title: Selective adhesion of nanoparticles to inflamed tissue in gastric ulcers.
abstract: OBJECTIVE
  Gastrointestinal deposition of nanoparticles was examined after oral administration to mice suffering from an experimental gastric ulcer model. Local drug delivery could reduce side effects and would be a distinct improvement compared to existing therapeutic approaches, e.g. in the local therapy of Helicobacter pylori.
  
  
  METHODS
  A gastric ulcer was induced to Swiss mice by acetic acid injection. Fluorescent polystyrene particles with a nominal size of 50, 200, and 750 nm were administered orally for 3 or 5 days and particle adhesion in the gastrointestinal tract analyzed.
  
  
  RESULTS
  In the ulcerated regions, an enhanced particle adhesion was observed compared to healthy controls. A size dependency of the deposition was found which further increased with a prolonged treatment period. For 750 nm particles only fair adhesion was observed (control, 2.0 +/- 1.4%; ulcer, 4.5 +/- 0.7% of daily administered particle mass), while already 200 nm particles showed higher binding (control, 2.9 +/- 1.3%; ulcer, 7.8 +/- 1.2%). Highest relative adhesion was found for 50 nm particles (control, 2.8 +/- 1.3%; ulcer, 10.0 +/- 1.5%). The targeting index of gastric ulcer versus healthy control was nearly constant around 2 after 3 days treatment, but increased distinctly for smaller particles after 5 days.
  
  
  CONCLUSIONS
  The use of sub-micron sized carriers holds promise for the targeted delivery of drugs to the ulcerated mucosal areas in the stomach.
authors.affiliation: Laboratory of Pharmaceutical Engineering (EA3924), School of Medicine and Pharmacy, University of Franche-Comté, Place Saint Jacques, 25000, Besançon, France.
authors.forename: Saad
authors.initials: S
authors.lastname: Hassani
authors.forename: Saad
authors.initials: S
authors.lastname: Hasani
authors.forename: Yann
authors.initials: Y
authors.lastname: Pellequer
authors.forename: Alf
authors.initials: A
authors.lastname: Lamprecht
mesh_terms: D000818:Animals; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D005456:Fluorescent Dyes; D005753:Gastric Mucosa / Q000378:metabolism*; D016481:Helicobacter Infections / Q000188:drug therapy*; D016480:Helicobacter pylori / Q000187:drug effects*; D008297:Male; D051379:Mice; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry / Q000627:therapeutic use; D010316:Particle Size; D011137:Polystyrenes; D013270:Stomach / Q000473:pathology; D013276:Stomach Ulcer / Q000188:drug therapy* / Q000473:pathology; D014018:Tissue Distribution
chemical_list: D004337:Drug Carriers; D005456:Fluorescent Dyes; D011137:Polystyrenes