Three‐Pronged Attack by Homologous Far‐red/NIR AIEgens to Achieve 1+1+1>3 Synergistic Enhanced Photodynamic Therapy

Abstract

Photodynamic therapy (PDT) has long been shown to be a powerful therapeutic modality for cancer. However, PDT is undiversified and has become stereotyped in recent years. Exploration of distinctive PDT methods is thus highly in demand but remains a severe challenge. Herein, an unprecedented 1+1+1>3 synergistic strategy is proposed and validated for the first time. Three homologous luminogens with aggregation‐induced emission (AIE) characteristics were rationally designed based on a simple backbone. Through slight structural tuning, these far‐red/near‐infrared AIE luminogens are capable of specifically anchoring to mitochondria, cell membrane, and lysosome, and effectively generating reactive oxygen species (ROS). Notably, biological studies demonstrated combined usage of three AIE photosensitizers gives multiple ROS sources simultaneously derived from several organelles, which gives superior therapeutic effect than that from a single organelle at the same photosensitizers concentration. This strategy is conceptually and operationally simple, providing an innovative approach and renewed awareness of improving therapeutic effect through three‐pronged PDT.

Controllable and Diversiform Topological Morphologies of Self‐Assembling Supra‐Amphiphiles with Aggregation‐Induced Emission Characteristics for Mimicking Light‐Harvesting Antenna

“…AIE refers to a unique phenomenon that some fluorophores are nonemissive or weakly emissive in the molecularly dissolved state but they emit intensively in aggregates due to the restriction of intramolecular motions (RIM). [ 29–33 ] Ascribe to their intrinsic advantages including bright emission in aggregates, high photobleaching threshold, and high signal‐to‐noise ratio, AIE luminogens (AIEgens) represent a class of extraordinary alternatives for constructing luminescent supramolecular materials. The utilization of AIEgens not only straightforwardly provides valuable insights in mechanistic understanding of supramolecular chemistry, but also powerfully functionalizes supramolecular materials with efficient fluorescence, making AIEgens‐based supramolecular materials highly useful in sensing, bioimaging, and optoelectronic devices.…”

Aggregation‐enhanced theranostics: AIE sparkles in biomedical field

“…[ 58,59 ] For instance, lots of AIE PSs have been reported to exhibit much higher ROS generation efficiency than the renowned PS Rose Bengal (RB). [ 22,44,82 ] Additionally, as hydrophobic organic molecules naturally aggregate in aqueous medium and are usually utilized in theranostics in the form of NPs, AIEgens offer the unique opportunity to form nanoaggregates or NPs with high emission brightness and efficient ROS production. Most attractively, AIE NPs display almost linear loading‐dependent increase in both brightness and ROS generation efficiency, which is essentially distinct from ACQ PSs‐based NPs that exhibit compromised brightness and photosensitization at high loading density [60] .…”

Aggregation‐Induced Emission Luminogens Married to 2D Black Phosphorus Nanosheets for Highly Efficient Multimodal Theranostics

“…[ 22–24 ] Additionally, it has been demonstrated that AIEgens can generally produce ROS efficiently in aggregates, enabling their application of high‐performance FLI‐guided PDT. [ 25–30 ] Although the emergence of AIE PSs has indeed triggered state‐of‐the‐art development of FLI‐guided PDT with initial success in the past few years, some major problems have yet to be solved. For instance, it is difficult to simultaneously achieve effective ROS generation and strong emission with long wavelength; [ 31,32 ] furthermore, combining well‐performed AIE PSs with functional nanomaterial to improve their versatility and to develop novel multifunctional theranostic nanoplatform for advanced anticancer therapeutics is urgently needed.…”