Development of single vial kits for preparation of ⁶⁸Ga‐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 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.

Transcriptomically Revealed Oligo-Fucoidan Enhances the Immune System and Protects Hepatocytes via the ASGPR/STAT3/HNF4A Axis

“…The animals were fed ad libitum. The 68 Ga-NOTA-HL ( 68 Ga-2,2’,2’’-(1,4,7-triazonane-1,4,7-triyl) triacetic acid-hexavalent lactoside) was synthesized by the Institute of Nuclear Energy Research (Atomic Energy Council, Yonghe Dist., New Taipei City, Taiwan) and was capable of binding to ASGPR in the body [ 27 ], which could be considered as the ligand for ASGPR. To confirm whether OF binds to ASGPR on hepatocytes in vivo, 100 mg OF and PBS was administrated respectively 1 h prior to the 68 Ga-NOTA-HL intravenous injection.…”

Low molecular weight fucoidan inhibits hepatocarcinogenesis and nonalcoholic fatty liver disease in zebrafish via ASGR/STAT3/HNF4A signaling

“…The in vivo competition assay was performed by using adult Balb/c mice and the 68 Ga‐NOTA‐hexavalent lactoside (HL) which was capable of binding to ASGR in the body, 38 as described previously 30 …”

“…The in vivo competition assay was performed by using adult Balb/c mice and the 68 Ga-NOTA-hexavalent lactoside (HL) which was capable of binding to ASGR in the body, 38 as described previously. 30 For time-dependent analysis of in vivo competition assay under the presence of OF, 100 mg OF was intravenously prescribed 1 hour prior to 68 Ga-NOTA-HL injection.…”

Recent Breakthrough in 68Ga-Radiopharmaceuticals Cold Kits for Convenient PET Radiopharmacy

“…Yu et al studied hexavalent lactose (HL) having high affinity toward asialoglycoprotein receptor (ASGPR) associated with chronic liver diseases (hepatitis, cirrhosis, and carcinoma). They developed single vial NOTA-HL cold kits for rapid preparation of 68 Ga-NOTA-HL . Constituents of kits were lactoside (40 μg), 1 M sodium acetate, and mannitol and were formulated with 68 GaCl 3 eluted in 0.1 N HCl (Eckert & Zeigler).…”