Phenanthriplatin(iv) conjugated multifunctional up-converting nanoparticles for drug delivery and biomedical imaging

Bo Teng, Yanqiu Han*, Xinyang Zhang, Haihua Xiao, Chang Yu, Hejie Li, Ziyong Cheng, Dayong Jin, Ka-Leung WONG, Ping'An Ma, Jun Lin

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

37 Citations (Scopus)


Platinum-based drugs cisplatin, carboplatin, and oxaliplatin are widely used in the clinical treatment of cancer. However, the clinical applications of platinum-based drugs are greatly limited by the side-effects, lack of selectivity, fast blood clearance, and intrinsic or acquired drug resistance. In this study, we report an anticancer drug delivery system based on phenanthriplatin(iv) (Phen-Pt(iv))-conjugated NaGdF4:Yb3+/Er3+ nanoparticles. The upconversion luminescent NaGdF4:Yb3+/Er3+ nanoparticles (UCNPs) were further modified with polyethyleneimine (PEI), poly(ethylene glycol) (PEG) and the cancer targeting ligand arginine-glycine-aspartic peptide (RGD), resulting in the formation of water-dispersible and biologically functionalized UCNP@PEI-Phen-Pt-PEG-RGD nanoparticles. The Phen-Pt-conjugated UCNP@PEI-Phen-Pt-PEG-RGD nanoparticles exhibited an obvious cytotoxic effect on Hep-2 cells (Human Laryngeal Carcinoma cell line) via MTT assay. Meanwhile, the endocytosis process of Phen-Pt-conjugated NaGdF4:Yb3+/Er3+ nanoparticles by Hep-2 cells was demonstrated through flow cytometry and ICP-MS. In addition, the upconversion luminescence image of UCNP@PEI-Phen-Pt-PEG-RGD taken up by cells shows green emission under 980 nm infrared laser excitation, making the UCNP@PEI-Phen-Pt-PEG-RGD nanocomposites promising candidates as bioimaging agents. Moreover, these UCNPs were further explored for in vitro and in vivo T1-weighted magnetic resonance (MR) imaging. The in vivo experiments on mice also confirmed that the Phen-Pt(iv)-conjugated nanoparticles have a relatively high tumor inhibition rate. These results indicate that the multifunctional nanoparticles can be expected to be a platform for simultaneous imaging and cancer therapeutic applications.

Original languageEnglish
Pages (from-to)5059-5068
Number of pages10
JournalJournal of Materials Chemistry B
Issue number31
Publication statusPublished - 2018

Scopus Subject Areas

  • Chemistry(all)
  • Biomedical Engineering
  • Materials Science(all)


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