The treatment of Diabetes Mellitus (DM), a chronic disease, is primarily based upon administration of insulin forms to patients. Conventional subcutaneous administration is associated with a large number of complications, therefore, several new strategies have been developed. Amongst these strategies, oral insulin administration is much less invasive and, therefore, well tolerated. In recent years, various nanoformulations were developed for the oral administration of insulin, allowing more effective stabilization of the active pharmaceutical ingredient and modified for better absorption along the gastrointestinal tract. The development of different oral insulin nanoformulations in academic research as well as in patents, including the development of nanoparticles, liposomes, nanoemulsions and the use of cyclodextrins deserves special attention. The future of oral insulin nanoformulations is dependent on strategies utilizing simple technologies that stabilize the raw material, including inclusion within cyclodextrins or inclusion in low weight molecular mass polymers/ oligomers. All of the theories developed here provide a solid foundation upon which to develop new methods for the production of pharmaceutical peptide formulations. In addition, the effective search for existing nanometric formulations of insulin could provide economically viable therapeutic options that can consequently be produced on an industrial scale.