Nanomicelles of Radium Dichloride [223Ra]RaCl2 Co-Loaded with Radioactive Gold [198Au]Au Nanoparticles for Targeted Alpha–Beta Radionuclide Therapy of Osteosarcoma

Abstract

Alpha and beta particulate radiation are used for non-treated neoplasia, due to their ability to reach and remain in tumor sites. Radium-223 (223Ra), an alpha emitter, promotes localized cytotoxic effects, while radioactive gold (198Au), beta-type energy, reduces radiation in the surrounding tissues. Nanotechnology, including several radioactive nanoparticles, can be safely and effectively used in cancer treatment. In this context, this study aims to analyze the antitumoral effects of [223Ra]Ra nanomicelles co-loaded with radioactive gold nanoparticles ([198Au]AuNPs). For this, we synthesize and characterize nanomicelles, as well as analyze some parameters, such as particle size, radioactivity emission, dynamic light scattering, and microscopic atomic force. [223Ra]Ra nanomicelles co-loaded with [198Au]AuNPs, with simultaneous alpha and beta emission, showed no instability, a mean particle size of 296 nm, and a PDI of 0.201 (±0.096). Furthermore, nanomicelles were tested in an in vitro cytotoxicity assay. We observed a significant increase in tumor cell death using combined alpha and beta therapy in the same formulation, compared with these components used alone. Together, these results show, for the first time, an efficient association between alpha and beta therapies, which could become a promising tool in the control of tumor progression.

Study of 211Bi and 211Pb Recoils Release from 223Ra Labelled TiO2 Nanoparticles

“…The same order of magnitude values could be expected for 211 Pb and 211 Bi progeny sorption on nTiO 2 . In our previous work, we also came to the assumption that the probability of back-implantation of the first-decay progeny should be statistically close to the value of 50% in the case of surface labelled NPs [19]. This effect should be further supported by the progeny resorption on the NPs surface, if ejected out of the NPs.…”

“…Many types of nanoparticles have been proposed and tested as carriers for alpha radionuclides in order to least partially prevent the significant release of radioactive progeny originating from the chain decay of used alpha-emitting radionuclides. Studies have included both organic [16][17][18] as well as various inorganic nanoparticles [19][20][21][22][23][24][25][26]. Contrary to the pitfall of the unwanted progeny release, one may benefit from the controlled release of the radioactive nuclei from the nanoparticle or polymer-based brachytherapy carriers, in order to exploit their relocation from their origin by diffusion, convection, or active transport, to irradiate the whole volume of the tumour [27][28][29][30][31][32].…”

Nano-Based Drug Delivery Systems: Potential Developments in the Therapy of Metastatic Osteosarcoma—A Narrative Review

“…Yang et al [ 109 ] spearheaded an intriguing study where they employed Pluronic F127 to formulate nanomicelles. These were entrusted with the task of delivering [223Ra] RaCl 2 —radium dichloride, an alpha-emitting radiopharmaceutical renowned for its ability to selectively adhere to bone malignancies and metastases [ 110 , 111 , 112 ]. Clinical explorations have lauded radium dichloride for its efficacy.…”

Methods for Radiolabeling Nanoparticles (Part 3): Therapeutic Use

“…Next, [ 198 Au]AuNPs were added to the solution and ultrasonicated for more than 2 min in an ice bath at 10 °C. The in vitro citotoxicity studies revealed a substantial increase in tumor-cell death when the treatments with both [ 223 Ra]RaCl 2 and [ 198 Au]Au-NPs were combined in the same formulation, compared to the [ 223 Ra]RaCl 2 or [ 198 Au]Au-NPs alone [ 35 ].…”