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Related Experiment Videos

Percutaneous penetration enhancement and its quantification

M Bach1, B C Lippold

  • 1Institut für Pharmazeutische Technologie, Heinrich-Heine-Universität Düsseldorf, Germany.

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V
|August 12, 1998
PubMed
Summary

Penetration enhancers increase drug diffusion and solubility in the skin barrier. These effects can be quantified by measuring drug fluxes or pharmacodynamic responses, considering thermodynamic drug activity.

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Area of Science:

  • Pharmacology
  • Dermatology
  • Physical Chemistry

Background:

  • Drug penetration through the stratum corneum is crucial for topical and transdermal therapies.
  • Structural alterations of the stratum corneum can enhance drug permeation.
  • Quantifying these enhancing effects is essential for developing effective drug delivery systems.

Purpose of the Study:

  • To elucidate the mechanisms of penetration enhancement.
  • To establish methods for quantifying drug penetration enhancement.
  • To relate penetration enhancement to thermodynamic drug activity.

Main Methods:

  • Direct determination of drug fluxes across the stratum corneum.
  • Indirect determination via pharmacodynamic response measurements.

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  • Consideration of thermodynamic drug activity in all measurements.
  • Main Results:

    • Penetration enhancers increase the drug diffusion coefficient (DB) and/or drug solubility in the barrier (csB).
    • Pharmacodynamic measurements allow quantification of enhancement by comparing activity-response lines.
    • Activity-standardized bioavailability factors (fa) reflect enhancer-induced changes in permeability (PB).

    Conclusions:

    • Penetration enhancement can be accurately quantified using direct or indirect methods.
    • Thermodynamic drug activity is a critical factor in assessing enhancement effects.
    • Understanding these principles aids in the design of improved transdermal drug delivery systems.