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A nanosized drug complex was explored to improve the efficiency of cancer chemotherapy, complementing it with nanodelivery and photodynamic therapy. For this, nanomolar amounts of a non-covalent nanocomplex of Doxorubicin (Dox) with carbon nanoparticle C 60 fullerene (C 60 ) were applied in 1:1 and 2:1 molar ratio, exploiting C 60 both as a drug-carrier and as a photosensitizer. The fluorescence microscopy analysis of human leukemic CCRF-CEM cells, in vitro cancer model, treated with nanocomplexes showed Dox's nuclear and C 60 's extranuclear localization. It gave an opportunity to realize a double hit strategy against cancer cells based on Dox's antiproliferative activity and C 60 's photoinduced pro-oxidant activity. When cells were treated with 2:1 C 60 -Dox and irradiated at 405 nm the high cytotoxicity of photo-irradiated C 60 -Dox enabled a nanomolar concentration of Dox and C 60 to efficiently kill cancer cells in vitro. The high pro-oxidant and pro-apoptotic efficiency decreased IC 50 16, 9 and 7 × 10 3 -fold, if compared with the action of Dox, non-irradiated nanocomplex, and C 60 's photodynamic effect, correspondingly. Hereafter, a strong synergy of therapy arising from the combination of C 60 -mediated Dox delivery and C 60 photoexcitation was revealed. Our data indicate that a combination of chemo- and photodynamic therapies with C 60 -Dox nanoformulation provides a promising synergetic approach for cancer treatment.

Synergy of Chemo- and Photodynamic Therapies with C60 Fullerene-Doxorubicin Nanocomplex