Enhancement of cytotoxicity of artemisinin toward cancer cells by transferrin-mediated carbon nanotubes nanoparticles

Abstract

Artemisinin (ART) is a kind of drug with an endoperoxide bridge which tends to react with Fe²⁺ to generate radicals for killing cancer cells. However, simultaneous delivery of hydrophobic ART and Fe²⁺ ions into cancer cells remains a major challenge. In this study, a multi-functional tumor-targeting drug delivery system employing hyaluronic acid-derivatized multi-walled carbon nanotubes (HA-MWCNTs) as drug carriers, transferrin (Tf) as targeting ligand and ART as a model drug for cancer treatment was constructed. This delivery system (HA-MWCNTs/Tf@ART) not only retained optical property of MWCNTs and cytotoxicity of ART but also demonstrated synergistic anti-tumor effect using ART and Tf. Compared with free ART, remarkably enhanced anti-tumor efficacy of this drug vehicle was realized both in cultured MCF-7 cells in vitro and in a tumor-bearing murine model in vivo, due to increased intracellular accumulation of ART and co-delivery of Tf and ART analogs. HA-MWCNTs/Tf@ART with laser irradiation demonstrated the highest inhibition effect compared to the other groups. This result may provide a new way of using promising natural drugs for cancer therapy.

• Chinese herb artemisinin
• co-delivery of Tf and ART
• reactive oxygen species
• tumor-targeting

Declaration of interest

The authors declare no conflicts of interest in relation to this work.

This work was supported by grants from the National Natural Science Foundation of China (No. 81273451 and 81101684).