Oral delivery of proteins and peptides as therapeutic agents is problematic due to their low bioavailability.
This study examined the effect of boronation on the transepithelial transport and metabolism of three
glycine-phenylalanine dipeptides in Caco-2 and HCT-8 cell monolayers. The three dipeptides exhibited
passive transport characteristics in the monolayer systems. However, metabolism of the boronated
dipeptides did occur, but to a lesser extent than the non-boronated glycine-phenylalanine dipeptide. The
same metabolic scheme was seen in both cell monolayer system, but greater metabolism was seen in the
HCT-8 cell monolayers.