Transferrin modified graphene oxide for glioma-targeted drug delivery: In vitro and in vivo evaluations

Guodong Liu, He Shen, Jinning Mao, Liming Zhang, Zhen Jiang, Tao Sun, Qing Lan*, Zhijun Zhang

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

160 Citations (Scopus)


Transferrin (Tf), an iron-transporting serum glycoprotein that binds to receptors overexpressed at the surface of glioma cells, was chosen as the ligand to develop Tf-conjugated PEGylated nanoscaled graphene oxide (GO) for loading and glioma targeting delivery of anticancer drug doxorubicin (Dox) (Tf-PEG-GO-Dox). Tf-GO with lateral dimensions of 100-400 nm exhibited a Dox loading ratio up to 115.4%. Compared with Dox-loaded PEGylated GO (PEG-GO-Dox) and free Dox, Tf-PEG-GO-Dox displayed greater intracellular delivery efficiency and stronger cytotoxicity against C6 glioma cells. A competition test showed that Tf was essential to glioma targeting in vitro. The HPLC assay for Dox concentration in tumor tissue and contrapart tissue of the brain demonstrated that Tf-PEG-GO-Dox could deliver more Dox into tumor in vivo. The life span of tumor bearing rats after the administration of Tf-PEG-GO-Dox was extended significantly compared to the rats treated with saline, Dox, and PEG-GO-Dox. In conclusion, we developed Tf-PEG-GO-Dox which exhibited significantly improved therapeutic efficacy for glioma both in vitro and in vivo.

Original languageEnglish
Pages (from-to)6909-6914
Number of pages6
JournalACS Applied Materials and Interfaces
Issue number15
Publication statusPublished - 14 Aug 2013


  • chemotherapy
  • doxorubicin
  • glioma
  • graphene oxide
  • in vivo
  • transferrin


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