Diagnostic and therapeutic applications of radiopharmaceutical agents: The medical use of radioactive iodine (I-131) therapy for hyperthyroidism treatments.

The treatment of hyperthyroidism with iodine-131 has been recognized on nuclear medicine as simple, effective and inexpensive, this kind of radiopharmaceutical is chosen by the majority of medical centers by administering a minimum effective dose enabling euthyroidism to be easily compensated as quickly as possible while avoiding radiation problems. In this mini_review, we are going to explain the diagnostic and therapeutic aspect of radiopharmaceuticals by taking an example of radioiodine I-131 and its role on hyperthyroidism treatment .

Towards the stable chelation of radium for biomedical applications with an 18-membered macrocyclic ligand

The therapeutic alpha-emitter 223Ra can be stably complexed in vivo, creating opportunities for the development of targeted radiopharmaceutical agents with this radionuclide.

Analysis of Unusual Adverse Effects After Radium-223 Dichloride Administration

Background: To our knowledge, no previous study or literature review has been performed about the effects of the extravasation of therapeutic radiopharmaceutical agents and its potential consequences, especially regarding alpha-particle emitting radiopharmaceuticals. Methods: Even if Radium-223 dichloride is known to be a relatively safe drug to manage, despite the correctness of the procedures applied , unexpected delayed adverse effects can occur. : In our vast experience, we rarely observed lymphedema, even after some time, at the site of administration. Results: Management of lymphedema caused by radiopharmaceuticals administration has been addressed through clinical examples. The sudden intervention allowed a fast remission of the signs and symptoms complained by patients treated with Radium-223 dichloride. Conclusions: The management of adverse effects after radiopharmaceuticals administration as in case of lymphedema onset, is extremely simple. These data confirm the safety of Radium-223 treatment.

Hydroxyapatite and porphyrin-fullerene nanoparticles for diagnostic and therapeutic delivery of paramagnetic ions and radionuclides

Nanoparticles for drug delivery are the subject of extensive research. Importantly, they can transform in size during synthesis or actual use, thereby changing their cytotoxic properties. The aim of the present work was to study the tendency of [67Zn] porphyrin-fullerene nanoparticles (BFNP) to aggregate over time and to compare the properties of hydroxyapatite (HAP) nanoparticles obtained through 3 different techniques. We found that aggregation of BFNP nanoparticles does not affect their function but attenuates their cytotoxicity against leukemia cells. We were also able to obtain HAP nanoparticles with programmable properties (such as size, shape or the capacity to adsorb metal ions, ligands and chemical complexes) through enzymatic synthesis by varying its conditions. The synthesized HAP nanoparticles contain short-lived isotopes of zinc and copper (in the form of ions and complexes with pyrimidine or thiazine derivatives). These tumoricidal components (a radionuclide and a ligand or a complex) determine the diagnostic and therapeutic potential of the obtained radiopharmaceutical agents.

New leads for fragment-based design of rhenium/technetium radiopharmaceutical agents

Multiple possibilities for the coordination offac-[Re(CO)3(H2O)3]+to a protein have been determined and include binding to Asp, Glu, Arg and His amino-acid residues as well as to the C-terminal carboxylate in the vicinity of Leu and Pro. The large number of rhenium metal complex binding sites that have been identified on specific residues thereby allow increased target identification for the design of future radiopharmaceuticals. The core experimental concept involved the use of state-of-art tuneable synchrotron radiation at the Diamond Light Source to optimize the rhenium anomalous dispersion signal to a large value (f′′ of 12.1 electrons) at itsLIabsorption edge with a selected X-ray wavelength of 0.9763 Å. At the Cu Kα X-ray wavelength (1.5418 Å) thef′′ for rhenium is 5.9 electrons. The expected peak-height increase owing to the optimization of the Ref′′ was therefore 2.1. This X-ray wavelength tuning methodology thereby showed the lower occupancy rhenium binding sites as well as the occupancies of the higher occupancy rhenium binding sites.