Use of targeting agents to increase uptake and localization of drugs to the intestinal epithelium.

Despite early successes in oral drug delivery of small molecules such as antibiotics, cephalosporins and vitamins, little success has been achieved with more recent pharmaceuticals such as peptides and proteins. This lack of success is primarily due to the impenetrable nature of the gastro-intestinal epithelial cell layers. Despite this, many bacteria, viruses and toxins are readily taken up from the intestine and thereby gain entry into the circulation. This review focuses on the use of various surface molecules from these organisms as well as toxin binding subunits as carriers for oral delivery of other molecules. It also describes the subversion of the natural uptake mechanisms for various vitamins and iron to allow for oral delivery of pharmaceuticals. These mechanisms provide exciting solutions to overcome the problems in oral delivery of peptides and proteins, which has been the nemesis of pharmaceutical scientists for many decades.