Photoacoustic (PA) imaging and photothermal therapy (PTT) have attracted extensive attention in disease diagnosis and treatment. Although many exogenous contrast agents have been developed for PA imaging and PTT, the design guidelines to amplify their imaging and therapy performances remain challenging and are highly demanded. Semiconducting polymer nanoparticles (SPNs) composed of polymers with π‐electron delocalized backbones can be designed to amplify their PA imaging and PTT performance, because of their clear structure–property relation and versatility in modifying their molecular structures to tune their photophysical properties. This review summarizes the recent advances in the photoacoustic imaging and photothermal therapy applications of semiconducting polymer nanoparticles with a focus on signal amplification and second near‐infrared (NIR‐II, 1000–1700 nm) construction. The strategies such as structure–property screening, fluorescence quenching, accelerated heat dissipation, and size‐dependent heat dissipation are first discussed to amplify the PA brightness of SPNs for in vivo PA. The molecular approaches to shifting the absorption of SPNs for NIR‐II PA imaging and PTT are then introduced so as to improve the tissue penetration depth for diagnosis and therapy. At last, current challenges and perspectives of SPNs in the field of imaging and therapy are discussed.
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