BACKGROUND: Radioligand therapy using alpha emitters has gained more and more prominence in the last decade. Despite continued efforts to identify new appropriate radionuclides, the combination of 225Ac/213Bi remains among the most promising. Bismuth-213 has been employed in clinical trials in combination with appropriate vectors to treat patients with various forms of cancer, such as leukaemia, bladder cancer, neuroendocrine tumours, melanomas, gliomas, or lymphomas. However, the half-life of 213Bi (T1⁄2 = 46 min) implies that its availability for clinical use is limited to hospitals possessing a 225Ac/213Bi radionuclide generator, which is still predominantly scarce. We investigated a new Ac/Bi generator system based on using the composite sorbent α-ZrP-PAN (zirconium(IV) phosphate as active component and polyacrylonitrile as matrix). The developed 225Ac/213Bi generator was subjected to long-term testing after its development. The elution profile was determined and the elution yield, the contamination of the eluate with the parent 225Ac and the contamination of the eluate with the column material were monitored over time. RESULTS: The high activity (75 MBq of parent 225Ac) generator with a length of 75 mm and a diameter of 4 mm containing the composite sorbent α-ZrP-PAN with a particle size of 0.8 to 1.0 mm as the stationary phase, eluted with a mixture of 10 mM DTPA in 5 mM nitric acid, provided 213Bi with yields ranging from 77 % to 96 % in 2.8 mL of eluate, with parent 225Ac contamination in the order of 10-3 %, up to twenty days of use. CONCLUSION: All the results of the monitored parameters indicate that the composite sorbent α-ZrP-PAN based separation system for the elution of 213Bi is a very promising and functional solution.
BACKGROUND: Targeted alpha therapy is one of the most powerful therapeutical modalities available in nuclear medicine. It's therapeutic potency is based on the nuclides that emit one or several alpha particles providing strong and highly localized therapeutic effects. However, some of these radionuclides, like e.g.223Ra or 225Ac decay in cascades, where the radioactive progeny originating from the consecutive alpha-decays may leave the original vector and cause unwanted irradiation of non-target organs. This progeny, even if partially retained in target tissues by internalization processes, typically do not follow the fate of originally targeted radiopharmaceutical and potentially spread over body following their own biodistribution. In this study we aimed to estimate 211Pb/211Bi progeny fate from the 223Ra surface-labelled TiO2 nanoparticles in vitro and the fate of 211Pb in vivo in a mice model. RESULTS: In vitro stability studies have shown significant differences between the release of the mother 223Ra and its progeny (211Pb, 211Bi) in all the biological matrices that have been tested. The lowest released activities were measured in saline, resulting in less than 5 % of released activity for all nuclides. Contrary to that, the highest released activity of 223Ra of up to 10 % within 48 h was observed in 5 % solution of albumin. The released activity of its progeny; the 211Pb and 211Bi was in the range of 20-40 % in this test medium. Significantly higher released activities of 211Pb and 211Bi compared to 223Ra by at least 10 % was observed in each biological medium, except saline, where no significant differences were observed. The in vivo biodistribution studies results in a mice model, show similar pattern, where it was found that even after accumulation of nanoparticles in target tissues, approximately 10 % of 211Pb is continuously released into the blood stream within 24 h, followed by its natural accumulation in kidneys. CONCLUSION: This study confirms our assumption that the progeny formed in a chain alpha decay of a certain nuclide, in this case the 223Ra, can be released from its original vector, leave the target tissue, relocate and could be deposited in non-target organs. We did not observe complete progeny wash-out from its original target tissues in our model. This indicates strong dependence of the progeny hot atom fate after its release from the original radiopharmaceutical preparation on multiple factors, like their internalization and retention in cells, cell membranes, extracellular matrices, protein binding, etc. We hypothesize, that also the primary tumour or metastasis size, their metabolic activity may significantly influence progeny fate in vivo, directly impacting the dose delivered to non-target tissues and organs. Therefore a bottom-up approach should be followed and detailed pre-/clinical studies on the release and biodistribution of radioactive progeny originating from the chain alpha emitters should be preferably performed.
- MeSH
- myši MeSH
- nanočástice * MeSH
- olovo MeSH
- radiofarmaka * terapeutické užití MeSH
- radionuklidy terapeutické užití MeSH
- tkáňová distribuce MeSH
- zvířata MeSH
- Check Tag
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
1,10-Phenanthroline was decorated with triterpenoid-based substituents bearing additional spermine units to form amphiphilic molecules. The synthetic procedure designed for the new phenanthroline-triterpenoid amphiphiles is described in detail. Besides 1,10-phenanthroline, all target structures bear 1,4-disubstituted 1,2,3-triazole rings. The target compounds self-assembled into either helical-like or sheet-like nanostructures, depending on the structure of the target molecule, either based on betulinic acid or oleanolic acid, and on the way of binding spermine subunits to the rest of the molecules. They also proved their ability to coordinate 64Cu(II) ions. Finally, the target compounds showed cytotoxicity that was partly dependent on the formation of nanostructures.
- MeSH
- fenantroliny chemie MeSH
- kyselina olenalová * MeSH
- spermin MeSH
- triazoly MeSH
- triterpeny * MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Targeted alpha therapy with radionuclides undergoing multiple alpha-particle decays is a promising method of nuclear medicine. To study the effectiveness of alpha versus beta emitters, survival of DU145 prostate cancer cells exposed to 223Ra or 177Lu was assessed. Per decay, the cells were much more sensitive to the alpha than beta emitter. However, per unit dose the sensitivities would be comparable, contrary to the well-known evidence, if the decay energy were deposited within the sample completely and homogeneously. Measurements by Timepix detectors showed about three times higher counts of alpha particles above than below the sample. After the first alpha decay of 223Ra to 219Rn, this gas likely moves upwards and its subsequent three alpha decays occur in the upper part of the sample. Correct estimation of absorbed dose is a critical issue when analysing in vitro data and when translating their results to clinical applications.
- MeSH
- alfa částice terapeutické užití MeSH
- lidé MeSH
- radiometrie metody MeSH
- radionuklidy terapeutické užití MeSH
- radium * MeSH
- Check Tag
- lidé MeSH
- mužské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
A set of fifteen triterpenoid pyrazines and pyridines was prepared from parent triterpenoid 3-oxoderivatives (betulonic acid, dihydrobetulonic acid, oleanonic acid, moronic acid, ursonic acid, heterobetulonic acid, and allobetulone). Cytotoxicity of all compounds was tested in eight cancer and two non-cancer cell lines. Evaluation of the structure-activity relationships revealed that the triterpenoid core determined whether the final molecule is active or not, while the heterocycle is able to increase the activity and modulate the specificity. Five compounds (1b, 1c, 2b, 2c, and 8) were found to be preferentially and highly cytotoxic (IC50 ≈ 1 μM) against leukemic cancer cell lines (CCRF-CEM, K562, CEM-DNR, or K562-TAX). Surprisingly, compounds 1c, 2b, and 2c are 10-fold more active in multidrug-resistant leukemia cells (CEM-DNR and K562-TAX) than in their non-resistant analogs (CCRF-CEM and K562). Pharmacological parameters were measured for the most promising candidates and two types of prodrugs were synthesized: 1) Sugar-containing conjugates, most of which had improved cell penetration and retained high cytotoxicity in the CCRF-CEM cell line, unfortunately, they lost the selectivity against resistant cells. 2) Medoxomil derivatives, among which compounds 26-28 gained activities of IC50 0.026-0.043 μM against K562 cells. Compounds 1b, 8, 21, 22, 23, and 24 were selected for the evaluation of the mechanism of action based on their highest cytotoxicity against CCRF-CEM cell line. Several experiments showed that the majority of them cause apoptosis via the mitochondrial pathway. Compounds 1b, 8, and 21 inhibit growth and disintegrate spheroid cultures of HCT116 and HeLa cells, which would be important for the treatment of solid tumors. In summary, compounds 1b, 1c, 2b, 2c, 24, and 26-28 are highly and selectively cytotoxic against cancer cell lines and were selected for future in vivo tests and further development of anticancer drugs.
- MeSH
- antitumorózní látky fytogenní * farmakologie MeSH
- antitumorózní látky * farmakologie MeSH
- chemorezistence MeSH
- HeLa buňky MeSH
- lidé MeSH
- membránový potenciál mitochondrií MeSH
- nádorové buněčné linie MeSH
- prekurzory léčiv * farmakologie MeSH
- pyraziny farmakologie MeSH
- pyridiny farmakologie MeSH
- triterpeny * farmakologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Cíl: Využití magnetických nanočástic jako multifunkčních materiálů pro současnou diagnostiku a terapii. Úvod: Rychlý vývoj v oblasti nanotechnologií usnadnil vznik nových nanomateriálů. S tímto trendem je také spojen zvýšený zájem o nano a mikro systémy tvořené magnetickými nosiči. Spojením magnetického nosiče s biologicky aktivní látkou lze dosáhnout unikátních vlastností využitelných v mnoha oblastech biotechnologie a medicíny. Popis problematiky: Mezi nejvíce studované materiály se řadí magnetické nanočástice tvořené oxidy železa. V současné době se velká pozornost věnuje superparamagnetickým nanočásticím oxidů železa, tzv. SPIONs (superparamagnetic iron oxide nanoparticles), které pod určitou hranicí velikosti (1–20 nm) vykazují jednodoménový charakter, který způsobuje jev zvaný superparamagnetismus. Vedle velikosti částic jsou důležité povrchové vlastnosti. Velikost povrchu (řádově 100 m2/g) umožňuje jeho modifikaci, čímž je zvýšena biokompatibilita částic a snížena toxicita. Magnetické nanočástice mají značný potenciál využití v biomedicínských aplikacích, a to zejména v oblasti teranostiky. V současnosti jsou nanočásticové systémy studovány zejména k zesílení kontrastu u zobrazovacích technik MRI, v pozitronové emisní tomografii, případně lze využít přeměny magnetické energie na energii tepelnou, čehož využívá metoda zvaná hypertermie. Další využití představuje separace, analýza buněk nebo značení buněk, které se zdá být slibné v oblasti zobrazovacích metod. Závěr: Jak se ukazuje, problematika uplatnění magnetických nanočástic v lékařství je rozsáhlá. Prvotní výzvou je syntéza těchto nanočástic, přičemž existuje řada postupů, které poskytují nanočástice o různých vlastnostech. Kvůli povaze nanočástic je také nutné věnovat velikou pozornost jejich stabilizaci, aby se předcházelo agregaci a v případě jejich použití jakožto nosiče je taktéž nutné vyřešit problém zachycení požadované látky. Tyto problémy jsou stále předmětem výzkumu, ale i přes tyto obtíže představují magnetické nanočástice potenciální mocný nástroj pro současnou diagnostiku a terapii.
Aim: Application of magnetic nanoparticles as multimodal materials for current diagnostics and therapy. Introduction: Rapid developments in nanotechnology have facilitated the emergence of new nanomaterials. This trend is also associated with an increased interest in nano and micro systems consisting of magnetic carriers. By combining a magnetic vector with a biologically active substance, unique properties can be achieved which can be used in many areas of biotechnology and medicine. Issues description: The most common materials are magnetic nanoparticles synthesised of iron oxides. Currently, widely studied are superparamagnetic iron oxide nanoparticles, socalled SPIONs, which below a certain size range (1–20 nm) exhibit a single-domain character, which causes a phenomenon called superparamagnetism. In addition to particle size, surface properties are important. The surface size (in the order of 100 m2/g) allows its modification, which increases the biocompatibility of particles and reduces toxicity. Magnetic nanoparticles have considerable potential for use in biomedical applications, especially in the field of teranostics. At present, nanoparticle systems are studied mainly as contrast agents in MR imaging techniques, in positron emission tomography, or the conversion of magnetic energy into thermal energy can be used, which uses a method called hyperthermia. Other uses include separation, cell analysis, or cell labeling, which appear promising in imaging methods. Conclusion: As shown, the application of magnetic nanoparticles in medicine is extensive. The primary challenge is the synthesis of these nanoparticles, and there are a number of processes that provide nanoparticles with different properties. Due to the nature of nanoparticles, the care must also be taken to stabilize them in order to prevent aggregation, and in the case of their use as carriers, it is also necessary to solve the problem of entrapment of the desired substance. These problems are still the subject of research, but despite these difficulties, magnetic nanoparticles are a potentially powerful tool for current diagnostics and therapy.
- MeSH
- indukovaná hypertermie MeSH
- kontrastní látky chemie terapeutické užití MeSH
- lidé MeSH
- magnetické nanočástice oxidů železa * chemie MeSH
- magnetické nanočástice chemie terapeutické užití MeSH
- magnetismus MeSH
- multimodální zobrazování MeSH
- pozitronová emisní tomografie MeSH
- teranostická nanomedicína MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- práce podpořená grantem MeSH
- přehledy MeSH
Cíl: Podrobnější přehled historie, současného stavu a nynějších trendů v získávání 68Ga, především z 68Ge/68Ga radionuklidového generátoru. Úvod: Pozitronová emisní tomografie (PET) je jednou z nejmodernějších metod nukleární medicíny. Stále nejhojněji využívaným radionuklidem při diagnostice pomocí PET je 18F, ale do popředí se dostávají i další pozitronové zářiče a velká pozornost je věnována právě 68Ga. Nespornou výhodou tohoto radionuklidu je způsob jeho získání. Oproti ostatním radionuklidům využívaným v PET diagnostice, které jsou připravovány téměř výhradně na cyklotronu, je 68Ga možné získat i pomocí radionuklidového generátoru, což výrazně zjednodušuje a urychluje další kroky jeho použití. Popis problematiky: Vývoj 68Ge/68Ga radionuklidových generátorů představoval komplexní výzkum separačních systémů, které jsou i dnes aktuálním tématem. V současnosti je dostupná řada separačních systémů, z nichž některé jsou již registrovány u Evropské agentury pro léčivé přípravky (EMA) či amerického Úřadu pro kontrolu potravin a léčiv (FDA) pro použití v humánní medicíně. Jiné jsou dostupné pouze pro výzkum a vývoj. S ohledem na technologické a legislativní těžkosti spojené s vývojem 68Ge/68Ga radionuklidového generátoru je navržení systému, který by poskytoval eluát 68Ga ve vhodné chemické formě a dostatečné radiochemické a radionuklidové čistotě, stále velkou výzvou a rozsáhlému studiu je věnována pozornost mnoha vědeckých týmů z celého světa. V České republice je dosud registrován jeden 68Ge/68Ga radionuklidový generátor a jeden kit pro značení 68Ga, SomaKit TOC pro diagnostiku neuroendokrinních tumorů (NET). Další kit, 68Ga-PSMA-11, je pak využíván pro diagnostiku karcinomu prostaty v rámci specifického léčebného programu. Ve světovém měřítku není však využití tohoto radionuklidu omezeno pouze na tyto aplikace a 68Ga je stále ve větší oblibě. Závěr: Rozsáhlé studie separačních systémů a cílících molekul by mohly v budoucnu vést u některých diagnostických procedur k nahrazení tradičního PET radionuklidu 18F právě 68Ga a to především díky možnosti eluce z radionuklidového generátoru.
Aim: Review of history, state of art and trends in gaining of 68Ga, especially from 68Ga/68Ge radionuclide generators. Introduction: Positron emission tomography (PET) is one of the most modern methods of nuclear medicine. Fluorine-18 is the most frequently used radionuclide for PET diagnostics, but there are other emerging radionuclides and the great attention is paid to 68Ga. The undeniable advantage of this radionuclide is its way of production. In contrast with other radionuclides for PET diagnostics almost exclusively prepared in the cyclotron, 68Ga can be gained also from a radionuclide generator which significantly simplifies and speeds up other steps of its use. Issue description: The development of 68Ge/68Ga radionuclide generators has been performed through the research of new separation systems which still remains a hot topic. Nowadays, the variety of separation systems is available. Some of them have a registration by European Medicines Agency (EMA) or American Food and Drug Administration (FDA) for use in human medicine. Others are suitable just for research and development. Regarding to technological and legislative difficulties connected with the development of 68Ge/68Ga radionuclide generator, the design of a system providing the eluate of 68Ga in convenient chemical form and sufficient radiochemical and radionuclide purity remains a great challenge and research teams around the world focus on the topic. Nowadays, there is one 68Ge/68Ga radionuclide generator and one kit for 68Ga labelling, SomaKit TOC, used for neuroendocrine tumours diagnostics registered in the Czech Republic. Other kit, 68Ga-PSMA-11, is used for diagnostics of prostate cancer in the specific treatment programme. However, the use of this radionuclide is not limited for these only applications and 68Ga enjoys the growing popularity in the world scale. Conclusion: Even though 18F remains the radionuclide of choice in PET, broad studies of separation systems and targeting molecules could lead to his replacement by 68Ga, mainly for the possibility of its elution from radionuclide generators.
- Klíčová slova
- gallium-68, germanium-68,
- MeSH
- pozitronová emisní tomografie * dějiny metody MeSH
- radioisotopové generátory * dějiny přístrojové vybavení MeSH
- radioizotopy galia * MeSH
- radionuklidy MeSH
- Publikační typ
- přehledy MeSH
Vzhledem k rostoucí incidenci gastroenteropankreatic- kých neuroendokrinních tumorů (GEP NET) jsou intenzivně hledány nové možnosti terapie. Konvenčními metodami terapie tohoto onemocnění stále zůstávají chirurgická léčba, radioterapie a u méně diferencovaných typů chemoterapie. V posledních dvou letech byla v ČR implementována nová terapeutická modalita nukleární medicíny [177 Lu]oxodotreo- tid, radiofarmakum vykazující vysokou afinitu vůči somato- statinovým receptorům typu 2 (SST2) zvýšeně exprimova- ným maligními buňkami GEP NET. Tato práce shrnuje nejdůležitější aspekty peptidové receptorové radioterapie pomocí [177 Lu]oxodotreotidu a první zkušenosti s tímto radiofarmakem v praxi v ČR, a to ve FN Motol.
The incidence of gastroenteropancreatic neuroendocrine tumors (GEP-NETs) leads to intensive research of new therapeutic modalities. Surgical therapy, radiotherapy and, for less differentiated types, chemotherapy are still the conventional methods of treatment. In the last two years, a new therapeutic modality of nuclear medicine used for palliative treatment has been implemented in the Czech Republic. It is [177 Lu]oxodotreotide, a radiopharmaceutical showing high affinity for somatostatin type 2 receptors (SST2) expressed by malignant GEP-NETs cells. This paper reviews the most important aspects of peptide receptor radiotherapy with [ 177 Lu]oxodotreotide and the first experience with this radiopharmaceutical in practise in the Czech Republic at the Motol University Hospital.
BACKGROUND: Prostate specific membrane antigen (PSMA) is a type II membrane protein widely expressed on the surface of prostate cancer cells. One of its functions is to act as a receptor mediating the ligand internalization. This PSMA property is employed in the diagnostics and therapy of prostate cancer. Over the years, small molecules with high affinity for PSMA have been developed and labelled with positron emitters (e.g. 68Ga, 18F, 11C, 64Cu, or 86Y). One of these radiolabelled ligands, [68Ga] PSMA-11, is one of the most widespread tracers for PET imaging of the prostate cancer. Many techniques have been proposed and tested for the 68Ga labelling of PSMA-11. The aim of our work was to design a labelling method of PSMA-11 that minimizes number of the used chemicals and steps, providing quantitative labelling yield at laboratory temperature and may be easily automated. METHODOLOGY: A68Ge/68Ga generator eluate in 0.1 M HCl was loaded on an activated Oasis MCX cartridge, and the cartridge was then thoroughly washed with water. The radionuclide 68Ga was eluted from the cartridge with 0.1 M NaHCO3 (pH = 8.5, n = 36) or with the same solution with pH adjusted to 7.2-9.0 (n = 38). Precursor PSMA-11 was mixed directly with the cartridge eluate of 68Ga in 0.1 M NaHCO3 of given pH. For the stability test, samples of 68GaPSMA-11 in 0.1 M NaHCO3 (pH 8.5) were mixed in ratio 1 : 1 with the following solutions: 0.1 M NaHCO3 (pH 8.5), human serum, PBS and 0.9% NaCl. In order to estimate an effect of the time elapsed between 68Ga elution from the cartridge in 0.1 M NaHCO3 (pH 8.5) and the labelling onset of PSMA-11, the latter was initiated 0, 5, 10 and 20 min post elution and radiochemical yield was monitored. All the PSMA-11 labelled samples were subjected to radiochemical purity test using HPLC. The whole process starting from generator elution up to HPLC analysis commencement took 10-15 min. RESULTS: Recovery of 68Ga from cartridge Oasis MCX using 0.1 M NaHCO3 at pH 8.5 was 71.5 ± 1.4%. Thirty six PSMA-11 samples (10 μg in reaction mixture) were labelled at pH 8.5 with total average radiochemical yield of 98 ± 2%. Recovery of 68Ga from cartridge Oasis MCX using 0.1 M NaHCO3 at variable pH of 7.2-9.0 was 62.5 ± 1.8% showing certain decrease with decreasing pH. A total of 138 samples of PSMA-11 were labelled with 68 Ga at variable pH (7.2-9.0) and four different amounts of PSMA-11 (1, 2.5, 5 and 10 μg) resulting in the labelling yields of 54.0 ± 5.3%, 88.2 ± 3.2%, 99.4 ± 0.3% and 99.9 ± 0.1%, respectively. Irrespective of the pH, the radiolabelling yield was quantitative for the molar ratio PSMA-11: 68Ga > 5000 : 1 in the reaction mixture. Stability tests in 0.1 M NaHCO3 (pH 8.5), human serum, PBS and 0.9% NaCl revealed no observable release of 68Ga from the 68Ga-PSMA-11 complex within 3 h. Similarly, the delay between the 68Ga elution from the Oasis MCX cartridge in 0.1 M NaHCO3 (pH 8.5) and start of the labelling of PSMA-11 labelling has no effect on the radiochemical yield. CONCLUSION: A new method of labelling PSMA-11 ligand with 68Ga in 0.1 M NaHCO3 using Oasis MCX cartridges was proposed, developed and tested. The results demonstrated that it is rapid, simple, reproducible and easy to automate.
- MeSH
- antigeny povrchové chemie MeSH
- chlornan sodný chemie MeSH
- glutamátkarboxypeptidasa II chemie MeSH
- lidé MeSH
- ligandy MeSH
- radioizotopy galia chemie MeSH
- reprodukovatelnost výsledků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Cíl: Podrobnější přehled historie, současného stavu a nynějších trendů v získávání 68Ga, především z 68Ge/68Ga radionuklidového generátoru. Úvod: Pozitronová emisní tomografie (PET) je jednou z nejmodernějších metod nukleární medicíny. Stále nejhojněji využívaným radionuklidem při diagnostice pomocí PET je 18F, ale do popředí se dostávají i další pozitronové zářiče a velká pozornost je věnována právě 68Ga. Nespornou výhodou tohoto radionuklidu je způsob jeho získání. Oproti ostatním radionuklidům využívaným v PET diagnostice, které jsou připravovány téměř výhradně na cyklotronu, je 68Ga možné získat i pomocí radionuklidového generátoru, což výrazně zjednodušuje a urychluje další kroky jeho použití. Popis problematiky: Vývoj 68Ge/68Ga radionuklidových generátorů představoval komplexní výzkum separačních systémů, které jsou i dnes aktuálním tématem. V současnosti je dostupná řada separačních systémů, z nichž některé jsou již registrovány u Evropské agentury pro léčivé přípravky (EMA) či amerického Úřadu pro kontrolu potravin a léčiv (FDA) pro použití v humánní medicíně. Jiné jsou dostupné pouze pro výzkum a vývoj. S ohledem na technologické a legislativní těžkosti spojené s vývojem 68Ge/68Ga radionuklidového generátoru je navržení systému, který by poskytoval eluát 68Ga ve vhodné chemické formě a dostatečné radiochemické a radionuklidové čistotě, stále velkou výzvou a rozsáhlému studiu je věnována pozornost mnoha vědeckých týmů z celého světa. V České republice je dosud registrován jeden 68Ge/68Ga radionuklidový generátor a jeden kit pro značení 68Ga, SomaKit TOC pro diagnostiku neuroendokrinních tumorů (NET). Další kit, 68Ga-PSMA-11, je pak využíván pro diagnostiku karcinomu prostaty v rámci specifického léčebného programu. Ve světovém měřítku není však využití tohoto radionuklidu omezeno pouze na tyto aplikace a 68Ga je stále ve větší oblibě. Závěr: Rozsáhlé studie separačních systémů a cílících molekul by mohly v budoucnu vést u některých diagnostických procedur k nahrazení tradičního PET radionuklidu 18F právě 68Ga a to především díky možnosti eluce z radionuklidového generátoru.
Aim: Review of history, state of art and trends in gaining of 68Ga, especially from 68Ga/68Ge radionuclide generators. Introduction: Positron emission tomography (PET) is one of the most modern methods of nuclear medicine. Fluorine-18 is the most frequently used radionuclide for PET diagnostics, but there are other emerging radionuclides and the great attention is paid to 68Ga. The undeniable advantage of this radionuclide is its way of production. In contrast with other radionuclides for PET diagnostics almost exclusively prepared in the cyclotron, 68Ga can be gained also from a radionuclide generator which significantly simplifies and speeds up other steps of its use. Issue description: The development of 68Ge/68Ga radionuclide generators has been performed through the research of new separation systems which still remains a hot topic. Nowadays, the variety of separation systems is available. Some of them have a registration by European Medicines Agency (EMA) or American Food and Drug Administration (FDA) for use in human medicine. Others are suitable just for research and development. Regarding to technological and legislative difficulties connected with the development of 68Ge/68Ga radionuclide generator, the design of a system providing the eluate of 68Ga in convenient chemical form and sufficient radiochemical and radionuclide purity remains a great challenge and research teams around the world focus on the topic. Nowadays, there is one 68Ge/68Ga radionuclide generator and one kit for 68Ga labelling, SomaKit TOC, used for neuroendocrine tumours diagnostics registered in the Czech Republic. Other kit, 68Ga-PSMA-11, is used for diagnostics of prostate cancer in the specific treatment programme. However, the use of this radionuclide is not limited for these only applications and 68Ga enjoys the growing popularity in the world scale. Conclusion: Even though 18F remains the radionuclide of choice in PET, broad studies of separation systems and targeting molecules could lead to his replacement by 68Ga, mainly for the possibility of its elution from radionuclide generators.
- MeSH
- germanium * MeSH
- izotopové značení MeSH
- lidé MeSH
- pozitronová emisní tomografie * dějiny trendy MeSH
- radioisotopové generátory * MeSH
- radioizotopy galia * MeSH
- radionuklidy * MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- přehledy MeSH
