The development of oral dosage forms that allows absorption of peptides to the systemic circulation still is one of the greatest challenges in pharmaceutical industry. The current drug delivery systems act merely as a vehicle, and none of them has exploited their potential physiological effect. In this thesis, we exploited the physiology of L cells, developing and further modifying an innovative nanocapsule-based nanosystem increasing the stimulation of glucagon-like peptide-1 (GLP-1) and the systemic absorption of exenatide (a GLP-1 receptor agonist) for the treatment of type 2 diabetes mellitus via oral route. This newly developed nanosystem was found to be at least as efficient as the current marketed drug (subcutaneous) at decreasing the hyperglycemia and hyperinsulinemia and treating type 2 diabetes mellitus. In conclusion, this work maximizes the potential of the nanocarriers over current approaches in incretin-based diabetic treatment via oral route.