Asialoglycoprotein-receptor-targeted hepatocyte imaging using 99mTc galactosylated chitosan

Kim, Eun-Mi; Jeong, Hwan-Jeong; Kim, Se-Lim; Sohn, Myung-Hee; Nah, Jae-Woon; Bom, Hee-Seung; Park, In-Kyu; Cho, Chong-Su

doi:10.1016/j.nucmedbio.2006.03.005

« Previous Next »Nuclear Medicine and Biology
Volume 33, Issue 4 , Pages 529-534, May 2006

Asialoglycoprotein-receptor-targeted hepatocyte imaging using ^99mTc galactosylated chitosan

Eun-Mi Kim
- Department of Nuclear Medicine, Research Institute of Clinical Medicine, Chonbuk National University School of Medicine, Jeonju, Jeonbuk, Republic of Korea
Hwan-Jeong Jeong
- Department of Nuclear Medicine, Research Institute of Clinical Medicine, Chonbuk National University School of Medicine, Jeonju, Jeonbuk, Republic of Korea
- Corresponding author. Department of Nuclear Medicine, Chonbuk National University Hospital, Jeonju, Jellabuk-do 561-756, Republic of Korea. Tel.: +82 63 250 1674; fax: +82 63 250 1676.
Se-Lim Kim
- Department of Nuclear Medicine, Research Institute of Clinical Medicine, Chonbuk National University School of Medicine, Jeonju, Jeonbuk, Republic of Korea
Myung-Hee Sohn
- Department of Nuclear Medicine, Research Institute of Clinical Medicine, Chonbuk National University School of Medicine, Jeonju, Jeonbuk, Republic of Korea
Jae-Woon Nah
- Division of Applied Materials Engineering, Department of Polymer Science and Engineering, Sunchon National University, Sunchon, Jeonnam, Republic of Korea
Hee-Seung Bom
- Department of Nuclear Medicine, Chonnam National University School of Medicine, Gwangju, Republic of Korea
In-Kyu Park
- School of Agricultural Biotechnology, Seoul National University, Seoul, Republic of Korea
Chong-Su Cho
- School of Agricultural Biotechnology, Seoul National University, Seoul, Republic of Korea

Received 23 March 2005; received in revised form 13 March 2006; accepted 13 March 2006. published online 02 May 2006.

Abstract

This study investigated the usefulness of ^99mTc hydrazinonicotinamide-galactosylated chitosan (HGC) in hepatocyte imaging. HGC was obtained by coupling the galactose moiety of both lactobionic acid and succinimidyl 6-hydrazinonicotinate hydrochloride (succinimidyl HYNIC). The coupled product was then radiolabeled with ^99mTc using stannous chloride and tricine as reducing agent and coligand, respectively. Labeling efficiency was >90% both in room temperature and in serum up to 24 h after injection. The hepatic uptake properties of ^99mTc HGC were studied in Balb/C mice. ^99mTc HGC and ^99mTc hydrazinonicotinamide chitosan (HC) were intravenously injected into mice, with receptor binding identified by coinjection with 9 and 14 mg of free galactose. Images were acquired with a γ-camera. After injection via the tail vein of the mice, ^99mTc HGC showed high selectivity for the liver, while ^99mTc HC without a galactose group showed low liver uptake. In addition, the hepatic uptake of ^99mTc HGC was blocked by coinjection of free galactose. Tissue distribution was determined at three different times (10, 60 and 120 min). The liver accumulated 13.16±2.72%, 16.11±5.70% and 16.55±2.28% of the injected dose per gram at 10, 60 and 120 min after injection, respectively. ^99mTc HGC showed specific and rapid targeting of hepatocytes. It is a promising receptor-specific radiopharmaceutical with potential applications in liver imaging for the evaluation of hepatocytic function.

Keywords: ^99mTc, Galactosylated chitosan, Hepatocyte, Asialoglycoprotein receptor