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Vascular disruption agent (combretastatin A-4 phosphate) and phototherapeutic (IEICO-4F) assembled nanoparticles (IFC NPs) were prepared for the first time. The IFC NPs have a high photo energy utilization efficiency of up to 96.1%, and could significantly inhibit tumor growth by photodynamic and photothermal therapy enhanced tumor vascular disruption. [ABSTRACT FROM AUTHOR]

Near infrared (NIR) fluorescence imaging guided photodynamic therapy (PDT) is a technique which has been developed in many clinical trials due to its advantage of real-time optical monitoring, specific spatiotemporal selectivity, and minimal invasiveness. For this, photosensitizers with NIR fluorescence emission and high 1O2 generation quantum yield are highly desirable. Herein, we designed and synthesized a "donor–acceptor" (D-A) structured semiconductor polymer (SP), which was then wrapped with an amphiphilic compound (Pluronic ® F127) to prepare water-soluble nanoparticles (F-SP NPs). The obtained F-SP NPs exhibit good water solubility, excellent particle size stability, strong absorbance at deep red region, and strong NIR fluorescent emission characteristics. The maximal mass extinction coefficient and fluorescence quantum yield of these F-SPs were calculated to be 21.7 L/(g ⋅ cm) and 6.5%, respectively. Moreover, the 1O2 quantum yield of 89% for F-SP NPs has been achieved under 635 nm laser irradiation, which is higher than Methylene Blue, Ce6, and PpIX. The outstanding properties of these F-SP NPs originate from their unique D-A molecular characteristic. This work should help guide the design of novel semiconductor polymer for NIR fluorescent imaging guided PDT applications. [ABSTRACT FROM AUTHOR]

Imaging-guided photodynamic therapy (PDT) represents an advantage in cancer therapy because of its optically controlled selectivity, negligible side effects, and ability to monitor the therapeutic effect in situ in real time. However, the photosensitizers currently in use have poor water solubility and an inability to target tumors, whereas semiconductor quantum dots and metal-based complexes that have excellent water dispersity have the disadvantage of exerting a potential toxicity because of the heavy metals. Therefore, this work describes the preparation of the red fluorescent N,S-doped carbon dots (N,S-CDs) from a polythiophene derivate that generate singlet oxygen (1O2) with a quantum yield of ∼8% under light irradiation. Moreover, these CDs possess the ability to penetrate tumor cells and mainly accumulate into the lysosome and mitochondria, as well as excellent biocompatibility, chemostability, and a large Stokes shift (215 nm). Hence, the N,S-CDs may be used as a potential effective photosensitizer for imaging-guided PDT. [ABSTRACT FROM AUTHOR]

Image‐guided photodynamic therapy (PDT) has received growing attention due to its non‐invasiveness and precise controllability. However, the PDT efficiency of most photosensitizers are decreased in living system due to the aggregation‐caused singlet oxygen (1O2) generation decreasing. Herein, we present an Iridium (III) pyridylpyrrole complex (Ir‐1) featuring of aggregation‐induced emission (AIE) and 1O2 generation characteristics for image‐guided PDT of cancer. Ir‐1 aqueous solution exhibits bright red phosphorescence peaked at 630 nm, large Stokes shift of 227 nm, and good 1O2 generation ability. The 1O2 generating rate of Ir‐1 in EtOH/water mixture solution is 2.3 times higher than that of Rose Bengal. In vitro experimental results revealed that Ir‐1 has better biocompatibility and higher phototoxicity compared with clinically used photosensitizers (Rose Bengal and Ce6), suggesting that Ir‐1 can serve as a photosensitizer for image‐guided PDT of cancer. [ABSTRACT FROM AUTHOR]

• The state-of-the-art strategies to improve the 1O 2 quantum yield are summarized. • The advantages and disadvantages of these strategies are highlighted and compared. • The challenges and obstacles encountered in clinical PDT are discussed. Singlet oxygen (1O 2) generation is an essential function of photosensitizer (PS) as applied to photodynamic therapy (PDT) of cancer. As illustrated in the Jablonski diagram, the generation of 1O 2 is directly related to the process of intersystem crossing (ISC), in which a high ISC efficiency typically correlates with a high quantum yield (QY) of 1O 2. In recent years, multiple strategies have been adopted to improve ISC efficiency, including tuning chemical structures and reducing aggregation-caused quenching (ACQ), thus increase the 1O 2 QY of PS. Here, we systematically summarize and compare the advantages and disadvantages of these strategies through analysis of some representative examples. In addition, we also discuss the challenges and obstacles encountered in the development of PS with high 1O 2 generation efficiency and propose directions for future clinical applications of PDT. [ABSTRACT FROM AUTHOR]

This tutorial review summarizes the strategies for improving the efficacy of PDT in hypoxic tumor therapy. The advantages of combining PDT with other therapeutics, such as chemotherapy, chemodynamic therapy, gas therapy, immunotherapy and gene therapy, are also demonstrated. Finally, the existing challenges and future perspectives on clinical PDT for hypoxic tumors are discussed. [Display omitted] • Advanced materials and strategies for PDT to overcome hypoxia are classified. • Novel nano-systems in enhancing anti-tumor effects are summarized. • Combining PDT with other therapeutics to achieve synergetic effects are reported. • The current challenges and further opportunities are discussed. Photodynamic therapy (PDT) has been a preferred clinical technology for treating superficial tumors due to its advantages of high selectivity, non-invasiveness and negligible drug resistance. However, the hypoxic tumor microenvironment weakens the efficiency of O 2 -dependent PDT. Moreover, the PDT process consumes a large amount of O 2 and destroys the tumor blood vessels and further blocks the O 2 supply to tumor sites. Therefore, developing more advanced materials and methods for PDT of the hypoxic tumor is an essential scientific significance. This tutorial review summarizes the strategies for improving the efficacy of PDT in hypoxic tumor therapy, which is categorized into three sections: (I) enhancing O 2 concentration in the tumor; (II) disregarding hypoxia; and (III) exploiting hypoxia. The advantages of combining PDT with other therapeutics, such as chemotherapy, chemo-dynamic therapy, gas therapy, immunotherapy and gene therapy, are also demonstrated. Finally, the existing challenges and future perspectives on clinical PDT for hypoxic tumors are discussed. [ABSTRACT FROM AUTHOR]

In this review, we summarize the latest progress of research on CDs in phototherapy, including their use as nanocarriers for organic phototherapy agents, and highlight the strategies which are adopted to improve the therapeutic efficacy of CDs-based phototheranostics. Furthermore, we also discuss the challenges and prospects of the CDs-based phototheranostics towards clinical applications. • The latest progress of research on CDs in phototherapy is summarized. • The strategies which are adopted to improve the therapeutic efficacy of CDs-based phototheranostics are highlighted. • The challenges and prospects of the CDs-based phototheranostics towards clinical applications are discussed. Carbon dots (CDs) are novel zero-dimensional carbonaceous nanomaterial, and they are featured with an attractive combination of physical, chemical, and biomedical properties including wide absorption spectrum, tunable fluorescence, excellent water solubility, outstanding photostability, and biocompatibility, which leads to their diverse applications as optically functional materials in various fields, e.g., fluorescence sensing, bioimaging, and drug delivery. Recently, it was revealed that CDs could be used as an effective photosensitizer to generate reactive oxygen species under light excitation, and/or a photothermal agent to convert light energy into heat, which enable them to be applied in photodynamic therapy or photothermal therapy for cancer treatment. In this review, we summarize the latest progress of research on CDs in phototherapy, including their use as nanocarriers for organic phototherapy agents, and highlight the strategies which are adopted to improve the therapeutic efficacy of CDs-based phototheranostics. Furthermore, we also discuss the challenges and prospects of the CDs-based phototheranostics towards clinical applications. We hope this review will provide critical insights to inspire new exciting discoveries on CDs from both fundamental and practical views so as to prompt their advances in the phototherapy. [ABSTRACT FROM AUTHOR]

An A-D-A structured AIEgen based nanoparticles was designed for long-term imaging, and effective photodynamic therapy. The small ΔE ST of 0.227 eV make BTZPP NPs possess excellent 1O 2 generation ability, and the lysosome-targeted property further assist the treatment effect of PDT. [Display omitted] • A-D-A structured AIE photosensitizer (BTZPP) with small ΔE ST was designed. • BTZPP has large Stokes shift, deep red fluorescence and high 1O 2 quantum yield. • The lysosome targeted ability make BTZPP NPs kill cancer cells more effectively. • Imaging guided PDT of cancer was demonstrated. Photosensitizers (PSs) with aggregation-induced emission (AIE) feature show promising applications in fluorescence imaging-guided photodynamic therapy (PDT) in virtue of their enhanced fluorescence and phototoxicity in aggregate state. Seeking the ideal AIE luminogens (AIEgens) with good capability of generating reactive oxygen species is still urgent. Here we rationally synthesized an acceptor-donor-acceptor (A-D-A) structured AIEgen (BTZPP) and then prepared it into nanoparticles (NPs) through a simple re-precipitation procedure. The obtained BTZPP NPs show a deep-red emission peaked at 635 nm, a large Stokes shift of 195 nm, and a high 1O 2 generation quantum yield of 72.3%. Moreover, these NPs can selectively target lysosomes in live cells and image mouse tumor with a high contrast and long-term tracking (up to 14 days) capability. The high-efficiency imaging-guided PDT against cancer cells and tumors is successfully demonstrated in vitro and in vivo. [ABSTRACT FROM AUTHOR]