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Over the past decade, there has been a burgeoning focus on exploring molecular-based drug delivery systems tailored for selective targeting in cancer research. This emerging field within cancer therapy offers a viable alternative to conventional anticancer drugs, with potential benefits such as cancer-selective uptake, minimal off-target toxicity, and the capability of active tumor targeting. These systems consist of a cancer-targeting unit, a fluorophore reporter connected to anticancer drugs through a labile chemical linker. The incorporation of a fluorophore not only facilitates a comprehensive understanding of the drug’s specific action on the target, but also enables the monitoring and tracking of its therapeutic response. In this chapter, we shed light on the pivotal role of fluorescence in the development of drug delivery systems, aiming to enhance therapeutic efficacy and lay the groundwork for the future of personalized cancer medicine.

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