Delivering amoxicillin at the infection site - a rational design through lipid nanoparticles

• Type: Article in International Scientific Journal
• Date: 2019

Authors

Lopes de Campos, D (Author) Other; Pinto, RM (Author) Other; Costa Lima, SAC (Author) Other; Santos, T (Author) Other; Sarmento, B (Author) Other; Nunes, C (Author) Other; Salette Reis (Author) FFUP

Journal

Title: International Journal of Nanomedicine

Vol. 14

Pages: 2781-2795

ISSN: 1176-9114

Publisher: Dove Medical Press

Indexing

ISI Web of Knowledge - 11 Citations

Scopus - 13 Citations

Other information

Authenticus ID: P-00Q-GE4

DOI: 10.2147/ijn.s193992

Abstract (EN): Purpose: Amoxicillin is a commonly used antibiotic, although degraded by the acidic pH of the stomach. This is an important limitation for the treatment of Helicobacter pylori infections. The purpose of this work was to encapsulate amoxicillin in lipid nanoparticles, increasing the retention time at the site of infection (gastric mucosa), while protecting the drug from the harsh conditions of the stomach lumen. Materials and methods: The nanoparticles were produced by the double emulsion technique and optimized by a three -level Box-Behnken design. Tween 80 and linolenic acid were used as potential therapeutic adjuvants and dioleoylphosphatidylethanolamine as a targeting agent to Helicobacter pylori. Nanoparticles were characterized regarding their physico-chemical features, their storage stability, and their usability for oral administration (assessment of in vitro release, in vitro cell viability, permeability, and interaction with mucins). Results: The nanoparticles were stable for at least 6 months at 4 degrees C. In vitro release studies revealed a high resistance to harsh conditions, including acidic pH and physiologic temperature. The nanoparticles have a low cytotoxicity effect in both fibroblasts and gastric cell lines, and they have the potential to be retained at the gastric mucosa. Conclusion: Overall, the designed formulations present suitable physico-chemical features for being henceforward used by oral administration to treat Helicobacter pylori infections.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 15