Efficacy and safety of nanoparticles of glibenclamide and organomodified layered double hydroxides in diabetics rats

Glibenclamide (GB) is an important drug in the treatment of type II diabetes mellitus (DM II); however, its low solubility causes variability in its oral bioavailability, negatively affecting the pharmacological treatment. Nanoparticles (NP) of GB and organophilized Layered Double Hydroxide (LDH) were developed to improve oral bioavailability and tested in streptozotocin-induced diabetic rats to evaluate therapeutic efficacy and safety. Blood glucose was measured for 12 h or after 28 days of treatment. In addition, body weight, water and feed consumption, hematological, biochemistry and morphological parameters and markers of oxidative stress were determined. After the treatment, GB with LDH normalized the blood glucose level, indicating a better release profile. Water and feed intake and body weight of animals treated with GB and GB with LDH were closer to the normoglycemic group and did not indicate signs of toxicity of the nanoparticles. The biochemical, hematological and histological results also showed no significant changes related to nanotoxicity. The combination of GB with LDH proved to be critical in the oxidative balance, as it reduced the oxidative stress of vascular tissue. In conclusion, NPs are a potential controlled release system for the treatment of DM II.

Automated summary

Glibenclamide nanoparticles combined with organophilized Layered Double Hydroxide were developed to improve the oral bioavailability of glibenclamide and showed potential as a controlled release system for the treatment of type II diabetes mellitus. The combination effectively normalized blood glucose levels without causing toxicity, and also improved the oxidative balance of vascular tissue.