Theranostics 2013; 3(9):633-649. doi:10.7150/thno.6630

Research Paper

Multifunctional Gold Nanostar Conjugates for Tumor Imaging and Combined Photothermal and Chemo-therapy

Haiyan Chen 1*, Xin Zhang 1*, Shuhang Dai3, Yuxiang Ma1, Sisi Cui 1, Samuel Achilefu2✉, Yueqing Gu1✉

1. Department of Biomedical Engineering, State Key Laboratory of Natural Medicines and School of Life Science and Technology, China Pharmaceutical University, 24 Tongjia Lane, Gulou District, Nanjing 210009, China
2. Department of Radiology, School of Medicine, Washington University, St. Louis , Missouri, United States
3. Department of Pharmaceutical Science, School of Pharmacy, China Pharmaceutical University, 24 Tongjia Lane, Gulou District, Nanjing 210009, China
* Haiyan Chen and Xin Zhang contributed equally to the work.

Abstract

Uniform gold nanostars (Au NS) were conjugated with cyclic RGD (cRGD) and near infrared (NIR) fluorescence probe (MPA) or anti-cancer drug (DOX) to obtain multi-functional nanoconstructs, Au-cRGD-MPA and Au-cRGD-DOX respectively. The NIR contrast agent Au-cRGD-MPA was shown to have low cytotoxicity. Using tumor cells and tumor bearing mice, these imaging nanoparticles demonstrated favorable tumor-targeting capability mediated by RGD peptide binding to its over-expressed receptor on the tumor cells. The multi-therapeutic analogue, Au-cRGD-DOX, integrates targeting tumor, chemotherapy and photo-thermotherapy into a single system. The synergistic effect of photo-thermal therapy and chemotherapy was demonstrated in different tumor cell lines and in vivo using S180 tumor-bearing mouse models. The viability of MDA-MB-231 cells was only 40 % after incubation with Au-cRGD-DOX and irradiation with NIR light. Both tail vein and intratumoral injections showed Au-cRGD-DOX treated mice exhibiting the slowest tumor increase. These results indicate that the multifunctional nanoconstruct is a promising combined therapeutic agent for tumor-targeting treatment, with the potential to enhance the anti-cancer treatment outcomes.

Keywords: gold nanostar, tumor-targeting, RGD receptor, near infrared imaging, photo-thermal therapy.

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How to cite this article:
Chen H, Zhang X, Dai S, Ma Y, Cui S, Achilefu S, Gu Y. Multifunctional Gold Nanostar Conjugates for Tumor Imaging and Combined Photothermal and Chemo-therapy. Theranostics 2013; 3(9):633-649. doi:10.7150/thno.6630. Available from http://www.thno.org/v03p0633.htm