ABSTRACT
Prodrugs are molecules that must undergo biotransformation prior to exhibiting their therapeutic effects. First defined by Adrian Albert, but practiced earlier, prodrug approaches to modified drug delivery have principally been used to overcome various shortcomings of therapeutic agents having some barrier to their optimal usefulness. The transport of a lipophilic compound in lymph in association with chylomicrons requires not only that the drug/prodrug have an affinity for the chylomicron relative to the aqueous fraction of lymph, but it must have the capacity to “dissolve” in that phase. The esters were administered in either oleic acid or other lipophilic solvents. The chapter aims to review the available data pertaining to the manipulation of small molecule delivery to the lymph. It focuses on delivery to the intestinal lymphatics after oral drug/prodrug administration because of the greater interest in oral drug delivery compared to parenteral routes of administration.
