FRET-based intracellular investigation of nanoprodrugs toward highly efficient anticancer drug delivery

Farsai Taemaitree, Beatrice Fortuni, Yoshitaka Koseki, Eduard Fron, Susana Rocha, Johan Hofkens, Hiroshi Uji-I, Tomoko Inose, Hitoshi Kasai

Research output: Contribution to journalArticlepeer-review

14 Citations (Scopus)


In order to overcome unpredictable side-effects and increased cytotoxicity of conventional carrier-based anticancer drug delivery systems, several systems that consist exclusively of the pure drug (or prodrug) have been proposed. The behavior and dynamics of these systems after entering cancer cells are, however, still unknown, hindering their progress towards in vivo and clinical applications. Here, we report a comprehensive in cellulo study of carrier-free SN-38 nanoprodrugs (NPDs), previously developed by our group. The work shows the intracellular uptake, localization, and degradation of the NPDs via FRET microscopy. Accordingly, new FRET-NPDs were chemically synthesized and characterized. Prodrug to drug conversion and therapeutic efficiency were also validated. Our work provides crucial information for the application of NPDs as drug delivery systems and demonstrates their outstanding potential as next-generation anticancer nanomedicines.

Original languageEnglish
Pages (from-to)16710-16715
Number of pages6
Issue number32
Publication statusPublished - 2020 Aug 28


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