Development of Single Vial Kits for Preparation of 68 Ga-Labelled Hexavalent Lactoside for PET Imaging of Asialoglycoprotein Receptor

• Published in: Journal of labelled compounds & radiopharmaceuticals 2018-10, Vol.61 (12), p.885-894
• Main Authors: Yu, Hung-Man, Chan, Chen-Hsin, Chen, Chun-Hung, Chien, Chuan-Yi, Wang, Ping-Yen, Juan, Wei-Cheng, Yang, Chun-Hung, Hsia, Hao-Ting, Wang, Mei-Hui, Lin, Wuu-Jyh
• Format: Article
• Language: English
• ISSN: 0362-4803; 1099-1344
• DOI: 10.1002/jlcr.3673

The aim of this study was to formulate and evaluate the freeze-dried kit of NOTA-hexavalent lactoside (NOTA-HL) for the preparation of Ga-labeled glycoligand for PET imaging of the asialoglycoprotein receptor (ASGPR). GaCl was obtained from a commercial Ge/ Ga generator. Single-vial kits of HL were formulated. Optimization of radiolabeling with Ga, various evaluations of NOTA-HL kits and in vitro stability study of Ga-HL were carried out. PET/CT imaging of normal mice injected with Ga-NOTA-HL was performed. NOTA-HL kit was successfully formulated. High radiochemical yields (>95%) were obtained by Ga radiolabeling. The NOTA-HL kits were stable for at least 12 months and Ga-NOTA-HL exhibited good in vitro stability. PET studies in normal mice revealed high specific accumulation of activity in the liver. The NOTA-HL kit was developed for fast Ga labeling. Ga-NOTA-HL showed high specific uptake in liver. The availability of ready-to-use NOTA-HL kits combined with Ge/ Ga generators would provide an efficient approach for PET imaging of ASGPR.