Development of Cefuroxime Axetil Nanoporous Microsponge for Prolonged Gastric Retention and Targeted Helicobacter pylori Treatment

Introduction: To develop a gastric-floating microsponge formulation of Cefuroxime Axetil (CFA) aimed at increasing the gastric residence time of the drug and enhancing eradication of Helicobacter pylori infection. Methods: CFA microsponges were prepared by a quasi-emulsion technique. The formulations were evaluated for production yield, drug content, entrapment efficiency, in vitro buoyancy, and drug release profile. The optimized microsponge (highest entrapment, sustained floatation, and prolonged in vitro drug release) was selected for further characterization using Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), and X-Ray Diffraction (XRD). In vivo gastric retention was assessed in Wistar albino rats via X-ray imaging. In vitro antimicrobial efficacy was tested in H. pylori cultures to determine the Minimum Inhibitory Concentration (MIC) and duration of action. Results: The optimized microsponge formulation achieved a production yield of 82.09% ± 0.075 with high entrapment efficiency (100% ± 4.05). It showed excellent in vitro buoyancy (> 8 hours) and sustained drug release over 12 hours. SEM revealed spherical microsponges with a nanoporous surface, while DSC and XRD confirmed the molecular dispersion of cefuroxime axetil. In vivo X-ray imaging demonstrated gastric retention for up to 6 h. The microsponge showed an MIC of 1 μg/mL against H. pylori, compared with 0.5 μg/mL for the pure drug. Discussion: High entrapment efficiency and sustained buoyancy support effective gastroretentive formulation performance. Nanoporous morphology and amorphous drug dispersion explain the controlled release behavior. Prolonged gastric retention indicates suitability for localized gastric delivery. Despite a slightly higher MIC, the microsponge provided prolonged antibacterial activity (96 hours) compared with the pure drug (48 hours), highlighting the benefit of sustained local drug exposure. Conclusion: The optimized gastric-floating microsponge formulation of CFA offers extended gastric retention (6 hours), sustained release, and prolonged antimicrobial activity against H. pylori. This system has strong potential for improved eradication of H. pylori infections.