Abstract
Graphene, including graphene quantum dots, its oxide and unoxidized
forms (pure graphene) have several properties, like fluorescence,
electrical conductivity, theoretical surface area, low toxicity, and
high biocompatibility. In this study, we evaluated genotoxicity (in
silico analysis using the functional density theory-FDT), cytotoxicity
(human glioblastoma cell line), in vivo pharmacokinetics, in vivo impact
on microcirculation and cell internalization assay. It was also
radiolabeled with lutetium 177 (177Lu), a beta emitter radioisotope to
explore its therapeutic use as nanodrug. Finally, the impact of its
disposal in the environment was analyzed using ecotoxicological
evaluation. FDT analysis demonstrated that graphene can construct
covalent and non-covalent bonds with different nucleobases, and graphene
oxide is responsible for generation of reactive oxygen species (ROS),
corroborating its genotoxicity. On the other hand, non-cytotoxic effect
on glioblastoma cells could be demonstrated. The pharmacokinetics
analysis showed high plasmatic concentration and clearance. Topical
application of 0.1 and 1 mg/kg of graphene nanoparticles on the hamster
skinfold preparation did not show inflammatory effect. The cell
internalization assay showed that 1-hour post contact with cells,
graphene can cross the plasmatic membrane and accumulate in the
cytoplasm. Radio labeling with 177Lu is possible and its use as
therapeutic nanosystem is viable. Finally, the ecotoxicity analysis
showed that A. silina exposed to graphene showed pronounced uptake and
absorption in the nauplii gut and formation of ROS. The data obtained
showed that although being formed exclusively of carbon and
carbon-oxygen, graphene and graphene oxide respectively generate
somewhat contradictory results and more studies should be performed to
certify the safety use of this nanoplatform.
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