title: Ethyl cellulose nanoparticles: clarithomycin encapsulation and eradication of H. pylori.
abstract: The extreme acidic environment of the stomach, its regular voidance of contents and the restricted access to the mucus covered habitat combined with the antibiotic resistance of the bacteria, all contribute to the poor success in the treatment of Helicobacter pylori gastric infections. Here, we demonstrate that by encapsulating clarithromycin into ethyl cellulose (EC) nanoparticles, the efficiency of H. pylori clearance in C57BL/6 mice infected with these bacteria was significantly improved. Clarithomycin-loaded EC nanoparticles were prepared via a simple yet effective anti-solvent particle induction method, to yield sub-micron sized particles with 22.3 ± 0.17% (w/w) clarithromycin loading at 86 ± 0.5% (w/w) encapsulation efficiency. The particles dispersed well in water and simulated gastric fluid and gave a minimum inhibitory concentration of 0.09-0.18 μg/ml against four strains of H. pylori. Encapsulation into EC particles not only enhanced the anti-adhesion activity of clarithromycin when tested with H. pylori and Hep-2 cells, but also gave significant enhancement of H. pylori clearance in the stomach of C57BL/6 mice infected with the bacteria.
authors.affiliation: Program in Biotechnology, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
authors.forename: Porntip
authors.initials: P
authors.lastname: Pan-In
authors.affiliation: Department of Pathology, Faculty of Veterinary Science, Chulalongkorn University, Bangkok 10330, Thailand.
authors.forename: Wijit
authors.initials: W
authors.lastname: Banlunara
authors.affiliation: Innovation Center for Research and Development of Medical Diagnostic Technology Project, Department of Transfusion Medicine, Faculty of Allied Health Sciences, Chulalongkorn University, Bangkok 10330, Thailand.
authors.forename: Nuntaree
authors.initials: N
authors.lastname: Chaichanawongsaroj
authors.affiliation: Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand; Nanotec-CU Center of Excellence on Food and Agriculture, Bangkok 10330, Thailand. Electronic address: psupason@chula.ac.th.
authors.forename: Supason
authors.initials: S
authors.lastname: Wanichwecharungruang
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry; D001422:Bacterial Adhesion / Q000187:drug effects; D045744:Cell Line, Tumor; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D017291:Clarithromycin / Q000008:administration & dosage* / Q000737:chemistry; D005260:Female; D016481:Helicobacter Infections / Q000188:drug therapy* / Q000382:microbiology; D016480:Helicobacter pylori / Q000187:drug effects; D008297:Male; D008810:Mice, Inbred C57BL; D008826:Microbial Sensitivity Tests; D053769:Nanocapsules / Q000008:administration & dosage* / Q000737:chemistry; D013270:Stomach / Q000382:microbiology / Q000473:pathology
chemical_list: D000900:Anti-Bacterial Agents; D053769:Nanocapsules; C013517:ethyl cellulose; D002482:Cellulose; D017291:Clarithromycin
keywords: Anti-adhesion; Clarithromycin; Encapsulation; Ethyl cellulose; Helicobacter pylori