Title:Development of a Berberine Loaded Multifunctional Design for the Treatment of Helicobacter pylori Induced Gastric Ulcer
VOLUME: 9 ISSUE: 1
Author(s):Sunil K. Jain*, Kamlesh Patel, Kuldeep Rajpoot and Akhlesh Jain
Affiliation:Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur (C.G.) 495 009, Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur (C.G.) 495 009, Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur (C.G.) 495 009, Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur (C.G.) 495 009
Keywords:H. pylori, berberine hydrochloride, polymethylmethacrylate, polyethylene oxide, Concanavalin-A, microspheres.
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.
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.
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.
