A Small-Molecule Diketopyrrolopyrrole-Based Dye for in vivo NIR-IIa Fluorescence Bioimaging

Organic small-molecule fluorophores with near-infrared IIa (NIR-IIa) emission have great potential in pre-clinical detection and inoperative imaging due to the high-spatial resolution and deep penetration. However, developments of the NIR-IIa fluorophores are still facing considerable challenges. In this work, a series of diketopyrrolopyrrole (DPP)-based fluorophores were designed and synthesized. Subsequently, nanomaterial T25@F127 with significant NIR-IIa emission properties was rationally prepared by encapsulating DPP-based fluorophore T25, and was selected for fluorescence angiography and cerebral vascular microscopic imaging with nearly 800 mu m penetrating depth and excellent signal-background ratio of 4.07 and 2.26 (at 250 and 400 mu m), respectively. Furthermore, the nanomaterial T25@cRGD with tumor targeting ability can image tiny metastatic tumor on intestine with a small size of 0.3 mmx1.0 mm and high-spatial resolution (SBR=3.84). This study demonstrates that the nanomaterials which encapsulated T25 behave as excellent NIR-IIa fluorescence imaging agents and have a great potential for in vivo biological application.