Cancer has become one of the major causes of death worldwide. Chemotherapy remains a cornerstone of cancer treatment. To enhance the tumor-targeting efficiency of chemotherapy agents, pharmaceutical scientists have developed nanocarriers. However, the in vivo structural integrity and dynamic changes in nanocarriers after administration are not well understood, which may significantly impact their tumor-targeting abilities. In this paper, we propose the use of environmentally responsive fluorescent probes to track the integrity of antitumor nanocarriers. We compare three main types of dyes: fluorescence resonance energy transfer (FRET) dyes, aggregation-induced emission (AIE) dyes, and aggregation-caused quenching (ACQ) dyes. Among them, ACQ dyes, possessing sensitive water-quenching properties and easily detected “on–off” switching behavior, are regarded as the most promising choice. We believe that ACQ dyes are suitable for investigating the in vivo fate of antitumor nanocarriers and can aid in designing improved nanoformulations for chemotherapy agents.
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