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Abstract Nanomedicine holds great interest over the past 20 years and nanotechnology has improved both diagnostics and therapeutics in several medical fields, including, but not limited to, oncology, cardiology, and diabetology. Indeed, multiple conventional antidiabetic agents are clinically approved for the treatment of Type 2 diabetes mellitus (T2DM) for improving the lives of patients and slowing the progression of disease. Alpha-glucosidase inhibitors (AGIs) have shown potential as effective therapies in the clinic among other treatment strategies. In this work, one such AGI, miglitol, was loaded into periodic mesoporous organosilica nanoparticles (PMO NPs) to improve the compound’s antidiabetic activity and minimize cytotoxicity. PMO NPs were initially constructed through a sol–gel technique, and were used to encapsulate high payloads of miglitol. TEM and DLS analysis revealed that both unloaded and loaded PMO NPs were spherical in shape with a diameter range of 324- 370 nm and a relatively high surface negative charge ranging between – 22 to –35 mV. TGA, FTIR, PXRD analyses also confirmed the effective loading of the drug into the PMO NPs (i.e., up to ca. 89.3% loading efficiency). Release kinetics experiment showed minimum release of drug from PMO, ensure major amount of drug remains associated with PMO. A 30 mg/kg dose of both pure miglitol drug and miglitol-loaded PMO (Mig-PMO) NPs were orally administered to diabetic rats and their treatment progression was monitored as compared with both healthy rats (positive control) and untreated diabetic rats (negative control). These animal studies revealed that the PMO nanoparticles are nontoxic consistent with in vitro results performed on RAW macrophages. Further, the Mig-PMO NPs exhibited a prolonged antidiabetic effect by lowering/controlling the blood glucose levels of diabetic rats over a 10 h period as compared to a 2 h sustained effect from free miglitol. The antidiabetic effect was positively correlated with inhibition of intestinal alpha-glucosidase enzyme. |