Automated microfluidic chip system for radiosynthesis of PET imaging probes / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

Positron emission tomography (PET) is a powerful non-invasive molecular imaging technique for the early detection, characterization, and "real-time" monitoring of disease, and for investigating the efficacy of drugs (Phelps, 2000; Ametamey et al., 2008). The development of molecular probes bearing short-lived positron-emitting radionuclides, such as 18F (half-life 110 min) or 11C (half-life 20 min), is crucial for PET imaging to collect in vivo metabolic information in a time-efficient manner (Deng et al., 2019). In this regard, one of the main challenges is rapid synthesis of radiolabeled probes by introducing the radionuclides into pharmaceuticals as soon as possible before injection for a PET scan. Although many potential PET probes have been discovered, only a handful can satisfy the demand for a highly efficient synthesis procedure that achieves radiolabeling and delivery for imaging within 1-2 radioisotope half-lives. Only a few probes, such as 2-deoxy-2-[18F]fluoro-D-glucose (18F-FDG) and [18F]fluorodopa, are routinely produced on a commercial scale for daily clinical diagnosis (Grayson et al., 2018; Carollo et al., 2019).

Size Control of 99mTc-tin Colloid Using PVP and Buffer Solution for Sentinel Lymph Node Detection

Colloidal particle size is an important characteristic that allows mapping sentinel nodes in lymphoscintigraphy. This investigation aimed to introduce different ways of making a 99mTc-tin colloid with a size of tens of nanometers. All agents, tin fluoride, sodium fluoride, poloxamer-188, and polyvinylpyrrolidone (PVP), were mixed and labeled with 99mTc. Either phosphate or sodium bicarbonate buffers were used to adjust the pH levels. When the buffers were added, the size of the colloids increased. However, as the PVP continued to increase, the size of the colloids was controlled to within tens of nanometers. In all samples, phosphate buffer added PVP (30 mg) stabilized tin colloid (99mTc-PPTC-30) and sodium bicarbonate solution added PVP (50 mg) stabilized tin colloid (99mTc-BPTC-50) were chosen for in vitro and in vivo studies. 99mTc-BPTC-50 (100 nm) mainly accumulated in the liver. When a rabbit was given a toe injection, the node uptake of 99mTc-PPTC-30 decreased over time, while 99mTc-BPTC-50 increased. Therefore, 99mTc-BPTC-50 could be a good candidate radiopharmaceutical for sentinel node detection. The significance of this study is that nano-sized tin colloid can be made very easily and quickly by PVP.

Preparation and evaluation of [99m]Tc-DMSA lyophilized kit for renal imaging

Dimercaptosuccinic acid [DMSA] has been evaluated and used with technetium 99m [[99m]Tc] in imaging of kidneys. DMSA lyophilized kits were prepared and radiolabelled with [99m]Tc. Paper and thin-layer chromatography have been employed using various eluent systems for the radiochemical analysis, percentage labeling and binding capacity of [99m]Tc-DMSA. Female albino rabbits were used for this study. Biological data obtained after intravenous injection of radiolabelled DMSA to female albino rabbits revealed 32.42% uptake and long retention time in the kidneys. On the basis of animal biodistribution data, it is suggested that DMSA when labeled with [99m]Tc is useful complex for renal imaging and can be successfully applied as a diagnostic tool in nuclear medicine. Clinical biodistribution and radiation dosimetry studies are planned in future

Marcación de un derivado de glucosa con 99mTc mediante la formación de un complejo Tc(V)-nitruro: estudios preliminares / Labelling of a glucose derivative with 99mTc through the formation of a Tc(V)-nitride symmetrical complex: preliminary studies

La preparación de derivados de glucosa marcados con 99mTc reviste gran interés para la evaluación del consumo de glucosa in vivo en oncología y cardiología nuclear. Este trabajo presenta la marcación de un análogo de glucosa (GLU-DTC) mediante la formación de un complejo Tc(V)-nitruro simétrico. Para ello se incorporó a la biomolécula un grupo ditiocarbamato capaz de coordinar al metal. La marcación fue realizada mediante sustitución de ligandos, obteniéndose una única especie con pureza radioquímica superior al 90 por cientp, la que se mantuvo durante al menos 4 hs. La caracterización fisicoquímica y biológica muestra que el complejo 99mTc(V)-nitruro(GLU-DTC)2 es un compuesto estable y altamente hidrofílico, aunque su unión a proteínas plasmáticas es mayor a la esperada, hecho que justificaría la alta actividad retenida en sangre y en hígado durante la evaluación biológica en ratones CD1 normales. Estos resultados indican que la marcación con 99mTc de este derivado de glucosa produce una alteración significativa de su comportamiento biológico.

The preparation of 99mTc-labeled glucose derivatives is of great interest to evaluate the in vivo glucose uptake in nuclear oncology and cardiology. This paper presents the labelling of a glucose analogue (GLU-DTC) through the formation of a Tc(V)-nitride symmetrical complex. For this purpose, a dithiocarbamate group was incorporated to the biomolecule, in order to coordinate the metal. The labelling reaction was carried out by substitution yielding a single complex with radiochemical purity above 90 percent. This complex was stable for at least 4 hours. The physicochemical and biological characterization shows that the 99mTc(V)-nitride(GLU-DTC)2 complex is a stable and highly hydrophilic compound, although its plasma protein binding is greater than expected, a fact which justifies the high activity retained in blood and liver during the biological evaluation in normal CD1 mice. These results indicate that 99mTc labelling of this glucose derivate alters significantly its biological behaviour.