Nanoparticulate-based drug delivery systems for small molecule anti-diabetic drugs: An emerging paradigm for effective therapy

Emergence of nanoparticulate drug delivery systems in diabetes has facilitated improved delivery of small molecule drugs which could dramatically improve the quality of life for diabetics. Conventional dosage forms of the anti-diabetic drugs exhibit variable/less bioavailability and short half-life, demanding frequent dosing and causing increased side-effects resulting in ineffectiveness of therapy and non-compliance with the patients. Considering the chronic nature of diabetes, nanotechnology-based approaches are more promising in terms of providing site-specific delivery of drugs with higher bioavailability and reduced dosage regimen. Nanomedicines act at the cellular and molecular levels to enhance the uptake of the drug into the cells or block the efflux mechanisms thus retaining the drug inside the cell for a longer duration of time. Many studies have hinted at the possibility of administering peptide drugs like glucagon like peptides orally by encapsulation into nanoparticles. Nanoparticles also allow further modifications including their encapsulation into microparticles, polyethylene glycol (PEG)-PEGylation- or functionalization with ligands for active targeting. Nevertheless, such remarkable benefits are fraught with their long-term safety concerns, regulatory hurdles, limitations of scale-up and ineffective patent protection which have hindered their commercialization. This review summarizes the latest advances in the area of nanoformulations as applied to the delivery of anti-diabetics. STATEMENT OF SIGNIFICANCE: The present work describes the latest advancements in the area of nanoformulations for anti-diabetic therapy along with highlighting the advantages that these nanoformulations offer at molecular level for diabetes. Although several potent orally active anti-hyperglycemic agents are available, the current challenges in efficient management of diabetes include optimization of the present therapies to ensure an optimum and stable level of glucose, and also to reduce the occurrence of long term complications associated with diabetes. Nanoformulations because of their high surface area to volume ratio provide improved efficacy, targeting their delivery to the desired site of action tends to minimize adverse effects and administration of peptide drugs by oral route is also possible by encapsulating them in nanoparticles. As we reflect on the success and failures of latest research on nanoformulations for the treatment of diabetes, it is important not to dwell on lack of FDA approvals but rather define future directions that guarantee more effective anti-diabetic treatment. In proposed review we have explored the latest advancement in anti-diabetic nanotechnology based formulations.