Theranostics 2012; 2(8):757-768. doi:10.7150/thno.4756

Research Paper

Gold Nanorods Conjugated with Doxorubicin and cRGD for Combined Anticancer Drug Delivery and PET Imaging

Yuling Xiao1, Hao Hong2,3, Vyara Z. Matson4, Alireza Javadi1, Wenjin Xu1, Yunan Yang2, Yin Zhang3, Jonathan W. Engle3, Robert J. Nickles2,3, Weibo Cai2,3✉, Douglas A. Steeber4, Shaoqin Gong1 ✉

1. Department of Biomedical Engineering and Wisconsin Institutes for Discovery, University of Wisconsin-Madison, Madison, WI 53706, USA;
2. Department of Radiology, University of Wisconsin-Madison, Madison, WI 53705, USA;
3. Department of Medical Physics, University of Wisconsin-Madison, Madison, WI 53705, USA;
4. Department of Biological Sciences, University of Wisconsin-Milwaukee, Milwaukee, WI 53211, USA.


A multifunctional gold nanorod (GNR)-based nanoplatform for targeted anticancer drug delivery and positron emission tomography (PET) imaging of tumors was developed and characterized. An anti-cancer drug (i.e., doxorubicin (DOX)) was covalently conjugated onto PEGylated (PEG: polyethylene glycol) GNR nanocarriers via a hydrazone bond to achieve pH-sensitive controlled drug release. Tumor-targeting ligands (i.e., the cyclo(Arg-Gly-Asp-D-Phe-Cys) peptides, cRGD) and 64Cu-chelators (i.e., 1,4,7-triazacyclononane-N, N', N''-triacetic acid (NOTA)) were conjugated onto the distal ends of the PEG arms to achieve active tumor-targeting and PET imaging, respectively. Based on flow cytometry analysis, cRGD-conjugated nanocarriers (i.e., GNR-DOX-cRGD) exhibited a higher cellular uptake and cytotoxicity than non-targeted ones (i.e., GNR-DOX) in vitro. However, GNR-DOX-cRGD and GNR-DOX nanocarriers had similar in vivo biodistribution according to in vivo PET imaging and biodistribution studies. Due to the unique optical properties of GNRs, this multifunctional GNR-based nanoplatform can potentially be optimized for combined cancer therapies (chemotherapy and photothermal therapy) and multimodality imaging (PET, optical, X-ray computed tomography (CT), etc.).

Keywords: Gold nanorod (GNR), drug delivery, nanoparticles, cancer, positron emission tomography (PET), cRGD peptide, tumor targeting

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How to cite this article:
Xiao Y, Hong H, Matson VZ, Javadi A, Xu W, Yang Y, Zhang Y, Engle JW, Nickles RJ, Cai W, Steeber DA, Gong S. Gold Nanorods Conjugated with Doxorubicin and cRGD for Combined Anticancer Drug Delivery and PET Imaging. Theranostics 2012; 2(8):757-768. doi:10.7150/thno.4756. Available from