Photodynamic therapy (PDT) has been gaining popularity in both scientific research and clinic applications due to its non-invasiveness and spatiotemporal targeting properties. Nevertheless, the local hypoxic microenvironment in tumor tissue impedes PDT universality. To overcome this drawback, a 2-pyridone-bearing BODIPY photosensitizer was synthesized rationally and introduced to polyethyleneglycol-b-poly(aspartic acid) to form a photosensitizer-1O2generation, storage/release agent dual-loading system (PEG-b-PAsp-BODIPY). The investigation of the PDT effect at different illumination conditions in vitroand in vivorevealed that the system tremendously inhibited tumor proliferation, indicating that this new PEG-b-PAsp-BODIPY could act as a potentially effective photo therapeutic system for cancer therapeutics.