[223Ra] RaCl2 nanomicelles showed potent effect against osteosarcoma: targeted alpha therapy in the nanotechnology era.

The treatment of bone metastatsis as primary bone cancer itself is still a challenge. The use od radium dichloride ([223Ra] RaCl2) has emerged in the last few years as one of the best treatment choice for bone cancer, with especial focus in bone metastasis. The alpha-emitter radiopharmaceutical has showed potent and efficient results in several clinical trials. In this study we have formulated radium dichloride ([223Ra] RaCl2) nanomicelles in order to evaluate and compare with pure radium dichloride ([223Ra] RaCl2). The results showed that nanomicelles at the same dose had a superior effect (20% higher efficient) when compared with pure radium dichloride ([223Ra] RaCl2). The results corroborated the effectiveness of the nanosystem validating the application of nanotechnology in alpha-radiotherapy with radium dichloride ([223Ra] RaCl2).

Graphene Quantum Dots for Molecular Radiotherapy: Radiolabeled Graphene Quantum Dots with Radium (223Ra) Showed Potent Effect Against Bone Cancer.

The necessity of new drugs with special attention for the therapy of cancer is increasing each day. Despite their properties, alpha therapeutic radiopharmaceuticals, especially based on the use of radium (223Ra) are good choices, due to the highest and differential cytotoxicity, low adverse effects, and higher bioaccumulation on tumor sites. The use of graphene quantum dots as the carrier for 223Ra is a promising approach since graphene quantum dots has low toxicity, high biocompatibility, and adequate size for tumor penetration. In this study, we developed, characterized, radiolabeled with 223Ra, and evaluated in vitro and in vivo graphene quantum dots radiolabeled with radium (223Ra) for bone cancer. The results showed that 223Ra is incorporated into the graphene quantum dot following the Fajans-Paneth-Hahn Law. The cell viability showed a potent effect on osteosarcoma cells (MG63 and SAOS2) but a lower effect in normal fibroblast cells (hFB), corroborating the preferential targeting. Also, the results showed a more prominent effect on MG63 than SAOS2 cells, corroborating the targeting for more undifferentiated cells. The in vivo results demonstrated a renal excretion, associated with fecal excretion and accumulation in bone. The results corroborate the efficacy of 223RaGQDs and open new perspectives for the use of use 223RaGQDs, in several other diseases.