Multi-functionalization of graphene for molecular targeted cancer therapy

“Three” kinds of regalia such as crown, orb, and sward are often necessary to be a high king for conquering the world. For fighting off cancerous diseases, what do we need? This “triple” chemical modified nanomaterial might be save the patient.

Cancer is a leading cause of death worldwide. Under this situation, a successful tumor selective drug targeting and minimized toxicity of cancer drug are urgently necessary.

Scientists from Japan Advanced Institute of Science and Technology (JAIST) and Centre national de la recherche scientifique (CNRS), and their colleagues have developed a type of nanomedicine based on multi-functional graphene that allows for targeted cancer treatment at molecular level.

Single molecular sheet graphene is a promising carbon nanomaterial for various fundamental and practical applications in the next decade because of its excellent physico-chemical features. Graphene has been also known to have a good biocompatibility and biodegradability, thus leading to explore this nanocarbon as drug delivery carrier. However, it is not easy to modify a lot of individual functional molecules onto a graphene nano-sheet at the same time for its biomedical applications.

Developed by Prof. Eijiro Miyako from JAIST (Nomi, Japan), Dr. Alberto Bianco from CNRS (Strasbourg, France), and their international teams, the multi-functional graphene as a drug delivery carrier are successfully synthesized with “three” type of molecules such as near-infrared (NIR) fluorescent probe (indocyanine green; ICG), tumor targeting molecule (Folic acid: FA), and anticancer drug (doxorubicin; Dox) by a covalent chemical modification technique (Figure 1). ICG (green color part in the picture) was chosen as fluorophore to follow the uptake and to track the material inside the cells. FA (blue) was covalently bound through a polyethylene glycol (pink) linked to graphene, to specifically target the cancer cells, and Dox (red) was used as anticancer drug.

Aside from testing the therapeutic abilities to eliminate cancer cells in a culture dish, the team found that the unique properties of this multi-functional graphene showed an enhanced anticancer activity with excellent cancer targeting effect. This would open the doors to future biomedical applications of this type of material. The team plans to continue exploring multi-functional graphene towards the cancer therapy using murine animal model.

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Paper titled “Rational chemical multifunctionalization of graphene interface enhances targeting cancer therapy”, published in Angewandte Chemie International Edition, DOI: 10.1002/anie.201916112

The work was supported by the Japan Society for the Promotion of Science KAKENHI Grant-in-Aid for Scientific Research (A) and (B), the KAKENHI Fund for the Promotion of Joint International Research, the Agence Nationale de la Recherche (ANR), the Graphene Flagship, the Spanish MINECO, the Generalitat Valenciana.