抄録
Unlike conventional carrier–based drug delivery systems, anticancer nano–prodrugs are carrier–free nanoparticles with a high drug loading capacity that have shown approximately 10–fold higher therapeutic efficacy compared to marketed drugs in animal experiments. However, their detailed biological behavior, particularly their cellular membrane permeability and intracellular degradation processes, remained unclear. Using fluorescence microscopy based on Förster resonance energy transfer (FRET), we successfully tracked the cellular uptake and intracellular dynamics of nano–prodrugs, which had previously been difficult to observe. This paper describes the comprehensive process from endocytic cellular uptake to intracellular particle degradation and conversion into active drug molecules.