title: 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 Fe(2+) to generate radicals for killing cancer cells. However, simultaneous delivery of hydrophobic ART and Fe(2+) 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.
authors.affiliation: School of Pharmaceutical Sciences, Zhengzhou University , Zhengzhou , China and.
authors.forename: Huijuan
authors.initials: H
authors.lastname: Zhang
authors.forename: Yandan
authors.initials: Y
authors.lastname: Ji
authors.forename: Qianqian
authors.initials: Q
authors.lastname: Chen
authors.forename: Xiaojing
authors.initials: X
authors.lastname: Jiao
authors.forename: Lin
authors.initials: L
authors.lastname: Hou
authors.forename: Xiali
authors.initials: X
authors.lastname: Zhu
authors.forename: Zhenzhong
authors.initials: Z
authors.lastname: Zhang
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D037621:Artemisinins / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D053938:DNA Fragmentation / Q000187:drug effects; D004337:Drug Carriers / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D004357:Drug Synergism; D006801:Humans; D006820:Hyaluronic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D061986:MCF-7 Cells; D051379:Mice; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D037742:Nanotubes, Carbon / Q000737:chemistry*; D017382:Reactive Oxygen Species / Q000378:metabolism; D014168:Transferrin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D023041:Xenograft Model Antitumor Assays
chemical_list: D037621:Artemisinins; D004337:Drug Carriers; D037742:Nanotubes, Carbon; D017382:Reactive Oxygen Species; D014168:Transferrin; D006820:Hyaluronic Acid; C031327:artemisinin
keywords: Chinese herb artemisinin; co-delivery of Tf and ART; reactive oxygen species; tumor-targeting