No abstract

44 Sc is a promising β + -emitter for molecular imaging with intermediate half-life of 4 h. Due to the chemical similarity of Sc 3+ to the Lu 3+ and Y 3+ cations, 44 Sc-DOTA bioconjugates are expected to demonstrate similar properties in vivo as the 177 Lu-and 90 Y-bioconjugates, what is important in planning the radionuclide therapy. 44 Sc can be obtained from the 44 Ti/ 44 Sc generator. An alternative method for 44 Sc production can be the irradiation of 44 Ca target at small cyclotrons. The aim of our work was to optimize the parameters of 44 CaCO 3 irradiation and to develop a simple procedure for 44 Sc separation from the calcium target. For optimization study, 44 CaCO 3 targets were irradiated by protons in the energy range of 5.6-17.5 MeV with 9 MeV being found to be the best energy for 44 Ca irradiations. A simple and fast separation procedure of 44 Sc from calcium target was developed using chelating resin Chelex 100. DOTATATE conjugate was successfully radiolabelled with high yield at elevated temperature using the produced 44 Sc. While 44 CaCO 3 is relatively expensive, the cost of 44 Sc-DOTATATE production can be reduced by target recovery. Due to low proton energy required to produce GBq activity level of 44 Sc, the availability of 44 Sc radioisotope could be enhanced to open new opportunities for applications in medical imaging.

Prostate cancer is the most commonly diagnosed malignancy in men and the second leading cause of cancer-related deaths in Western civilization. Although localized prostate cancer can be treated effectively in different ways, almost all patients progress to the incurable metastatic castration-resistant prostate cancer. Due to the significant mortality and morbidity rate associated with the progression of this disease, there is an urgent need for new and targeted treatments. In this review, we summarize the recent advances in research on identification of prostate tissue-specific antigens for targeted therapy, generation of highly specific and selective molecules targeting these antigens, availability of therapeutic radionuclides for widespread medical applications, and recent achievements in the development of new-generation small-molecule inhibitors and antibody-based strategies for targeted prostate cancer therapy with alpha-, beta-, and Auger electron-emitting radionuclides.

The 223Ra, 224Ra, and 225Ra radioisotopes exhibit very attractive nuclear properties for application in radionuclide therapy. Unfortunately the lack of appropriate bifunctional ligand for radium is the reason why these radionuclides have not found application in receptor-targeted therapy. In the present work, the potential usefulness of the NaA nanozeolite as a carrier for radium radionuclides has been studied. 224Ra and 225Ra, α-particle emitting radionuclides, have been absorbed in the nanometer-sized NaA zeolite (30–70 nm) through simple ion exchange. 224,225Ra-nanozeolites exhibited very high stability in solutions containing physiological salt, EDTA, amino acids, and human serum. To make NaA nanozeolite particles dispersed in water their surface was modified with a silane coupling agent containing poly(ethylene glycol) molecules. This functionalization approach let us covalently attach a biomolecule to the NaA nanozeolite surface.

No abstract

Highly localized radiotherapy with radionuclides is a commonly used treatment modality for patients with unresectable solid tumors. Herein, we propose a novel α-nanobrachytherapy approach for selective therapy of human epidermal growth factor receptor 2 (HER2)-positive breast cancer. This uses local intratumoral injection of 5-nm-diameter gold nanoparticles (AuNPs) labeled with an α-emitter (211At), modified with polyethylene glycol (PEG) chains and attached to HER2-specific monoclonal antibody (trastuzumab). The size, shape, morphology, and zeta potential of the 5 nm synthesized AuNPs were characterized by TEM (Transmission Electron Microscopy) and DLS (Dynamic Light Scattering) techniques. The gold nanoparticle surface was modified by PEG and subsequently used for antibody immobilization. Utilizing the high affinity of gold for heavy halogens, the bioconjugate was labelled with 211At obtained by α irradiation of the bismuth target. The labeling yield of 211At was greater than 99%. 211At bioconjugates were stable in human serum. Additionally, in vitro biological studies indicated that 211At-AuNP-PEG-trastuzumab exhibited higher affinity and cytotoxicity towards the HER2-overexpressing human ovarian SKOV-3 cell line than unmodified nanoparticles. Confocal and dark field microscopy studies revealed that 211At-AuNP-PEG-trastuzumab was effectively internalized and deposited near the nucleus. These findings show promising potential for the 211At-AuNP-PEG-trastuzumab radiobioconjugate as a perspective therapeutic agent in the treatment of unresectable solid cancers expressing HER2 receptors.

Alpha particle emitting isotopes are of considerable interest for radionuclide therapy because of their high cytotoxicity and short path length. Due to the relatively high availability,

The therapeutic radionuclide 47Sc was produced through the 48Ca(p,2n) channel on a proton beam accelerator. The obtained results show that the optimum proton energies are in the range of 24–17 MeV, giving the possibility to produce 47Sc radionuclide containing 7.4% of 48Sc. After activation, the powdery CaCO3 target material was dissolved in HCl and scandium isotopes were isolated from the targets. The performed separation experiments indicate that, due to the simplicity of the operations and the chemical purity of the obtained 47Sc the best separation process is when scandium radioisotopes are separated on the 0.2 µm filter.