Korean J Nucl Med.  2004 Jun;38(3):253-258.

Nuclear Imaging Evaluation of Galactosylation of Chitosan

Affiliations
  • 1Department of Nuclear Medicine, Wonkwang University School of Medicine, Iksan, Korea. leokim@wonkwang.ac.kr
  • 2Wonkwnag Institute of Medical Science, Iksan, Korea. leokim@wonkwang.ac.kr
  • 3School of Agricultural Biotechnology, Seoul National University, Seoul, Korea.
  • 4Department of Nuclear Medicine, Chonnam National University School of Medicine, Gwang-ju, Korea.

Abstract

PURPOSE
Chitosan has been studied as a non-viral gene delivery vector, drug delivery carrier, metal chelater, food additive, and radiopharmaceutical, among other things. Recently, galactose-graft chitosan was studied as a non-viral gene and drug delivery vector to target hepatocytes. The aim of this study was to investigate the usefulness of nuclear imaging for in vivo evaluation of targeting the hepatocyte by galactose grafting. METHODS AND MATERIALS: Galactosyl methylated chitosan (GMC) was produced by methylation to lactobionic acid coupled chitosan. Cytotoxicity of 99mTc-GMC was determined by MTT assay. Rabbits were injected via their auricular vein with 99mTc-GMC and 99mTc-methylated chitosan (MC), the latter of which does not contain a galactose group, and images were acquired with a gamma camera equipped with a parallel hole collimator. The composition of the galactose group in galactosylated chitosan (GC), as well as the tri-, di-, or mono-methylation of GMC, was confirmed by NMR spectroscopy. RESULTS: The results of MTT assay indicated that 99mTc-GMC was non-toxic. 99mTc-GMC specifically accumulated in the liver within 10 minutes of injection and maintained high hepatic uptake. In contrast, 99mTc-MC showed faint liver uptake. 99mTc-GMC scintigraphy of rabbits showed that the galactose ligand principally targeted the liver while the chitosan functionalities led to excretion through the urinary system. CONCLUSION: Bioconjugation with a specific ligand endows some degree of targetability to an administered molecule or drug, as in the case of galactose for hepatocyte in vivo, and evaluating said targetabililty is a clear example of the great benefit proffered by nuclear imaging.

Keyword

99mTc; hepatocyte-targeted; nuclear imaging; galactosylated chitosan

MeSH Terms

Chitosan*
Food Additives
Galactose
Gamma Cameras
Hepatocytes
Liver
Magnetic Resonance Spectroscopy
Methylation
Rabbits
Radionuclide Imaging
Transplants
Veins
Chitosan
Food Additives
Galactose
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