Automated synthesis of [(68)Ga]oxine, improved preparation of (68)Ga-labeled erythrocytes for blood-pool imaging, and preclinical evaluation in rodents

[(68)Ga]oxine 的自动化合成、用于血池成像的 (68)Ga 标记红细胞的改进制备以及啮齿动物的临床前评估

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Abstract

Radiolabeled erythrocytes have multiple applications in nuclear medicine, including blood pool imaging. Historically they have been labeled with SPECT radionuclides. A PET blood pool imaging agent is highly desirable as it would improve clinical applications with better image quality and resolution, higher sensitivity, and dynamic scanning capabilities. With the coming of age of modern (68)Ge/(68)Ga generator systems, gallium-68 is now widely accessible. In this paper we describe an updated method for the preparation of (68)Ga-labeled erythrocytes and their preliminary use in rodent blood pool imaging. A novel automated synthesis of [(68)Ga]oxine using a (68)Ga/(68)Ge generator and automated synthesis module is reported. [(68)Ga]Oxine was synthesized in 50 ± 5% (n = 3) non-decay corrected radiochemical yield and >99% radiochemical purity. Rat and human erythrocytes were successfully labeled with the complex in 42% RCY, and the (68)Ga-labeled erythrocytes have been shown to clearly image the blood pool in a healthy rat. Human erythrocytes labelled with [(68)Ga]oxine were shown to be viable up to 2 hours post-labelling, and washout of the radiolabel was minimal up to 1 hour post-labelling. Further optimization of the labeling method to translate for use in human cardiac and oncologic blood pool PET imaging studies, is underway.

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