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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Acknowledgements
Alf Lamprecht is grateful to the “Institut Universitaire de France” for the financial support. The project was co-financed by the Region of Franche-Comté (grant VJ000610).
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An erratum to this article can be found at http://dx.doi.org/10.1007/s11095-009-9872-8
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Hasani, S., Pellequer, Y. & Lamprecht, A. Selective Adhesion of Nanoparticles to Inflamed Tissue in Gastric Ulcers. Pharm Res 26, 1149–1154 (2009). https://doi.org/10.1007/s11095-009-9834-1
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DOI: https://doi.org/10.1007/s11095-009-9834-1