In vitro toxicity of cationic micelles and liposomes in cultured human hepatocyte (HepG2) and lung epithelial (A549) cell lines

Toxicol In Vitro. 2016 Oct:36:164-171. doi: 10.1016/j.tiv.2016.08.002. Epub 2016 Aug 3.

Abstract

The aim of this study was to compare the effects of cationic micelle and liposome drug delivery systems on liver and lung cells in a toxicological in vitro screening model, with observations on cytotoxicity and genotoxicity. A screening battery was established for assessment of a broad range of parameters related to adverse effects. Clear concentration response effects were observed related to impairment of mitochondrial function, membrane integrity and oxidative stress markers, but no effect was observed on genotoxicity. The adverse effects were highest for the liposomes. The High Content Screening seems optimal for initial screening of adverse effects, and combined with standard cytotoxicity measurements initial screening can be performed for predictive toxicological screening.

Keywords: Comet assay; Drug delivery systems; Hepatocytes; In vitro toxicology; Liposomes; Lung epithelial cells; Micelles; Nanomedicine.

MeSH terms

  • A549 Cells
  • Cell Survival / drug effects
  • Cholesterol / toxicity
  • Drug Delivery Systems
  • Epithelial Cells / drug effects*
  • Epithelial Cells / metabolism
  • Fatty Acids, Monounsaturated / toxicity
  • Hep G2 Cells
  • Hepatocytes / drug effects*
  • Humans
  • Interleukin-6 / metabolism
  • Liposomes / toxicity*
  • Lung / cytology
  • Micelles*
  • Polyethylene Glycols / toxicity
  • Polymethacrylic Acids / toxicity
  • Quaternary Ammonium Compounds / toxicity
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Fatty Acids, Monounsaturated
  • IL6 protein, human
  • Interleukin-6
  • Liposomes
  • Micelles
  • Polymethacrylic Acids
  • Quaternary Ammonium Compounds
  • Tumor Necrosis Factor-alpha
  • Polyethylene Glycols
  • Cholesterol
  • 1,2-dioleoyloxy-3-(trimethylammonium)propane