Abstract

A smart multitool platform for theranostics would be useful for monitoring the administration of therapies in vivo. However, the integration of multiple functions into a single small-molecule platform remains a challenge. In this study, we developed a multifunctional probe based on a small-molecule platform. The properties of this probe were investigated via hyperpolarized 129Xe NMR/MRI, fluorescence imaging in cells and in vivo, and photodynamic therapy (PDT) in tumor mouse models. This multifunctional probe shows good pH response across a broad range of pH values. It also exhibits excellent fluorescence in vivo for mapping its biodistribution. Additionally, it produces enough 1O2 radicals for in vivo PDT. The combination of these functionalities into a single small-molecule platform, rather than a bulky nanoconstruct, offers unique possibilities for molecular imaging and therapy.

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