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Graphene quantum dots : from efficient preparation to safe renal excretion Hadad, Caroline González-Domínguez, José Miguel Armelloni, Silvia Mattinzoli, Deborah Ikehata, Masami Istif, Akcan Ostric, Adrian Cellesi, Francesco Alfieri, Carlo Maria Messa, Piergiorgio Ballesteros, Belén Da Ros, Tatiana Graphene quantum dots Podocytes Biodistribution Uptake pathway Renal clearance Nanocarrier Carbon nanomaterials offer excellent prospects as therapeutic agents, and among them, graphene quantum dots (GQDs) have gained considerable interest thanks to their aqueous solubility and intrinsic fluorescence, which enable their possible use in theranostic approaches, if their biocompatibility and favorable pharmacokinetic are confirmed. We prepared ultra-small GQDs using an alternative, reproducible, top-down synthesis starting from graphene oxide with a nearly 100% conversion. The materials were tested to assess their safety, demonstrating good biocompatibility and ability in passing the ultrafiltration barrier using an in vitro model. This leads to renal excretion without affecting the kidneys. Moreover, we studied the GQDs in vivo biodistribution confirming their efficient renal clearance, and we demonstrated that the internalization mechanism into podocytes is caveolae-mediated. Therefore, considering the reported characteristics, it appears possible to vehiculate compounds to kidneys by means of GQDs, overcoming problems related to lysosomal degradation. 2021 Article European Commission 734381 European Commission 734834 Ministerio de Ciencia e Innovación IJCI-2016-27789 Ministerio de Economía y Competitividad SEV-2017-0706 Nano research ; Vol. 14, issue 3 (March 2021), p. 674-683 open access Aquest document està subjecte a una llicència d'ús Creative Commons. Es permet la reproducció total o parcial, la distribució, la comunicació pública de l'obra i la creació d'obres derivades, fins i tot amb finalitats comercials, sempre i quan es reconegui l'autoria de l'obra original. https://creativecommons.org/licenses/by/4.0/