Effects of transferrin conjugated multi-walled carbon nanotubes in lung cancer delivery

Mater Sci Eng C Mater Biol Appl. 2016 Oct 1:67:313-325. doi: 10.1016/j.msec.2016.05.013. Epub 2016 May 7.

Abstract

The aim of this study was to develop multi-walled carbon nanotubes (MWCNT) which were covalently conjugated with transferrin by carbodiimide chemistry and loaded with docetaxel as a model drug for effective treatment of lung cancer in comparison with the commercial docetaxel injection (Docel™). d-Alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) was used as amphiphilic surfactant to improve the aqueous dispersity and biocompatibility of MWCNT. Human lung cancer cells (A549 cells) were employed as an in-vitro model to access cellular uptake, cytotoxicity, cellular apoptosis, cell cycle analysis, and reactive oxygen species (ROS) of the docetaxel/coumarin-6 loaded MWCNT. The cellular uptake results of transferrin conjugated MWCNT showed higher efficiency in comparison with free C6. The IC50 values demonstrated that the transferrin conjugated MWCNT could be 136-fold more efficient than Docel™ after 24h treatment with the A549 cells. Flow cytometry analysis confirmed that cancerous cells appeared significantly (P<0.05) in the sub-G1 phase for transferrin conjugated MWCNT in comparison with Docel™. Results of transferrin conjugated MWCNT have showed better efficacy with safety than Docel™.

Keywords: Docetaxel; Endocytosis; Lung cancer; Nanomedicine; Safety; Transferrin conjugation.

MeSH terms

  • A549 Cells
  • Animals
  • Apoptosis / drug effects
  • Bronchoalveolar Lavage Fluid
  • Cell Cycle / drug effects
  • Coumarins / chemistry
  • Docetaxel
  • Drug Delivery Systems / methods*
  • Drug Liberation
  • Endocytosis / drug effects
  • Flow Cytometry
  • Humans
  • Intracellular Space / metabolism
  • Lung / drug effects
  • Lung / pathology
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / pathology
  • Microscopy, Atomic Force
  • Nanotubes, Carbon / chemistry*
  • Nanotubes, Carbon / ultrastructure
  • Particle Size
  • Rats
  • Reactive Oxygen Species / metabolism
  • Spectroscopy, Fourier Transform Infrared
  • Staining and Labeling
  • Static Electricity
  • Taxoids / pharmacology
  • Taxoids / therapeutic use
  • Thiazoles / chemistry
  • Transferrin / metabolism*

Substances

  • Coumarins
  • Nanotubes, Carbon
  • Reactive Oxygen Species
  • Taxoids
  • Thiazoles
  • Transferrin
  • coumarin 6
  • Docetaxel