Abstract
Peptides are small biomolecules known to stimulate or inhibit important functions in the human body. The clinical use of peptides by oral delivery, however, is very limited due to their sensitive structure and physiological barriers present in the gastrointestinal tract. These barriers can be overcome with chemical and mechanical approaches protease inhibitors, permeation enhancers, and polymeric encapsulation. Studying the success of these approaches pre-clinically with imaging techniques such as fluorescence imaging (IVIS) and optical microscopy is difficult due to the lack of in-depth penetration. In comparison, nuclear imaging provides a better platform to observe the gastrointestinal transit and quantitative distribution of radiolabeled peptides. This review provides a brief background on the oral delivery of peptides and states examples from the literature on how nuclear imaging can help to observe and analyze the gastrointestinal transit of oral peptides. The review connects the fields of peptide delivery and nuclear medicine in an interdisciplinary way to potentially overcome the challenges faced during the study of oral peptide formulations.