Combining imaging and drug delivery of "theranostic" nanoparticles has enabled concurrent diagnosis and therapy of diseases. Here, we describe a novel theranostic system that combines two imaging tracers, Perfluorooctyl Bromide (PFOB) for (19)F magnetic resonance imaging (MRI) and Indocyanine Green (ICG) for near infrared (NIR) imaging, with the chemotherapeutic agent Doxorubicin (Dox) into poly (lactic-co-glycolic acid)- poly (ethylene-glycol)-Folate (PLGA-PEG-Folate) nanoparticles. Cell culture studies using flow cytometry, confocal laser scanning microscope imaging, and (19)F MRI showed enhanced uptake of nanoparticles via folate receptors expressed on human nasopharyngeal epidermal carcinoma (KB) cells. In vivo, higher MRI and fluorescence signals were obtained from tumors with (19)F MRI and NIR, respectively, using folate-receptor-targeted nanoparticles compared with non-targeted equivalents. An in vitro cytotoxicity assay showed that folate-targeted nanoparticles were able to kill cancer cells more efficiently than non-folate conjugated particles. Our results suggest a potential use of PLGA-PEG-Folate PFOB/ICG/Dox nanoparticles as a targeted chemotherapy agent traceable by either (19)F MRI or NIR imaging.