Low cytotoxicity of solid lipid nanoparticles in in vitro and ex vivo lung models

Inhal Toxicol. 2009 Jul:21 Suppl 1:104-9. doi: 10.1080/08958370903005769.

Abstract

The aim of this study was to investigate the potential cytotoxicity of solid lipid nanoparticles (SLN) for human lung as a suitable drug delivery system (DDS). Therefore we used a human alveolar epithelial cell line (A549) and murine precision-cut lung slices (PCLS) to estimate the tolerable doses of these particles for lung cells. A549 cells (in vitro) and precision-cut lung slices (ex vivo) were incubated with SLN20 (20% phospholipids in the lipid matrix of the particles) and SLN50 (50% phospholipids in the lipid matrix of the particles) in increasing concentrations. The cytotoxic effects of SLN were evaluated in vitro by lactate dehydrogenase (LDH) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Vitality of lung slices was controlled by staining with calcein AM/ethidium homodimer 1 using confocal laser scanning microscopy and followed by quantitative image analysis with IMARIS software. A549 cell line revealed a middle effective concentration (EC(50)) for MTT assay for SLN20 of 4080 microg/ml and for SLN50 of 1520 microg/ml. The cytotoxicity in terms of LDH release showed comparable EC(50) values of 3431 microg/ml and 1253 microg/ml for SLN20 and SLN50, respectively. However, in PCLS we determined only SLN50 cytotoxic values with a concentration of 1500 microg/ml. The lung slices seem to be a more sensitive test system. SLN20 showed lower toxic values in all test systems. Therefore we conclude that SLN20 could be used as a suitable DDS for the lung, from a toxicological point of view.

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Drug Carriers*
  • Female
  • Humans
  • Image Processing, Computer-Assisted
  • Inhibitory Concentration 50
  • L-Lactate Dehydrogenase / metabolism
  • Lung / drug effects*
  • Lung / pathology
  • Mice
  • Mice, Inbred BALB C
  • Microscopy, Confocal
  • Nanoparticles / toxicity*
  • Phospholipids / toxicity*
  • Risk Assessment
  • Tissue Culture Techniques
  • Toxicity Tests*

Substances

  • Drug Carriers
  • Phospholipids
  • L-Lactate Dehydrogenase