Radiolabeling of new generation magnetic poly(HEMA-MAPA) nanoparticles with (131) I and preliminary investigation of its radiopharmaceutical potential using albino Wistar rats

• Published in: Journal of labelled compounds & radiopharmaceuticals 2013-12, Vol.56 (14), p.708-716
• Main Authors: Avcıbaşı, Uğur, Demiroğlu, Hasan, Ediz, Melis, Akalın, Hilmi Arkut, Özçalışkan, Emir, Şenay, Hilal, Türkcan, Ceren, Özcan, Yeşim, Akgöl, Sinan, Avcıbaşı, Nesibe
• Format: Article
• Language: English
• Subjects: Albinism; Animals; Iodine Radioisotopes - chemistry; Isotope Labeling; Magnetite Nanoparticles - chemistry; Phenylalanine - analogs & derivatives; Phenylalanine - chemistry; Polyhydroxyethyl Methacrylate - chemistry; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - pharmacokinetics; Rats; Rats, Wistar; Tissue Distribution
• ISSN: 1099-1344
• DOI: 10.1002/jlcr.3108

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 (131) I [(131) I-mag-poly(HEMA-MAPA)], and the radiopharmaceutical potential of (131) I-mag-poly(HEMA-MAPA) was investigated. Quality control studies were carried out by radiochromatographic method to be sure that (131) I binded to mag-poly(HEMA-MAPA) efficiently. In this sense, binding yield of (131) I-mag-poly(HEMA-MAPA) was found to be about 95-100%. In addition to this, optimum radiodination conditions for (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 (131) I-mag-poly(HEMA-MAPA) were realized. It was determined that lipophilicities of mag-poly(HEMA-MAPA) and (131) I-mag-poly(HEMA-MAPA) were 0.12 ± 0.01 and 1.79 ± 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 1440 min. It was found that (131) I-mag-poly(HEMA-MAPA) existed as a stable complex in rat serum within 60 min. After that, biodistribution and scintigraphy studies were carried out by using albino Wistar rats. It was determined that the most important (131) I activity uptake was observed in the breast, the ovary, and the pancreas. Scintigraphy studies well supported biodistribution results.