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Theranostics 2016; 6(5):679-687. doi:10.7150/thno.14556

Research Paper

Cisplatin Prodrug-Conjugated Gold Nanocluster for Fluorescence Imaging and Targeted Therapy of the Breast Cancer

Fangyuan Zhou^1,2*, Bing Feng^1*, Haijun Yu^1✉, Dangge Wang¹, Tingting Wang¹, Jianping Liu¹, Qingshuo Meng¹, Siling Wang^2✉, Pengcheng Zhang¹, Zhiwen Zhang¹, Yaping Li^1✉

1. State Key Laboratory of Drug Research & Center of Pharmaceutics, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;
2. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
* Equal contribution to this study.

Abstract

Theranostic nanomedicine has emerged as a promising modality for cancer diagnosis and treatment. In this study, we report the fabrication of fluorescence gold nanoclusters (GNC) conjugated with a cisplatin prodrug and folic acid (FA) (FA-GNC-Pt) for fluorescence imaging and targeted chemotherapy of breast cancer. The physio-chemical properties of FA-GNC-Pt nanoparticles are thoroughly characterized by fluorescence/UV-Vis spectroscopic measurement, particle size and zeta-potential examination. We find that FA-modification significantly accelerated the cellular uptake and increased the cytotoxicity of GNC-Pt nanoparticles in murine 4T1 breast cancer cells. Fluorescence imaging in vivo using 4T1 tumor bearing nude mouse model shows that FA-GNC-Pt nanoparticles selectively accumulate in the orthotopic 4T1 tumor and generate strong fluorescence signal due to the tumor targeting effect of FA. Moreover, we demonstrate that FA-GNC-Pt nanoparticles significantly inhibit the growth and lung metastasis of the orthotopically implanted 4T1 breast tumors. All these data imply a good potential of the GNC-based theranostic nanoplatform for fluorescence tumor imaging and cancer therapy.

Keywords: Theranostic Nanomedicine, Gold Nanoclusters, Fluorescence Imaging, Targeted Therapy.