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

Abstract

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

Keywords: PET; asialoglycoprotein receptor; gallium-68; hexavalent lactoside; liver.