Kaohsiung Journal of Medical Sciences
Volume 24, Issue 1 , Pages 1-9, January 2008

Evaluation of Tc-99m (V) DMSA Binding to Human Plasma Proteins

  • Bi-Fang Lee

      Affiliations

    • Department of Nuclear Medicine, National Cheng Kung University Hospital, Tainan, Taiwan
    • Corresponding Author InformationAddress correspondence and reprint requests to: Dr Bi-Fang Lee, Department of Nuclear Medicine, National Cheng Kung University Hospital, 138 Sheng-Li Road, Tainan 704, Taiwan
    • ,
  • Jwu-Lai Yeh

      Affiliations

    • Department of Pharmacology, Kaohsiung Medical University, Kaohsiung, Taiwan
    • ,
  • Nan-Tsing Chiu

      Affiliations

    • Department of Nuclear Medicine, National Cheng Kung University Hospital, Tainan, Taiwan
    • ,
  • Gin-Chung Liu

      Affiliations

    • Department of Radiology, Kaohsiung Medical University, Kaohsiung, Taiwan
    • ,
  • Hsin-Su Yu

      Affiliations

    • Institute of Graduate Medicine, Kaohsiung Medical University, Kaohsiung, Taiwan
    • ,
  • Mei-Hui Wang

      Affiliations

    • Institute of Nuclear Energy, Lungtan, Taiwan
    • ,
  • Lie-Hang Shen

      Affiliations

    • Institute of Nuclear Energy, Lungtan, Taiwan

Received 2 May 2007; accepted 14 October 2007.

Article Outline

As a critical step toward elucidating the mechanism of localization of Tc-99m (V) dimercaptosuccinic acid (DMSA), we investigated its binding and transport in blood in comparison with Ga-67 citrate. The studies were performed in vitro by incubating Tc-99m (V) DMSA with blood (one sample at 4°C and another at 37°C) to assess its binding to plasma proteins using ulrrafilrration, dialysis, electrophoresis, gel filtration chromatography and affinity chromatography A parallel experiment for determining the blood binding of Ga-67 citrate was performed using the same procedures. Using ulrrafilrration, dialysis, electrophoresis and gel filtration chromatography, labeled plasma samples showed that protein binding for Tc-99m (V) DMSA was 45-54% at 37°C and 73-80% at 4°C. The figures for Ga-67 citrate were 43-53% at 37°C and 75-81% at 4°C. Electrophoresis showed that Tc-99m (V) DMSA was mostly bound to plasma albumin (36.05 + 2.48% at 37°C and 60.04 + 1.87% at 4°C), and that the proportion of Ga-67 radioactivity associated with β-globulin was 34.23 + 1.37% at 37°C and 55.71 + 3.69% at 4°C. In affinity chromatography experiments, Tc-99m (V) DMSA did not bind to transferrin, unlike Ga-67 citrate. This study demonstrates that, at the radiopharmaceutical tracer level, most Tc-99m (V) DMSA in blood is protein-bound, primarily to albumin, but not to transferrin. In contrast, Ga-67 citrate was bound primarily to transferrin. The knowledge that albumin is the main transport protein of Tc-99m (V) DMSA may contribute to a better understanding of its biodistribution and pharmacokinetics.

Key Words:  albumin , Ga-67 citrate , plasma proteins , Tc-99m (V) DMSA , transferrin

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PII: S1607-551X(08)70066-4

doi:10.1016/S1607-551X(08)70066-4

Kaohsiung Journal of Medical Sciences
Volume 24, Issue 1 , Pages 1-9, January 2008

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