PRODRUG STRATEGIES TO ENHANCE THE INTESTINAL-ABSORPTION OF PEPTIDES

Clinical development of orally active peptide drugs has been restricte d by the unfavorable physicochemical properties of these molecules lim iting intestinal mucosal permeation and the lack of stability of pepti des against enzymatic degradation. Successful oral delivery of pep tid es will depend, therefore, on strategies designed to alter the physico chemical characteristics of these potential drugs,without changing the ir biological activity, in order to increases the permeation across in testinal cells. This manuscript will focus on the biological barrier p roperties that limit oral peptide bioavailabiiity and on prodrug strat egies designed to overcome these barriers.