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Iontophoretic delivery of biomolecules is an attractive strategy for overcoming skin permeability barriers, since it allows the delivery of molecules at the tissue interface. Molecules to be delivered by iontophoresis include pendant groups for enhanced permeation, such as a fatty acid moiety. The effective use of a transdermal microneedle device for iontophoretic delivery could be an alternative strategy for the delivery of these molecules. In this work, an iontophoretic prodrug formulation (pro-transfene) is developed using the transdermal transport of an alanine-substituted methionine salt and the use of a microneedle array to enhance the skin permeability of this compound. This approach is the first report of an iontophoretically enhanced prodrug formulation for transferrin in vitro and in vivo.|object_id|obj_id|