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Related Experiment Videos

Iontophoretic transport pathways: dependence on penetrant physicochemical properties

N G Turner1, R H Guy

  • 1Department of Biopharmaceutical Sciences, University of California-San Francisco 94143-0446, USA.

Journal of Pharmaceutical Sciences
|January 10, 1998
PubMed
Summary

Iontophoresis enhances skin penetration differently based on molecule properties. Charged molecules like calcein use follicular pathways, while neutral molecules like nile red show minimal enhancement.

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Area of Science:

  • Dermal drug delivery
  • Transdermal iontophoresis
  • Skin penetration science

Background:

  • Understanding molecular transport across skin is crucial for effective transdermal drug delivery.
  • Physicochemical properties significantly influence how molecules interact with and permeate biological barriers like skin.

Purpose of the Study:

  • To investigate how molecular physicochemical properties dictate preferred iontophoretic transport pathways in skin.
  • To compare the skin penetration routes of hydrophilic, charged molecules versus lipophilic, neutral molecules using iontophoresis.

Main Methods:

  • Utilized laser scanning confocal microscopy (LSCM) to visualize the distribution of fluorescently labeled molecules in hairless mouse skin.
  • Employed iontophoresis and passive delivery methods to study the percutaneous transport of calcein (hydrophilic, -4 charge) and nile red (lipophilic, neutral).

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  • Conducted sequential (dual) transport studies with both fluorophores to directly compare their pathways.

    • Main Results:

    • Nile red, a lipophilic molecule, permeated the skin via distinct inter- and intracellular routes, with minimal iontophoretic enhancement.
    • Calcein, a hydrophilic, charged molecule, showed negligible passive skin entry but significant iontophoretic transport, primarily through follicular pathways.
    • Dual transport studies confirmed the distinct pathways utilized by molecules with differing physicochemical properties.

    Conclusions:

    • Iontophoretic transport pathways across the skin are primarily determined by the penetrant's physicochemical properties.
    • Molecular affinity for different skin microenvironments dictates the preferential route of iontophoretic delivery.
    • Targeted iontophoretic strategies can be developed by considering molecular charge and lipophilicity for optimized transdermal delivery.