FORMULATION AND IN VITRO EVALUATION OF OIL ENTRAPPED BUOYANT BEADS FOR STOMACH SPECIFIC DELIVERY OF METRONIDAZOLE

Objective: This work focused on the development of floating alginate beads for stomach specific delivery of Metronidazole towards the effective eradication of Helicobacter pylori , a major causative agent of peptic ulcers. Methods: Different formulations of sunflower oil entrapped gel beads were prepared by emulsion gelation technique using sodium alginate as gelling agent. The prepared beads were evaluated for size, surface morphology, drug entrapment efficiency, in vitro floatuing and in vitro drug release properties. Results: It was found that the percentage of oil plays an important role in controlling the floating of oil-entrapped alginate beads. All batches of beads floated for >24 hours with a very short lag time of 151–187 seconds. Scanning electron microscopy (SEM) revealed that the beads were spherical in shape with small pores on the surface. SEM of the cross section of the beads demonstrated minute oil globules throughout the inner portion of the beads confirming oil entrapment. The results clearly indicated that amount of polymer (% w/v) and amount of sunflower oil (% v/v) affected the bead size, floating, encapsulation efficiency and drug release of the beads. It was observed that the drug release kinetics was best fitted with the Higuchi model and drug release from the polymer matrix system was non fickian (anomalous transport) type. Conclusion: The results provide evidence that formulated gel beads may be used to incorporate antimicrobials like Metronidazole and may be effective when administered locally in the stomach to cure Helicobacter pylori infection.