title: Graphene quantum dots for cancer targeted drug delivery.
abstract: A biocompatible and cell traceable drug delivery system Graphene Quantum Dots (GQD) based, for the targeted delivery of the DNA intercalating drug doxorubicin (DOX) to cancer cells, is here reported. Highly dispersible and water soluble GQD, synthesized by acidic oxidation and exfoliation of multi-walled carbon nanotubes (MWCNT), were covalently linked to the tumor targeting module biotin (BTN), able to efficiently recognize biotin receptors over-expressed on cancer cells and loaded with DOX. Biological test performed on A549 cells reported a very low toxicity of the synthesized carrier (GQD and GQD-BTN). In GQD-BTN-DOX treated cancer cells, the cytotoxicity was strongly dependent from cell uptake which was greater and delayed after treatment with GQD-BTN-DOX system with respect to what observed for cells treated with the same system lacking of the targeting module BTN (GQD-DOX) or with the free drug alone. A delayed nuclear internalization of the drug is reported, due to the drug detachment from the nanosystem, triggered by the acidic environment of cancer cells.
authors.affiliation: Department of Engineering, University of Messina, Contrada Di Dio, I-98166 Messina, Italy. Electronic address: diannazzo@unime.it.
authors.forename: Daniela
authors.initials: D
authors.lastname: Iannazzo
authors.affiliation: Department of Engineering, University of Messina, Contrada Di Dio, I-98166 Messina, Italy.
authors.forename: Alessandro
authors.initials: A
authors.lastname: Pistone
authors.affiliation: Department of Engineering, University of Messina, Contrada Di Dio, I-98166 Messina, Italy.
authors.forename: Marina
authors.initials: M
authors.lastname: Salamò
authors.affiliation: Department of Engineering, University of Messina, Contrada Di Dio, I-98166 Messina, Italy.
authors.forename: Signorino
authors.initials: S
authors.lastname: Galvagno
authors.affiliation: Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Annunziata, I-98168 Messina, Italy.
authors.forename: Roberto
authors.initials: R
authors.lastname: Romeo
authors.affiliation: Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Annunziata, I-98168 Messina, Italy.
authors.forename: Salvatore V
authors.initials: SV
authors.lastname: Giofré
authors.affiliation: Department of Mathematical and Computer Sciences, Physical Sciences and Earth Sciences, Viale F. Stagno d'Alcontres, 98166 Messina, Italy.
authors.forename: Caterina
authors.initials: C
authors.lastname: Branca
authors.affiliation: Department of Biomedical and Dental Sciences and Morphological and Functional Images, University Hospital of Messina, Via Consolare Valeria, 1, 98100, Messina, Italy.
authors.forename: Giuseppa
authors.initials: G
authors.lastname: Visalli
authors.affiliation: Department of Biomedical and Dental Sciences and Morphological and Functional Images, University Hospital of Messina, Via Consolare Valeria, 1, 98100, Messina, Italy.
authors.forename: Angela
authors.initials: A
authors.lastname: Di Pietro
mesh_terms: D000072283:A549 Cells; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage / Q000737:chemistry*; D001710:Biotin / Q000008:administration & dosage / Q000737:chemistry*; D002470:Cell Survival / Q000187:drug effects; D004317:Doxorubicin / Q000008:administration & dosage / Q000737:chemistry*; D016503:Drug Delivery Systems; D006108:Graphite / Q000008:administration & dosage / Q000737:chemistry*; D006801:Humans; D037742:Nanotubes, Carbon / Q000737:chemistry; D009369:Neoplasms / Q000378:metabolism; D045663:Quantum Dots / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D000903:Antibiotics, Antineoplastic; D037742:Nanotubes, Carbon; D001710:Biotin; D006108:Graphite; D004317:Doxorubicin
keywords: Anticancer activity; Drug delivery system; Graphene quantum dots; Targeted delivery