I型光敏剂(PS)的低氧依赖性使其成为治疗实体瘤的流行选择。然而,水溶性差的缺点,短发射波长,稳定性差,无法区分癌细胞和正常细胞限制了大多数I型PSs在临床治疗中的应用。因此,开发新型I型PSs来克服这些问题是一项紧迫但具有挑战性的任务。在这里,通过利用阴离子-π+相互作用的独特结构特征,首次制备了具有聚集诱导发射(AIE)特征和近红外(NIR)发射的高水溶性I型PS(DPBC-Br)。DPBC-Br显示出显着的水溶性(7.3mM)和出色的耐光漂白性,通过NIR-I成像,以无洗和长期跟踪的方式实现肿瘤细胞和正常细胞之间的有效和精确区分。此外,由DPBC-Br产生的优异的I型活性氧(ROS)在体外提供对癌细胞的特异性杀伤和在体内抑制肿瘤生长,全身毒性可忽略不计。本研究合理地构建了一种高水溶性的I型PS,与传统的纳米粒子配方程序相比,具有更高的可靠性和可控性,为临床癌症治疗提供了巨大的潜力。
The low oxygen dependence of type I photosensitizers (PSs) has made them a popular choice for treating solid tumors. However, the drawbacks of poor water solubility, short emission wavelength, poor stability, and inability to distinguish cancer cells from normal cells limit the application of most type I PSs in clinical therapy. Thereby, developing novel type I PSs for overcoming these problems is an urgent but challenging task. Herein, by utilizing the distinctive structural characteristics of anion-π+ interactions, a highly water-soluble type I PS (DPBC-Br) with aggregation-induced emission (AIE) characteristic and near-infrared (NIR) emission is fabricated for the first time. DPBC-Br displays remarkable water solubility (7.3 mM) and outstanding photobleaching resistance, enabling efficient and precise differentiation between tumor cells and normal cells in a wash-free and long-term tracking manner via NIR-I imaging. Additionally, the superior type I reactive oxygen species (ROS) produced by DPBC-Br provide both specific killing of cancer cells in vitro and inhibition of tumor growth in vivo, with negligible systemic toxicity. This study rationally constructs a highly water-soluble type I PS, which has higher reliability and controllability compared with conventional nanoparticle formulating procedures, offering great potential for clinical cancer treatment.