Abstract

Photodynamic therapy (PDT) is emerging as an excellent strategy to treat different types of cancers. The advantages of using PDT over other cancer treatment modalities are owing to its non-invasive nature, spatiotemporal precession, controllable photoactivity, and least side effects. The photosensitization ability of traditional photosensitizers (PSs) are severely curtailed by aggregation-induced quenching (ACQ). On the contrary, aggregation induced emission (AIE) molecules/fluorogens (AIEgens) show enhanced fluorescence emission and high reactive oxygen species (ROS)/singlet oxygen (1O2) production capability in the aggregated state. These unique characteristics of AIEgens make them potential AIE-PSs for fluorescence/luminescence image-guided combination PDT. In this chapter, we discussed the strategies that are developed to synthesize small molecule-based AIE-PSs, metal complex-based AIE-PSs, and AIE-PSs with two-photon absorbance (TPA) properties, polymer-based AIE-PSs, and nanoparticles based AIE-PSs for PDT. We have also discussed the rational design of targeting peptide conjugated AIE-PSs to selective target cancer cells over normal cells. Furthermore, recent findings on nanoparticle-based combination AIE-PSs are also discussed, where the combination AIE-PSs show synergistically improved anticancer activity and overcome the drug resistance. Finally, we shed light on the recent development, ongoing challenges, and future directions for designing better AIE-PS for PDT.

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