Radiolabeling of new generation magnetic poly(HEMA-MAPA) nanoparticles with super(131)I and preliminary investigation of its radiopharmaceutical potential using albino Wistar rats
In this study, N-methacryloyl-l-phenylalanine (MAPA) containing poly(2-hydroxyethylmethacrylate) (HEMA)-based magnetic poly(HEMA-MAPA) nanobeads [mag-poly(HEMA-MAPA)] were radiolabeled with super(131)I [ super(131)I-mag-poly(HEMA-MAPA)], and the radiopharmaceutical potential of super(131)I-mag-poly(...
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Veröffentlicht in: | Journal of labelled compounds & radiopharmaceuticals 2013-12, Vol.56 (14), p.708-716 |
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Sprache: | eng |
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Zusammenfassung: | In this study, N-methacryloyl-l-phenylalanine (MAPA) containing poly(2-hydroxyethylmethacrylate) (HEMA)-based magnetic poly(HEMA-MAPA) nanobeads [mag-poly(HEMA-MAPA)] were radiolabeled with super(131)I [ super(131)I-mag-poly(HEMA-MAPA)], and the radiopharmaceutical potential of super(131)I-mag-poly(HEMA-MAPA) was investigated. Quality control studies were carried out by radiochromatographic method to be sure that super(131)I binded to mag-poly(HEMA-MAPA) efficiently. In this sense, binding yield of super(131)I-mag-poly(HEMA-MAPA) was found to be about 95-100%. In addition to this, optimum radiodination conditions for super(131)I-mag-poly(HEMA-MAPA) were determined by thin-layer radiochromatography studies. In addition to thin-layer radiochromatography studies, lipophilicity (partition coefficient) and stability studies for super(131)I-mag-poly(HEMA-MAPA) were realized. It was determined that lipophilicities of mag-poly(HEMA-MAPA) and super(131)I-mag-poly(HEMA-MAPA) were 0.12 plus or minus 0.01 and 1.79 plus or minus 0.76 according to ACD/logP algorithm program, respectively. Stability of the radiolabeled compound was investigated in time intervals given as 0, 30, 60, 180, and 1440min. It was found that super(131)I-mag-poly(HEMA-MAPA) existed as a stable complex in rat serum within 60min. After that, biodistribution and scintigraphy studies were carried out by using albino Wistar rats. It was determined that the most important super(131)I activity uptake was observed in the breast, the ovary, and the pancreas. Scintigraphy studies well supported biodistribution results. Copyright copyright 2013 John Wiley & Sons, Ltd. In the current study, we have synthesized novel magnetic poly(HEMA-MAPA) nanobeads and radiolabeled them with super(131)I using iodogen method for the first time in the literature. Accumulation of the labeled compound in albino Wistar rat metabolism was investigated with imaging and biodistributional studies. We have observed that super(131)I-mag-poly(HEMA-MAPA) showed specifity in the breast, the ovary, and the pancreas. Thus, this novel nanostructure, labeled with super(131)I, may be proposed as an imaging or therapeutic agent for various cancers related with these organs. |
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ISSN: | 0362-4803 1099-1344 |
DOI: | 10.1002/jlcr.3108 |