PT  - JOURNAL ARTICLE
AU  - Maria Luisa Bondì
AU  - Maria Ferraro
AU  - Serena Di Vincenzo
AU  - Stefania Gerbino
AU  - Gennara Cavallaro
AU  - Gaetano Giammona
AU  - Mark Gjomarkaj
AU  - Elisabetta Pace
TI  - Nanostructured lipid carriers as drug delivery systems for fluticasone propionate: Effects in cigarette smoke stimulated bronchial epithelial cells
DP  - 2013 Sep 01
TA  - European Respiratory Journal
PG  - 223
VI  - 42
IP  - Suppl 57
4099  - http://erj.ersjournals.com/content/42/Suppl_57/223.short
4100  - http://erj.ersjournals.com/content/42/Suppl_57/223.full
SO  - Eur Respir J2013 Sep 01; 42
AB  - Cigarette smoke extracts (CSE) alter TLR4 expression and activation and increase intracellular oxidative stress contributing to reduced corticosteroid activity. Nanotechnological approaches have considerable potential for the treatment of airway diseases. This manuscript describes the preparation and characterization of fluticasone propionate (FP) entrapped into nanostructured lipid carriers (NLC) and tests their biocompatibility and the efficacy in a human bronchial epithelial cell line (16-HBE) stimulated with cigarette smoke extracts (CSE). The obtained nanoparticles were characterized by means of dynamic light scattering, surface charge and storage stability. The amount of entrapped FP into NLC was evaluated by HPLC analysis and the biocompatibility and efficacy of the FP-loaded NLC was assessed testing cell necrosis, cell apoptosis, intracellular reactive oxygen species (ROS) production, total gluthatione (GSH), TLR4 expression in CSE stimulated 16-HBE. Empty-NLC or FP-loaded NLC did not induce cell necrosis (propidium positive cells) or cell apoptosis (Annexin V positive/propidium negative cells). CSE increased intracellular ROS production and TLR4 expression in bronchial epithelial cells. Free FP was not able to significantly reduce these CSE mediated effects in bronchial epithelial while FP-loaded NLC were more effective in reducing these CSE mediated effects and in increasing GSH levels in comparison with free FP.In conclusion, the present study provides compelling evidences that NLC may be considered a promising strategy to improve corticosteroid mediated effects in cellular models associated to corticosteroid resistance.