Saad Hassani1, Saad Hasani, Yann Pellequer, Alf Lamprecht. 1. Laboratory of Pharmaceutical Engineering (EA3924), School of Medicine and Pharmacy, University of Franche-Comté, Place Saint Jacques, 25000, Besançon, France.
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.
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.
Authors: Marlene A Lopes; Bárbara Abrahim-Vieira; Claudia Oliveira; Pedro Fonte; Alessandra M T Souza; Tammy Lira; Joana A D Sequeira; Carlos R Rodrigues; Lúcio M Cabral; Bruno Sarmento; Raquel Seiça; Francisco Veiga; António J Ribeiro Journal: Int J Nanomedicine Date: 2015-09-18
Authors: Daniela Lopes-de-Campos; Rita M Pinto; Sofia A Costa Lima; Tiago Santos; Bruno Sarmento; Cláudia Nunes; Salette Reis Journal: Int J Nanomedicine Date: 2019-04-23