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Related Experiment Videos

Hydrocortisone (cortisol) concentration and penetration gradient

G Kranz, H Schaefer, A Zesch

    Acta Dermato-Venereologica
    |January 1, 1977
    PubMed
    Summary
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    Higher hydrocortisone (Cortisol) concentrations in ointments do not proportionally increase skin penetration or therapeutic effects beyond a certain threshold. Removing the skin's horny layer significantly enhances drug absorption.

    Area of Science:

    • Dermatology
    • Pharmacokinetics
    • Formulation Science

    Background:

    • Hydrocortisone (Cortisol) is a widely used topical corticosteroid.
    • Understanding drug penetration through skin layers is crucial for topical formulation efficacy.
    • The stratum corneum (horny layer) acts as a primary barrier to topical drug absorption.

    Purpose of the Study:

    • To investigate hydrocortisone penetration into excised skin layers from various ointment concentrations.
    • To determine the impact of the stratum corneum on hydrocortisone absorption.
    • To assess the relationship between hydrocortisone concentration and vasoconstrictive effect.

    Main Methods:

    • Incorporation of hydrocortisone into four ointments at concentrations of 0.1%, 0.3%, 1%, and 3%.

    Related Experiment Videos

  • In vitro skin penetration studies using excised skin with and without the horny layer.
  • In vivo vasoconstriction testing to evaluate biological response.

    • Main Results:

    • Below 1% (intact stratum corneum) or 0.3% (removed stratum corneum), ointment concentration linearly correlated with tissue concentration.
    • Above these levels, doubling ointment concentration yielded only a 20-50% increase in tissue concentration.
    • Stratum corneum removal increased dermal hydrocortisone concentrations 100-fold.
    • Vasoconstrictive effects plateaued above 1% hydrocortisone concentration.

    Conclusions:

    • Hydrocortisone penetration and vasoconstrictive efficacy show diminishing returns at higher concentrations.
    • The stratum corneum significantly limits topical hydrocortisone absorption.
    • Optimizing topical steroid efficacy involves considering formulation concentration relative to skin barrier function.