TY - JOUR
T1 - FRET-based intracellular investigation of nanoprodrugs toward highly efficient anticancer drug delivery
AU - Taemaitree, Farsai
AU - Fortuni, Beatrice
AU - Koseki, Yoshitaka
AU - Fron, Eduard
AU - Rocha, Susana
AU - Hofkens, Johan
AU - Uji-I, Hiroshi
AU - Inose, Tomoko
AU - Kasai, Hitoshi
N1 - Publisher Copyright:
© 2020 The Royal Society of Chemistry.
PY - 2020/8/28
Y1 - 2020/8/28
N2 - 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.
AB - 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.
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U2 - 10.1039/d0nr04910g
DO - 10.1039/d0nr04910g
M3 - Article
C2 - 32785392
AN - SCOPUS:85089787126
VL - 12
SP - 16710
EP - 16715
JO - Nanoscale
JF - Nanoscale
SN - 2040-3364
IS - 32
ER -
