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Phenanthriplatin (IV) Conjugated Multifunctional Up-Converting Nanoparticles for Drug Delivery and Biomedical Imaging

Abstract

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 side-effects, lack of selectivity, fast blood clearance, 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. Upconversion luminescent NaGdF4:Yb3+/Er3+ nanoparticles (UCNPs) were further modified with polyethyleneimine (PEI), poly (ethylene glycol) (PEG) and 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 exhibit 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 nanocomposite 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 confirm that the Phen-Pt(IV)-conjugated nanoparticles have relatively high tumor inhibition rate. These results indicate that the multifunctional nanoparticles are expected to be a platform for simultaneous imaging and cancer therapeutic applications.

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Supplementary files

Publication details

The article was received on 20 Apr 2018, accepted on 11 Jul 2018 and first published on 13 Jul 2018


Article type: Paper
DOI: 10.1039/C8TB01034J
Citation: J. Mater. Chem. B, 2018, Accepted Manuscript
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    Phenanthriplatin (IV) Conjugated Multifunctional Up-Converting Nanoparticles for Drug Delivery and Biomedical Imaging

    B. Teng, Y. Han, X. Zhang, H. Xiao, C. Yu, H. Li, Z. Cheng, D. Jin, P. Ma, K. L. Wong and J. Lin, J. Mater. Chem. B, 2018, Accepted Manuscript , DOI: 10.1039/C8TB01034J

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