Farsai Taemaitree, Beatrice Fortuni, Yoshitaka Koseki, Eduard Fron, Susana Rocha, Johan Hofkens, Hiroshi Uji-i, Tomoko Inose, Hitoshi Kasai
Nanoscale 12 32 16710 - 16715 2020年
[査読有り] 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 towardsin vivoand clinical applications. Here, we report a comprehensivein cellulostudy of carrier-free SN-38 nanoprodrugs (NPDs), previously developed by our group. The work shows the intracellular uptake, localization, and degradation of the NPDsviaFRET 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.