-Benzylethanolammonium Ionic Liquids and Molten Salts in the Synthesis of Ga- and AlF-Labeled Radiopharmaceuticals.

Ionic liquids (ILs), due to their structural features, have unique physical and chemical properties and are environmentally friendly. Every year, the number of studies devoted to the use of ILs in medicine and pharmaceutics is growing. In nuclear medicine, the use of ILs with self-buffering capacity in the synthesis of radiopharmaceuticals is extremely important.

Calcium carbonate carriers for combined chemo- and radionuclide therapy of metastatic lung cancer.

Considering the clinical limitations of individual approaches against metastatic lung cancer, the use of combined therapy can potentially improve the therapeutic effect of treatment. However, determination of the appropriate strategy of combined treatment can be challenging. In this study, combined chemo- and radionuclide therapy has been realized using radionuclide carriers (Lu-labeled core-shell particles, Lu-MPs) and chemotherapeutic drug (cisplatin, CDDP) for treatment of lung metastatic cancer.

Impact of metallic coating on the retention of Ac and its daugthers within core-shell nanocarriers.

Currently, alpha-emitting radionuclide Ac is one of the most promising isotopes in alpha therapy due to its high linear energy transfer during four sequential alpha decays. However, the main obstacle preventing the full introduction of Ac into clinical practice is the lack of stable retention of radionuclides, leading to free circulation of toxic isotopes in the body. In this work, the surface of silica nanoparticles (SiO NPs) has been modified with metallic shells composed of titanium dioxide (TiO) and gold (Au) nanostructures to improve the retention of Ac and its decay products within the developed nanocarriers.

Calcium Carbonate Core-Shell Particles for Incorporation of Ac and Their Application in Local α-Radionuclide Therapy.

Actinium-225 (Ac) radiolabeled submicrometric core-shell particles (SPs) made of calcium carbonate (CaCO) coated with biocompatible polymers [tannic acid-human serum albumin (TA/HSA)] have been developed to improve the efficiency of local α-radionuclide therapy in melanoma models (B16-F10 tumor-bearing mice). The developed Ac-SPs possess radiochemical stability and demonstrate effective retention of Ac and its daughter isotopes. The SPs have been additionally labeled with zirconium-89 (Zr) to perform the biodistribution studies using positron emission tomography-computerized tomography (PET/CT) imaging for 14 days after intratumoral injection.

An investigation of calcium carbonate core-shell particles for incorporation of Ac and sequester of daughter radionuclides: in vitro and in vivo studies.

Alpha therapy provides an outstanding prospect in the treatment of recalcitrant and micrometastatic cancers. However, side effects on the normal tissues and organs (especially, kidneys) due to the release of daughter isotopes from α-emitters remain a bottleneck. In this work, calcium carbonate core-shell particles of different sizes were considered as isotope carriers for encapsulation of Ac (highly powerful alpha-emitter that generates 4 net alpha particle isotopes in a short decay chain) in order to achieve in vitro and in vivo retention of Ac and its daughter isotopes.

On the consensus nomenclature rules for radiopharmaceutical chemistry - Reconsideration of radiochemical conversion.

Radiochemical conversion is an important term to be included in the "Consensus nomenclature rules for radiopharmaceutical chemistry". Radiochemical conversion should be used to define reaction efficiency by measuring the transformation of components in a crude reaction mixture at a given time, whereas radiochemical yield is better suited to define the efficiency of an entire reaction process including, for example, separation, isolation, filtration, and formulation.

Tetrabutylammonium tosylate as inert phase-transfer catalyst: The key to high efficiency S2 radiofluorinations.

Here we describe use of the tetrabutylammonium p-toluenesulfonate (TBAOTs) as an inert phase transfer catalyst allowing high efficient aliphatic radiofluorination of labeling precursors for the preparation of common radiotracers using only 0.2-1.2 mg of the substrates.

Radiolabeling Strategies of Micron- and Submicron-Sized Core-Shell Carriers for Studies.

Core-shell particles made of calcium carbonate and coated with biocompatible polymers using the Layer-by-Layer technique can be considered as a unique drug-delivery platform that enables us to load different therapeutic compounds, exhibits a high biocompatibility, and can integrate several stimuli-responsive mechanisms for drug release. However, before implementation for diagnostic or therapeutic purposes, such core-shell particles require a comprehensive evaluation in terms of physicochemical and pharmacokinetic properties. Positron emission tomography (PET) is an advanced imaging technique for the evaluation of biodistribution of drug carriers; nevertheless, an incorporation of positron emitters in these carriers is needed.

Use of capillary electrophoresis for the determination of impurities in preparations of fluorine-18 labelled PET radiopharmaceuticals.

Fluorine-18 labelled radiotracers are the most common diagnostic agents employed in positron emission tomography (PET). Despite well-established quality control (QC) procedures, introduction of new synthetic methods demands continuous development of analytical methodology. Here we propose capillary electrophoresis (CE) as a simple, fast and cost-efficient analytical method, allowing for the evaluation of potentially toxic impurities, including transition metals, in the formulated preparations.