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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 (ie, 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 (ie, the cyclo (Arg-Gly-Asp-D-Phe-Cys) peptides, cRGD) and 64 Cu-chelators (ie, 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 (ie, GNR-DOX-cRGD) exhibited a higher cellular uptake and cytotoxicity than non-targeted ones (ie, GNR-DOX) in vitro. However, GNR-DOX-cRGD and GNR-DOX nanocarriers …