Influence of surface charge on the potential toxicity of PLGA nanoparticles towards Calu-3 cells

Simona Mura^1,2, Herve Hillaireau^1,2, Julien Nicolas^1,2, Benjamin Le Droumaguet^1,2, Claire Gueutin^1,2, Sandrine Zanna³, Nicolas Tsapis^1,2, Elias Fattal^1,2
1Univ Paris-Sud, UMR 8612, Châtenay Malabry, F-92296; ²CNRS, Châtenay Malabry, F-92296; ³Laboratoire de Physico-Chimie des Surfaces, CNRS-ENSCP (UMR 7045), Ecole Nationale Superiore de Chimie de Paris, France

Background: Because of the described hazards related to inhalation of manufactured nanoparticles, we investigated the lung toxicity of biodegradable poly (lactide-co-glycolide) (PLGA) nanoparticles displaying various surface properties on human bronchial Calu-3 cells.
Methods: Positively and negatively charged as well as neutral nanoparticles were tailored by coating their surface with chitosan, Poloxamer, or poly (vinyl alcohol), respectively. Nanoparticles were characterized in terms of size, zeta potential, and surface chemical composition, confirming modifications provided by hydrophilic polymers.
Results: Although nanoparticle internalization by lung cells was clearly demonstrated, the cytotoxicity of the nanoparticles was very limited, with an absence of inflammatory response, regardless of the surface properties of the PLGA nanoparticles.
Conclusion: These in vitro results highlight the safety of biodegradable PLGA nanoparticles in the bronchial epithelium and provide initial data on their potential effects and the risks associated with their use as nanomedicines.

Keywords: nanoparticles, PLGA, surface properties, Calu-3, toxicity, inflammation