الفهرس | Only 14 pages are availabe for public view |
Abstract This study aimed to explore the possibility of developing glibenclamide (GLC) loaded nanosponges by complexation with β-cyclodextrin, which offers advantages of extended drug release and improved oral bioavailability. Blank nanosponges were developed by linking β-cyclodextrin monomers together using the crosslinker carbonyl-diimidazole (CDI) at various molar ratios (1:2, 1:3, 1:4, 1:6, and 1:8). The solubility study was carried out to determine the appropriate ratio of maximal solubilization extent before loading GLC. Different physicochemical characterizations were performed. Pharmacokinetic, pharmacodynamic, and histological evaluations were performed in rats. Results demonstrated that GLC: NS1:4 has the highest solubility (46.36 ± 2.44 %) and loading efficiency (36.1 ± 0.57 %) with optimum particle size (352±6.1nm) and zeta potential (˗25.3 ± –0.3mV). The in vivo studies showed a significant decrease in blood glucose level (69.6%) with rapid onset and extended-release effect over 24 hrs. These results show the improvement of oral bioavailability and prolonged drug release, which will help achieve patient compliance with long-term diabetes treatment. Keywords: Glibenclamide, nanosponges, cyclodextrins, diabetes mellitus, and extended release. |