Genipin-cross-linked fucose–chitosan/heparin nanoparticles for the eradication of Helicobacter pylori

• Published in: Biomaterials Vol. 34; no. 18; pp. 4466 - 4479
• Main Authors: Lin, Yu-Hsin, Tsai, Shih-Chang, Lai, Chih-Ho, Lee, Che-Hsin, He, Zih Sian, Tseng, Guan-Chin
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier Ltd 01.06.2013
• Subjects: Advanced Basic Science; Amoxicillin - pharmacology; Amoxicillin - therapeutic use; Animals; Cell Line; Cell Survival - drug effects; Chitosan - chemistry; Chitosan - pharmacology; Coculture Techniques; Cross-Linking Reagents - chemistry; Cross-Linking Reagents - pharmacology; Dentistry; Fluorescent Antibody Technique; Fucose - chemistry; Fucose - pharmacology; Fucose-conjugated chitosan; Gastric inflammation; Genipin-cross-linked nanoparticles; Helicobacter Infections - drug therapy; Helicobacter Infections - microbiology; Helicobacter pylori; Helicobacter pylori - drug effects; Helicobacter pylori - growth & development; Helicobacter pylori - ultrastructure; Heparin - pharmacology; Humans; Hydrogen-Ion Concentration; Infected animal model; Iridoids - chemistry; Iridoids - pharmacology; Male; Mice; Mice, Inbred C57BL; Microbial Sensitivity Tests; Nanoparticles - chemistry; Nanoparticles - ultrastructure; Particle Size; Spectroscopy, Fourier Transform Infrared; Static Electricity; Genipin-cross-linked nanoparticles; Gastric inflammation; Infected animal model; Helicobacter pylori; Fucose-conjugated chitosan
• ISSN: 0142-9612; 1878-5905
• DOI: 10.1016/j.biomaterials.2013.02.028

Abstract Helicobacter pylori is a significant human pathogen that recognizes specific carbohydrate receptors, such as the fucose receptor, and produces the vacuolating cytotoxin, which induces inflammatory responses and modulates the cell–cell junction integrity of the gastric epithelium. The clinical applicability of topical antimicrobial agents was needed to complete the eradication of H. pylori in the infected fundal area. In the present study, we combined fucose-conjugated chitosan and genipin-cross-linking technologies in preparing multifunctional genipin-cross-linked fucose–chitosan/heparin nanoparticles to encapsulate amoxicillin of targeting and directly make contact with the region of microorganism on the gastric epithelium. The results show that the nanoparticles effectively reduced drug release at gastric acids and then released amoxicillin in an H. pylori survival situation to inhibit H. pylori growth and reduce disruption of the cell–cell junction protein in areas of H. pylori infection. Furthermore, with amoxicillin-loaded nanoparticles, a more complete H. pylori clearance effect was observed, and H. pylori –associated gastric inflammation in an infected animal model was effectively reduced.