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Supramolecular approaches have opened up vast possibilities to construct versatile materials, especially those with stimuli‐responsiveness and integrated functionalities of multi‐modal diagnosis and synergistic therapeutics. In this study, a hybrid theranostic nanosystem named TTPY‐Py⊂CP5@AuNR is constructed via facile host–guest interactions, where TTPY‐Py is a photosensitizer with aggregation‐induced emission and CP5@AuNR represents the carboxylatopillar[5]arene (CP5)‐modified Au nanorods. TTPY‐Py⊂CP5@AuNR integrates the respective advantages of TTPY‐Py and CP5@AuNR such as the high performance of reactive oxygen species generation and photothermal conversion, and meanwhile shows fluorescence responses to both temperature and pH stimuli. The successful modification of CP5 macrocycles on AuNRs surfaces can eliminate the cytotoxicity of AuNRs and enable them to serve as the nanocarrier of TTPY‐Py for further theranostic applications. Significantly, in vitro and in vivo evaluations demonstrate that this supramolecular nanotheranostic system possesses multiple modalities including intensive fluorescence imaging (FLI), photoacoustic imaging (PAI), efficient photodynamic therapy (PDT), and photothermal therapy (PTT), indicating its great potential for FLI‐PAI imaging‐guided synergistic PDT‐PTT therapy. Moreover, TTPY‐Py can be released upon activation by the acidic environment of lysosomes and then specifically light up mitochondria. This study demonstrates a new strategy for the design of versatile nanotheranostics for accurate tumor imaging and cancer therapies. [ABSTRACT FROM AUTHOR]

The ingenious construction of versatile cancer phototheranostics involving fluorescence imaging (FLI) and photodynamic and photothermal therapies (PDT, PTT) concurrently has attracted great interest. By virtue of their inherent twisted structures and plentiful motion moieties, aggregation‐induced emission luminogens (AIEgens) have been proven to be perfect templates for the development of multimodal phototheranostic systems as their diverse energy consumption pathways can be flexibly regulated through tuning the intramolecular motions. Side‐chain engineering is generally accepted as a useful regulation strategy for intramolecular motions through altering the side‐chain structure of the molecule, but has rarely been reported for the construction of AIE‐active multimodal phototheranostics. Herein, by taking full advantage of the side‐chain engineering strategy, an AIE‐active multifunctional phototheranostic system (TBFT2 nanoparticles) is successfully constructed by intentionally manipulating the length of side chains. Bearing the longest alkyl chain, all of those three energy dissipation pathways including radiative decay, nonradiative thermal deactivation, and intersystem crossing process of TBFT2 are retained simultaneously and controllably in the aggregate state. In vitro and in vivo evaluations verify that TBFT2 nanoparticles perform well in terms of FLI‐guided PDT and PTT synergistic cancer therapy. This study thus provides new insight into the exploration of superior versatile phototheranostics through side‐chain engineering. [ABSTRACT FROM AUTHOR]

Fluorescence imaging in the second near‐infrared region (NIR‐II) can penetrate tissue at centimeter depths and obtain high image fidelity. However, facile synthesis of small‐molecule fluorescent photosensitizers for efficient NIR‐II fluorescence imaging as well as photodynamic and photothermal combinatorial therapies is still a challenging task. Herein, a rational design and facile synthesis protocol are reported for a series of novel NIR‐emissive zwitterionic luminogens with aggregation‐induced emission (AIE) features for cancer phototheranostics. Consistent with the intrinsic features including long emission wavelength, effective reactive oxygen species generation, and excellent photothermal conversion efficiency (35.76%), in vitro and in vivo evaluation show that one of these presented AIE luminogens provides excellent performance in NIR‐II fluorescence imaging‐guided synergistic phototherapy against cancer. [ABSTRACT FROM AUTHOR]