Formulation and In-vitro Evaluation of pH-Sensitive Oil Entrapped Polymeric Blend Amoxicillin Beads for the Eradication of Helicobacter pylori

Abstract

Oral pH sensitive drug delivery systems are of utmost importance as these systems deliver the drug at specific part of the gastrointestine (GI) as per the pH of GI, resulting in improved patient therapeutic efficacy and compliance. The pH range of fluids in various segments of the GI tract may provide environmental stimuli for drug release. The aim of this study was to design buoyant beads containing amoxicillin (Am) and to evaluate its potential for the eradication of Helicobacter pylori (H. pylori). The gel bead of gellan, wherein the oil was entrapped, was blended with hydroxypropyl methyl cellulose or Carbopol 934. Buoyant beads of gellan were prepared through ionotropic gellation technique to achieve the controlled and pH-sensitive drug release in stomach. The effects of processing variables such as particle size, buoyancy, percent encapsulation efficiency and in-vitro antimicrobial activity were evaluated. Thescanning electron micrograph indicated that prepared beads were spherical in shape and all the beads showed satisfactory floating efficiency in the phthalate buffer solution. The diameter of the gel beads was increased through raising the gellan gum and calcium carbonate concentration. The formulation exhibited sustained release profile and was best fitted in the Peppas model with n< 0.45. Subsequent coating of microbeads exhibited zero-order sustained pattern of the drug release up to 8 h. In-vitro growth inhibition study showed complete eradication of the isolated H. pylori strain .These results provide evidence that the optimized formulation bearing antibiotics like amoxicillin should be useful in H. pylori treatment.