干旱区生态环境知识资源中心(Arid): Simple new method for labelling of PSMA-11 with Ga-68 in NaHCO3

Arid

DOI	10.1016/j.apradiso.2021.109692
	Simple new method for labelling of PSMA-11 with Ga-68 in NaHCO3
	Urbanova, Kamila; Seifert, Daniel; Vinsova, Hana; Vlk, Martin; Lebeda, Ondrej
通讯作者	Lebeda, O (corresponding author), CAS, Nucl Phys Inst, Husinec Rez 130, Rez 25068, Czech Republic.
来源期刊	APPLIED RADIATION AND ISOTOPES
ISSN	0969-8043
EISSN	1872-9800
出版年	2021
卷号	172
英文摘要	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. Ga-68, F-18, C-11, Cu-64, or Y-86). One of these radiolabelled ligands, [Ga-68] 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 Ga-68 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: A Ge-68/Ga-68 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 Ga-68 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 PSMA11 was mixed directly with the cartridge eluate of Ga-68 in 0.1 M NaHCO3 of given pH. For the stability test, samples of (68)GaPSMA-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 Ga-68 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 radio-chemical 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 Ga-68 from cartridge Oasis MCX using 0.1 M NaHCO3 at pH 8.5 was 71.5 +/- 1.4%. Thirty six PSMA-11 samples (10 mu g in reaction mixture) were labelled at pH 8.5 with total average radiochemical yield of 98 +/- 2%. Recovery of Ga-68 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 Ga-68 at variable pH (7.2-9.0) and four different amounts of PSMA-11 (1, 2.5, 5 and 10 mu g) 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: Ga-68 > 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 Ga-68 from the Ga-68-PSMA-11 complex within 3 h. Similarly, the delay between the Ga-68 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 Ga-68 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.
英文关键词	PSMA-11 Ga-68 NaHCO3 Labelling methods
类型	Article
语种	英语
收录类别	SCI-E
WOS记录号	WOS:000640178800030
WOS关键词	POSITRON-EMISSION-TOMOGRAPHY ; PROSTATE-CANCER ; PET/CT ; LIGAND ; CHELATORS
WOS类目	Chemistry, Inorganic & Nuclear ; Nuclear Science & Technology ; Radiology, Nuclear Medicine & Medical Imaging
WOS研究方向	Chemistry ; Nuclear Science & Technology ; Radiology, Nuclear Medicine & Medical Imaging
资源类型	期刊论文
条目标识符	http://119.78.100.177/qdio/handle/2XILL650/349495
作者单位	[Urbanova, Kamila; Seifert, Daniel; Vinsova, Hana; Lebeda, Ondrej] Czech Acad Sci, Nucl Phys Inst, Dept Radiopharmaceut, Rez, Czech Republic; [Urbanova, Kamila; Vlk, Martin] Czech Tech Univ, Fac Nucl Sci & Phys Engn, Dept Nucl Chem, Prague, Czech Republic
推荐引用方式 GB/T 7714	Urbanova, Kamila,Seifert, Daniel,Vinsova, Hana,et al. Simple new method for labelling of PSMA-11 with Ga-68 in NaHCO3[J],2021,172.
APA	Urbanova, Kamila,Seifert, Daniel,Vinsova, Hana,Vlk, Martin,&Lebeda, Ondrej.(2021).Simple new method for labelling of PSMA-11 with Ga-68 in NaHCO3.APPLIED RADIATION AND ISOTOPES,172.
MLA	Urbanova, Kamila,et al."Simple new method for labelling of PSMA-11 with Ga-68 in NaHCO3".APPLIED RADIATION AND ISOTOPES 172(2021).