Fabrication of pantoprazole-loaded microsphere clusters with enteric and mucoadhesive properties for enhanced ulcer...

The present study aimed to formulate and evaluate, both in vitro and in vivo, enteric-coated mucoadhesive microspheres of pantoprazole using xanthan gum and Eudragit L100-55 in order to protect pantoprazole from gastric acid degradation and to create a temporary drug reservoir in the gastrointestinal tract, thereby achieving enhanced targeting. The goal was to assess their potential in preventing ketorolac-induced gastric ulcers in rats. Various formulations of pantoprazole microspheres were prepared and developed via an extrusion method using ionotropic gelation and dip coating. The formulations were evaluated for encapsulation efficiency, particle size, mucoadhesive properties, swelling percentage, resistance to gastric acid, and drug release over six hours in vitro. The optimized formulation (10 mg/kg) was subsequently tested in vivo on rats with ketorolac-induced (30 mg/kg) gastric ulcers, and the gastric tissue was examined for histopathological changes. The formulation containing 1% xanthan gum showed the highest drug release (80% w/w) and suitable loading (77.58% w/w), with a swelling index of 50.84% w/w, average particle size of 1.19 mm, an adhesion strength of 2.71 ± 0.87 N per 0.1 g and was fully resistant to acidic conditions. In vivo, it prevented gastric ulcers as effectively as the marketed product and, unlike the marketed product, also prevented vascular rupture in all ketorolac-induced ulcer rats. The optimized formulation performed well, suggesting its potential as an oral delivery alternative.