Development of single vial kits for preparation of 68 Ga-labelled hexavalent lactoside for PET imaging of asialoglycoprotein receptor.

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-68-labeled glycoligand for PET imaging of the asialoglycoprotein receptor (ASGPR). (GaCl3)-Ga-68 was obtained from a commercial Ge-68/Ga-68 generator. Single-vial kits of HL were formulated. Optimization of radiolabeling with Ga-68, various evaluations of NOTA-HL kits, and in vitro stability study of Ga-68-HL were carried out. PET/CT imaging of normal mice injected with Ga-68-NOTA-HL was performed. NOTA-HL kit was successfully formulated. High radiochemical yields (>95%) were obtained by Ga-68 radiolabeling. The NOTA-HL kits were stable for at least 12months, and Ga-68-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-68 labeling. Ga-68-NOTA-HL showed high specific uptake in liver. The availability of ready-to-use NOTA-HL kits combined with Ge-68/Ga-68 generators would provide an efficient approach for PET imaging of ASGPR.