IMPROVEMENT OF ORAL PEPTIDE BIOAVAILABILITY - PEPTIDOMIMETICS AND PRODRUG STRATEGIES

Clinical development of orally active peptide drugs has been restricte d by their unfavorable physicochemical properties, which limit their i ntestinal mucosal permeation and their lack of stability against enzym atic degradation. Successful oral delivery of peptides will depend, th erefore, on strategies designed to alter the physicochemical character istics of these potential drugs, without changing their biological act ivity, in order to overcome the physical and biochemical barrier prope rties of the intestinal cells. This manuscript will focus on the physi ological limitations for oral peptide delivery and on various strategi es using chemical modifications to improve oral bioavailability of pep tide-based drugs. (C) 1997 Elsevier Science B.V.