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The development of semiconducting polymers (SPs) with simultaneous second near‐infrared (NIR‐II) absorption and multimodal phototheranostic functions is highly desired in the field of oncotherapy. Aggregation‐induced emission luminogens (AIEgens) have been acknowledged to possess unique potential in integrating multiple diagnostic and therapeutic modalities into one organic molecule. Nevertheless, SPs are hard to achieve AIE activity due to their extended π‐conjugated skeletons as well as the large and planar configuration of commonly‐used electrophilic acceptor moieties. Herein, an ingenious acceptor dimerization‐based acceptor distortion strategy is proposed in current work by taking advantage of the sterically encumbered acceptors with large and planar structure for the successful construction of AIE‐active SPs. Through further finely adjusting the molecular donor–acceptor interaction strength, one of the obtained AIE‐active SPs named SP3 bearing the highest intramolecular charge transfer effect presented desired NIR‐II absorption and aggregation‐induced NIR‐II fluorescence emission, good reactive oxygen species production ability, as well as superior photothermal conversion performance. Accordingly, SP3 is selected to fabricate into nanoparticles and successfully applied in the NIR‐II laser‐triggered fluorescence‐photoacoustic imaging‐guided photodynamic‐photothermal therapy of tumors. This study represents the first NIR‐II excitable AIE‐active SP, and offers a new perspective on designing advanced multimodal phototheranostic polymers for efficient treatment of malignant tumor. [ABSTRACT FROM AUTHOR]

Construction of versatile nanotemplate bearing inherent distinctive functions and prominent drug‐carrying capability is an appealing yet significantly challenging task. Here, inspired by the guiding role of surfactant in preparing nanoparticles, an amphiphilic aggregation‐induced emission (AIE) photosensitizer, namely MeOTTVP, is synthesized with attractive near‐infrared (NIR) emission and high‐performance reactive oxygen species production, and followed by dual‐templating‐assisted one‐pot method involving MeOTTVP as the skeleton to fabricate organosilica nanoparticles (AIE‐ONs). The presented AIE‐ONs perfectly inherit the functions of MeOTTVP, and are also capable of loading antibiotics and anticancer drugs. Doxorubicin can be assembled on AIE‐ONs and then capped with hyaluronic acid, endowing the resulting hybrid with NIR fluorescence imaging‐guided synergetic photodynamic/chemotherapy performance, thereby offering boosted anticancer efficacy and reduced side effects. Furthermore, by loading antibiotic rifampicin, the newly obtained AIE‐ONs integrating chemo‐photodynamic antibacterial functions provide broad‐spectrum antibacterial activity and fluorescence monitoring behavior. This study thus not only offers a promising strategy to fabricate NIR nanoparticles on a large scale, but also provides useful insights into designing an advanced theranostic protocol for treating both cancer and bacterial infections. [ABSTRACT FROM AUTHOR]

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]

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]