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Transdermal peptide delivery.

H E Bodde¹, J C Verhoef, M Ponec

¹Center for Bio-Pharmaceutical Sciences, Leiden, The Netherlands.

Biochemical Society Transactions

|October 1, 1989

Summary

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Transdermal delivery of peptide drugs like des-enkephalin-gamma-endorphin shows potential. Enhancing peptide flux, possibly via iontophoresis, is key to improving transdermal bioavailability, as intra-epidermal degradation is minimal.

Area of Science:

Pharmacology
Drug Delivery
Dermatology

Background:

Transdermal drug delivery offers advantages in pharmacotherapeutics and patient compliance for peptide drugs.
Peptide drugs face challenges in transdermal delivery due to hydrophilicity and high molecular mass.
Iontophoresis has shown promise in achieving effective in vivo transdermal dosing for peptides.

Purpose of the Study:

To investigate the transepidermal permeation of the dodecapeptide, des-enkephalin-gamma-endorphin, in vitro.
To study the in vitro intra(epi-)dermal biotransformation of des-enkephalin-gamma-endorphin.
To assess methods for enhancing the transdermal delivery of this peptide.

Main Methods:

In vitro study of transepidermal permeation through human stratum corneum.

Related Experiment Videos

In vitro assessment of peptide biotransformation within epidermal and dermal layers.

Evaluation of skin lipid fluidizers to enhance peptide flux.

Main Results:

Measurable, albeit small, peptide fluxes were observed through human stratum corneum in vitro.
Skin lipid fluidizers demonstrated an ability to enhance these peptide fluxes.
The peptide exhibited a surprisingly long half-life in both epidermis and dermis compared to human plasma.

Conclusions:

Enhancing transdermal flux, potentially using iontophoresis, is the primary strategy for improving peptide bioavailability.
Intra(epi-)dermal degradation is a minor limiting factor in the transdermal delivery of this dodecapeptide.
Transdermal delivery of des-enkephalin-gamma-endorphin is feasible, with flux enhancement being the main challenge.