Abstract

The lack of sensitive detection techniques and agents for early-stage tumors, which are characterized by small size, juvenile blood vessels and scarce secreted markers, has hampered timely cancer therapy and human well-being. Herein, the natural product pyropheophorbide-a (PPa) and FDA-approved Pluronic F127 are organized to develop F127–PPa nanomicelles with favorable size, red-shifted fluorescence and decent biocompatibility. After intravenous (i.v.) injection, the F127–PPa nanomicelles could not only accurately identify early-stage xenografted tumors, but also sensitively detect cancer metastasis in lungs through near-infrared (NIR) fluorescence imaging. The fluorescence signals are consistent with radionuclide imaging, photoacoustic (PA) imaging and bioluminescence imaging of tumors, consolidating the reliability of using F127–PPa nanomicelles for sensitive cancer diagnosis in a non-invasive and low-cost manner. Moreover, the fluorescence intensity of small tumors is linearly correlated with the tumoral mass ranging from 10 to 120 mg with a fluorescence coefficient of 4.5 × 107 mg−1. Under the guidance of multimodal imaging, the tumors could be thoroughly eradicated by F127–PPa under laser irradiation due to efficient reactive oxygen species (ROS) generation. These findings may provide clinically translatable agents and strategies for sensitive diagnosis of early-stage tumors and timely cancer therapy.