Abstract
In spite of the fact that delivery via the transdermal route is now a commercial reality for a variety of chemically and pharmacologically diverse agents, including scopolamine,1 nitroglycerin,2–4 Clonidine,5 and estradiol,6 the numbers of drugs that meet the physicochemical criteria and have suitable pharmacokinetic properties and adequate potency to be considered as feasible candidates for transdermal delivery is quite limited. The majority of drugs are precluded from consideration for transdermal application because of their limited ability to penetrate the skin at a sufficient rate. For such compounds, methods to enhance penetration must be considered. Penetration enhancement may be accomplished by alteration of the barrier properties of stratum corneum through the use of chemical penetration enhancers, providing an additional driving force for transport (e.g., iontophoresis), or by chemically modifying the drug itself through prodrug formation. The latter approach is the subject of this chapter.
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