Enhancing singlet oxygen generation in semiconducting polymer nanoparticles through fluorescence resonance energy transfer for tumor treatment

Abstract

Photosensitizers (PSs) are of particular importance for efficient photodynamic therapy (PDT). Challenges for PSs simultaneously possessing strong light-absorbing ability, high ¹O₂ generation by effective intersystem crossing from the singlet to the triplet state, good water-solubility and excellent photostability still exist. Reported here are a new kind of dual-emissive semiconducting polymer nanoparticles (SPNs) containing fluorescent BODIPY derivatives and near-infrared (NIR) phosphorescent iridium(iii) complexes. In the SPNs, the BODIPY units serve as the energy donors in the fluorescence resonance energy transfer (FRET) process for enhancing the light absorption of the SPNs. The NIR emissive iridium(iii) complexes are chosen as the energy acceptors and efficient photosensitizers. The ionized semiconducting polymers can easily self-assemble to form hydrophilic nanoparticles and homogeneously disperse in aqueous solution. Meanwhile, the conjugated backbone of SPNs provides effective shielding for the two luminophores from photobleaching. Thus, an excellent overall performance of the SPN-based PSs has been realized and the high ¹O₂ yield (0.97) resulting from the synergistic effect of BODIPY units and iridium(iii) complexes through the FRET process is among the best reported for PSs. In addition, owing to the phosphorescence quenching of iridium(iii) complexes caused by ³O₂, the SPNs can also be utilized for O₂ mapping <i>in vitro</i> and <i>in vivo</i>, which assists in the evaluation of the PDT process and provides important instructions in early-stage cancer diagnosis.