ROS-Responsive and active targeted drug delivery based on conjugated polymer nanoparticles for synergistic chemo-/photodynamic therapy

Stimuli-responsive and active targeted drug release is highly significant and challenging for precise and effective cancer therapy. Herein, a reactive oxygen species (ROS)-responsive drug delivery system iRGD-BDOX@CPNs with active targeting for chemo-/photodynamic (PDT) synergistic therapy has been reported. This nanocarrier iRGD-BDOX@CPNs is constructed by the self-assembly of conjugated polymer poly(fluorene-co-vinylene) (PFV), prodrug BDOX (doxorubicin modified with a phenylboronic acid ester group) and an amphiphilic polymer (DSPE-PEG) modified with internalized RGD (DSPE-PEG-iRGD). The hydrophobic inner cores formed by PFV main chains tightly enclose BDOX. Due to PFV generating many ROS by light triggering, the BDOX prodrug can be in situ activated, resulting in the highly efficient drug release. In addition, the remarkable fluorescence recovery could be used for real-time monitoring of drug delivery and guiding antitumor therapy. Contributing to the specific recognition between iRGD and integrin αvβ3 receptors over-expressed on the surface of tumor cells, the active targeting and uptake of iRGD-BDOX@CPNs in tumor cells are greatly enhanced. The prominent anti-cancer effect of iRGD-BDOX@CPNs is realized by targeted drug delivery and synergistic therapeutic effects of PDT/chemotherapy. This study illustrates that the development of ROS-responsive and targeted drug delivery nanocarriers iRGD-BDOX@CPNs provides a new insight for controllable drug release and tumor precision therapy.