Abstract:
Herein, we report on the role of endocytosis in the selective chemotherpeutic toxicity of
Rhodamine 6G (R6G) based nanomaterials, i.e. nanoGUMBOS, that are derived from a Group of
Uniform Materials Based on Organic Salts (GUMBOS). Evaluation of cellular uptake in the
presence and absence of endocytosis inhibitors suggests nanoGUMBOS internalization via
clathrin-mediated endocytosis in cancer cells and reveals lack of endocytic internalization in
normal cells. Results from characterization of these nanomaterials suggest that endocytic
internalization in cancer cells leads to nanoGUMBOS dissociation within the endosomal
environment. This ultimately results in selective cytotoxicity of the nanoGUMBOS for cancer
cells with no toxicity towards normal cells under examined conditions. Following examination of
the selectivity mechanism, in vivo investigations were performed to examine potential
therapeutic properties of these nanoparticles. Remarkably, nanoGUMBOS treatment using a
mouse xenograft model reduced the tumor volume by 50% suggesting retention of in vitro
therapeutic properties in vivo. These results corroborate the selective behavior of nanoGUMBOS
and demonstrate their in vivo therapeutic effects, providing further insight into the possible use
of these nanomaterials as potential chemotherapeutic agents.
