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