Development of a Berberine Loaded Multifunctional Design for the Treatment of Helicobacter pylori Induced Gastric Ulcer

Abstract

Background and Objective: The H. pylori infection causes chronic inflammation and significantly increases the risk of developing duodenal and gastric ulcer disease and gastric cancer. Infection with H. pylori is the well-known risk factor for gastric cancer. It is highly desirable to develop a delivery system that localizes the antibiotic at the site of infection to achieve bactericidal concentration for a longer period of time. Thus, present work aimed to develop Concanavalin-A (Con-A) conjugated gastro-retentive microspheres of polymethylmethacrylate (PMMA) and polyethylene oxide (PEO) containing berberine hydrochloride (BBR) for the treatment of H. pylori infection. </P><P> Methods: Microspheres were prepared by solvent evaporation method and characterized by particles size distribution, surface morphology, % drug entrapment and in vitro drug release in the simulated gastric fluid. Optimized microspheres were conjugated with Con-A and further characterized for Con-A conjugation efficiency, in vitro drug release and ex vivo mucoadhesive properties. </P><P> Results and Conclusion: Enhanced mucoadhesion (88±1.9%) was shown by Con-A conjugated microspheres as compared with non-conjugated microspheres (14.5±3.6%). This significant difference (p<0.05) in the mucoadhesion may be due to affinity of the Con-A towards glycoproteins of mucus membrane of stomach. Attachment of lectin (Con-A) to the microspheres significantly enhanced the mucoadhesiveness as well as also controlled the berberine release for 10 h study period. The preliminary results from this study advised that Con-A conjugated PMMA and PEO microspheres could be used to incorporate some more herbal drugs and may be used for oral administration against H. pylori in the stomach.

Development and Evaluation of Cholestyramine-Amoxicillin Trihydrate-Loaded Gastro-Retentive Microspheres for Attaining Extended Therapeutic Effect Against H. Pylori Infection

“…In addition, this strategy has also been utilized to enhance bioavailability of drugs and attaining a steeper concentration gradient (by using relatively lesser drug), which usually improve performance of drug by maintaining its concentration in the given therapeutic window (i.e., minimum effective concentration (MEC)≤therapeutic window≥ maximum safe concentration (MSC)). Furthermore, such kind of systems may decrease some undesirable toxic effects due to sitespecific (mucoadhesive property) delivery of drug, which restricts unnecessary distribution of drug to other tissues/organs [7,8].…”