simple model based on physicochemical properties can predict percutaneous flux.
    • Intercellular lipids are the primary determinant of molecular transport across the stratum corneum.
    • The model provides insights into the biophysical mechanisms of skin penetration.