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Stability of $^{188}Re$ Labeled Antibody for Radioimmunotherapy and the Effect of Stabilizing Agents  

Chang, Young-Soo (Department of Nuclear Medicine, Seoul National University College of Medicine)
Kim, Bo-Kwang (Department of Nuclear Medicine, Seoul National University College of Medicine)
Jeong, Jae-Min (Department of Nuclear Medicine, Seoul National University College of Medicine)
Chung, June-Key (Department of Nuclear Medicine, Seoul National University College of Medicine)
Lee, Seung-Jin (College of Pharmacy, Ewha Woman University)
Lee, Dong-Soo (Department of Nuclear Medicine, Seoul National University College of Medicine)
Lee, Myung-Chul (Department of Nuclear Medicine, Seoul National University College of Medicine)
Publication Information
The Korean Journal of Nuclear Medicine / v.36, no.3, 2002 , pp. 195-202 More about this Journal
Abstract
Purpose: For clinical application of beta-emitter labeled antibody, high specific activity is imporiant. Carrier-free $^{188}Re$ from $^{188}W/^{188}Re$ generator is an ideal radionuclide for this purpose. However, low stability of $^{188}Re$ labeled antibody, especially in high specific activity, due to radiolytic decomposition by high energy (2.1 MeV) beta ray was problem. We studied the stability of $^{188}Re$ labeled antibody, and stabilizing effect of several stabilizers. Materials and Methods: Pre-reduced monoclonal antibody (CEA79.4) was labeled with $^{188}Re$ by incubating with generator-eluted $^{188}Re-perrhenate$ in the presence of stannous tartrate for 2 hr at room temperature. Radiochemical purity of each preparation was determined by chromatography. Human serum albumin was added to the labeled antibodies (2%). Stability of $^{188}Re-CEA79.4$ was investigated in the presence of ascorbic acid, ethanol, of Tween 80 as stabilizing agents. Results: Labeling efficiencies were $88{\pm}4%\;(n=12)$. Specific activities of $1.25{\sim}4.77MBq/{\mu}g$ were obtained. If stored after purging with $N_2$, all the preparations were stable for 10 hr. However, stability decreased in the presence of air. Perrhenate and $^{188}Re-tartrate$ was major impurity in declined preparation. colloid-formation was not a significant problem in all cases. Addition of ascorbic acid stabilized the labeled antibodies either under $N_2$ or under air by reducing the formation of perrhenate. Conclusion: High specific activity $^{188}Re$ labeled antibody is unstable, especially, in the presence of oxygen. Addition of ascorbic acid increased the stability.
Keywords
Antibody; Stability; $^{188}Re$; Ascorbic acid;
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