Design of One-for-All Near-Infrared Aggregation-Induced Emission Nanoaggregates for Boosting Theranostic Efficacy

Fluorescence-guided phototherapy, including photodynamic and photothermal therapy, is considered an emerging noninvasive strategy for cancer treatments. Organic molecules are promising theranostic agents because of their facile construction, simple modification, and good biocompatibility. Organic systems that integrated multifunctionalities in a single component and achieved high efficiency in both imaging and therapies are rarely reported as the inherently competitive energy relaxation pathways are hard to modulate, and fluorescence quenching occurs upon molecular aggregation. Herein, a versatile theranostic platform with near-infrared emission, high fluorescence quantum yield, robust reactive oxygen species production, and excellent photothermal conversion efficiency was developed based on an aggregation-induced emission luminogen, namely, TPA-TBT. In vivo studies revealed that the TPA-TBT nanoaggregates exhibit outstanding photodynamic and photothermal therapy efficacy to ablate tumors inoculated in a mouse model. This work offers a design strategy to develop one-for-all cancer theranostic agents by modulating and utilizing the relaxation energy of excitons in full.

Automated summary

Fluorescence-guided phototherapy is an emerging noninvasive cancer treatment strategy. Organic molecules, with their easy construction, simple modification, and good biocompatibility, have shown promise as theranostic agents. This study successfully developed a versatile theranostic platform based on an aggregation-induced emission luminogen, TPA-TBT, which exhibited near-infrared emission, high fluorescence quantum yield, robust reactive oxygen species production, and excellent photothermal conversion efficiency. In vivo studies demonstrated its outstanding efficacy in both photodynamic and photothermal therapies against tumors in a mouse model. This work provides a design strategy for developing all-in-one cancer theranostic agents by modulating and utilizing the relaxation energy of excitons.