Over the last years, the interest of the pharmaceutical industry in the use of therapeutic peptides in diabetes treatment has been increased. However, these are restricted to parenteral administration. In order to mimic the natural physiological response, many efforts have been made towards oral peptide delivery in diabetes treatment. This review article aims to give an overview on the progress in the nanomedicine field towards the design and optimization of nanoparticle-based drug delivery systems capable of overcoming the harsh gastrointestinal environment and achieving an adequate bioavailability following oral administration. The reported data clearly illustrate the promise of nanomedicine for antidiabetic oral peptide delivery