多功能纳米粒子，集成准确的多诊断和高效的治疗，在肿瘤治疗学方面具有巨大的前景。然而，为实现成像引导下的肿瘤有效根治，开发多功能纳米粒子仍然是一项具有挑战性的任务。本文通过将2,6-二碘-二吡咯甲烷（2,6-diiodo-BODIPY）与氮杂硼-双吡咯甲烷（Aza-BODIPY）偶联，开发了近红外（NIR）有机荧光剂Aza/I-BDP。通过包覆一个两性亲水的生物相容性共聚物DSPE-mPEG5000，制备了均匀分布的Aza/I-BDP纳米粒子（NPs），其表现出了高1O2产生率、高光热转换效率和出色的光稳定性。值得注意的是，Aza/I-BDP和DSPE-mPEG5000的共聚组装有效抑制了Aza/I-BDP在水溶液中的H聚集，并将亮度同时增强了31倍。更重要的是，体内实验证明，Aza/I-BDP NPs可以用于近红外荧光和光声成像引导下的光动力和光热治疗。

Multifunctional nanoparticles integrating accurate multi-diagnosis and efficient therapy hold great prospects in tumor theranostics. However, it is still a challenging task to develop multifunctional nanoparticles for imaging-guided effective eradication of tumors. Herein, we developed a near-infrared (NIR) organic agent Aza/I-BDP by coupling 2,6-diiodo-dipyrromethene (2,6-diiodo-BODIPY) with aza-boron-dipyrromethene (Aza-BODIPY). Through encapsulating with an amphiphilic biocompatible copolymer DSPE-mPEG5000, well-distributed Aza/I-BDP nanoparticles (NPs) were developed, which exhibited high 1O2 generation, high photothermal conversion efficiency, and excellent photo-stability. Notably, coassembly of Aza/I-BDP and DSPE-mPEG5000 effectively inhibits H-aggregation of Aza/I-BDP in aqueous solution and enhances the brightness simultaneously up to 31-fold. More importantly, in vivo experiments demonstrated that Aza/I-BDP NPs might be used for NIR fluorescent and photoacoustic imaging-guided photodynamic and photothermal therapy.