Floating-bioadhesive microspheres containing acetohydroxamic acid for clearance of Helicobacter pylori.

ABSTRACT

A new strategy based on gastric retention is proposed for the treatment of Helicobacter pylori. (H. pylori). A synergism between a floating and a bioadhesive system has been explored. Floating microspheres containing the antiurease drug acetohydroxamic acid (AHA) were prepared by a novel quasi-emulsion solvent diffusion method. The microballons were characterized for size distribution, morphology, drug content, drug release, and in vitro floating property. The microballons were coated with 2% w/v solution of polycarbophil by the air suspension coating method. The bioadhesive property of the microspheres was investigated by the detachment force measurement method. In vitro growth inhibition studies were performed in isolated H. pylori culture. The results suggest that AHA-loaded floating microspheres are superior as potent urease inhibitors whereas urease plays an important role in the colonization of H. pylori. We suggest that an oral dosage containing floating-bioadhesive microspheres may form a useful drug delivery system for the treatment of H. pylori.