Drug delivery methods based on nanoparticles have shown great promise in the effective administration of medicinal drugs, such as inhibitors of Dipeptidyl Peptidase (DPP). In the treatment of type 2 diabetes, DPP inhibitors are commonly used, and their formulation as nanoparticles offers numerous advantages, such as enhanced bioavailability, controlled release, and targeted delivery. However, several challenges exist in formulating DPP inhibitors into nanoparticles, including drug stability, particle size control, and sustained release kinetics. This review article aims to discuss the challenges associated with nanoparticle formulation of DPP inhibitors and highlight recent innovative approaches to overcome these limitations.