Gm. Pauletti et al., IMPROVEMENT OF ORAL PEPTIDE BIOAVAILABILITY - PEPTIDOMIMETICS AND PRODRUG STRATEGIES, Advanced drug delivery reviews, 27(2-3), 1997, pp. 235-256
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.