Table of Contents
Metal-Based Drugs
Volume 3 (1996), Issue 6, Pages 277-286

Transepithelial Transport and Metabolism of Boronated Dipeptides Across Caco-2 and HCT-8 Cell Monolayers

1Division of Medicinal Chemistry and Natural Products, School of Pharmacy, Beard Hall, CB# 7360, University of North Carolina, Chapel Hill 27599-7360, NC, USA
2Boron Biologicals, Inc., 620 Huitton St., Suite 104, Raleigh 27606, NC, USA
3School of Pharmacy, Samford University, Birmingham 35229, AL, USA

Received 29 December 1996

Copyright © 1996 Hindawi Publishing Corporation. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


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.