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Related Experiment Videos

Percutaneous absorption: in vivo experiments.

W J Albery, J Hadgraft

    The Journal of Pharmacy and Pharmacology
    |March 1, 1979
    PubMed
    Summary
    This summary is machine-generated.

    Percutaneous absorption of nicotinic acid esters in humans shows erythema develops before steady-state diffusion. Methyl nicotinate penetrates the skin via interstitial channels, not keratinized cells, regardless of the formulation.

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    Area of Science:

    • Dermatology
    • Pharmacokinetics
    • Skin Physiology

    Background:

    • Percutaneous absorption is crucial for topical drug delivery.
    • Understanding the penetration pathway of active ingredients is essential for formulation development.
    • Nicotinic acid esters are known to cause skin flushing (erythema).

    Purpose of the Study:

    • To investigate the percutaneous absorption kinetics of nicotinic acid esters in humans.
    • To determine the primary route of penetration for methyl nicotinate through the skin.
    • To compare absorption characteristics with other substances and formulations.

    Main Methods:

    • In vivo human studies measuring erythema onset time.
    • Continuous and 'pulse' application experiments.

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  • Analysis of diffusion coefficients and penetration pathways using mathematical models and comparative data.

    • Main Results:

    • Erythema occurred significantly before steady-state diffusion across the epidermis was achieved.
    • The penetration of methyl nicotinate followed the equation D/l² = 2.3 X 10⁻⁴ s⁻¹.
    • Methyl nicotinate penetration occurred through interstitial channels, not keratinized cells, irrespective of the external phase (e.g., glycerol-water mixtures, creams, ointments).
    • Comparative data for salicylic acid, carbinoxamine, and other substances also support an interstitial route of penetration.

    Conclusions:

    • The percutaneous absorption of methyl nicotinate is a rapid process where erythema precedes epidermal steady-state diffusion.
    • Skin penetration of methyl nicotinate occurs primarily via interstitial pathways.
    • The route of penetration is independent of the vehicle formulation, suggesting a consistent biological pathway.