Topical Delivery Using Prodrugs
The objective of any prodrug approach is to transiently mask a particular functional group in a drug and thus change its physicochemical properties (solubility profile, degree of ionization), protect it from premature chemical or biological metabolism, or facilitate its active or passive transport across a biological barrier, to name only a few of the more obvious applications. In the example of the use of a prodrug approach to enhance topical delivery, a change in the physicochemical properties of the drug is the objective. That change is designed to facilitate the passive absorption across the stratum corneum (SC)—wherein lies the major barrier to permeation—into the viable epidermis and beyond, if necessary. More complete descriptions of the skin can be found in other references (Barry, 1983). Here, we use the term “topical delivery” to include dermal delivery (delivery into the skin) and transdermal delivery (delivery through the skin into systemic circulation).
KeywordsParent Drug Aqueous Solubility Receptor Phase Topical Delivery Hairless Mouse Skin
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