Real‐Time In Vivo Hepatotoxicity Monitoring through Chromophore‐Conjugated Photon‐Upconverting Nanoprobes

Abstract

Abstract Drug toxicity is a long‐standing concern of modern medicine. A typical anti‐pain/fever drug paracetamol often causes hepatotoxicity due to peroxynitrite ONOO − . Conventional blood tests fail to offer real‐time unambiguous visualization of such hepatotoxicity in vivo. Here we report a luminescent approach to evaluate acute hepatotoxicity in vivo by chromophore‐conjugated upconversion nanoparticles. Upon injection, these nanoprobes mainly accumulate in the liver and the luminescence of nanoparticles remains suppressed owing to energy transfer to the chromophore. ONOO − can readily bleach the chromophore and thus recover the luminescence, the presence of ONOO − in the liver leads to fast restoring of the near‐infrared emission. Taking advantages of the high tissue‐penetration capability of near‐infrared excitation/emission, these nanoprobes achieve real‐time monitoring of hepatotoxicity in living animals, thereby providing a convenient screening strategy for assessing hepatotoxicity of synthetic drugs.