Assessment of the antidiabetic potentiality of glyburide loaded glyceryl monostearate solid lipid nanoparticles

Abstract

The high rate homogenisation techniques was used for preparing glyburide loaded glyceryl monostearate solid lipid nanoparticles (Glb-SLNs) to improve the drug's solubility and oral bioavailability. It was mediated through pseudo-ternary phase diagrams to optimize the surfactant/co-surfactant ratio. The optimized Glb-SLNs were characterized by FT-IR spectroscopy, DSC, powder X-ray diffraction study and SEM analysis. In rat skeletal muscle cells (L6 myocytes) and in streptozotocin and high-fat diet-induced diabetic rats, anti-diabetic activity was evaluated. Flow cytometry analysis has accessed the effects of glucose uptake performed by the 2-(N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl) amino)-2- deoxyglucose (2-NBDG) in L6 myotubes. In normal rats and diabetic rats, parameters such as the blood glucose level, serum insulin, serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), lipid peroxidase, catalase, glutathione, and HbA1c levels were assessed. Glb-SLNs at a dose of 50 μM showed a relative increase in relative fluorescence intensity of 92.5% to represent the glucose uptake potentiality. In vivo results revealed that the treatment with SLNs of glyburide (Glb-SLNs) normalized blood-glucose levels and serum biochemical parameters as compared with those of STZ controls. The protective effect was further confirmed by histopathological examination of the liver. These animals showed a comparable histopathological regeneration on Glb-SLNs treatment. These positive results demonstrated the success of the proposed SLNs approach in enhancing glyburide oral bioavailability and confirmed its potential as an effective system for diabetes treatment.