Abstract | PURPOSE: 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.
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Authors | Saad Hassani, Saad Hasani, Yann Pellequer, Alf Lamprecht |
Journal | Pharmaceutical research
(Pharm Res)
Vol. 26
Issue 5
Pg. 1149-54
(May 2009)
ISSN: 1573-904X [Electronic] United States |
PMID | 19205850
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Drug Carriers
- Fluorescent Dyes
- Polystyrenes
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Topics |
- Animals
- Drug Carriers
(administration & dosage, chemistry, pharmacokinetics, therapeutic use)
- Fluorescent Dyes
- Gastric Mucosa
(metabolism)
- Helicobacter Infections
(drug therapy)
- Helicobacter pylori
(drug effects)
- Male
- Mice
- Nanoparticles
(administration & dosage, chemistry, therapeutic use)
- Particle Size
- Polystyrenes
- Stomach
(pathology)
- Stomach Ulcer
(drug therapy, pathology)
- Tissue Distribution
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