'In-house' preparation of 99mTc-EDDA/HYNIC-TOC, a specific targeting agent for somatostatin receptor scintigraphy
| Autor: | Sonja Kuzmanovska, Olivija Vaskova, Marina Zdraveska Kocovska |
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| Jazyk: | angličtina |
| Rok vydání: | 2012 |
| Předmět: | |
| Zdroj: | Makedonsko Farmacevtski Bilten, Vol 57, Iss (1, 2), Pp 65-70 (2012) |
| Druh dokumentu: | article |
| ISSN: | 1409-8695 1857-8969 |
| Popis: | The use of radiolabeled peptide ligands as diagnostics and therapeutics in nuclear oncology has increased recently. One of the most frequently used radiopharmaceutical is 99mTc-EDDA/HYNIC-TOC, a somatostatin analog with affinity for certain types of somatostatin receptors, overexpressed in tumors of neuroendocrine origin. The radiopharmaceutical is not readily available; therefore we introduced its “in house” preparation within project activities supported by the International Atomic Energy Agency (IAEA). We optimized the radiolabeling protocol, prepared a small batch of frozen kits, performed ITLC quality control and animal biodistribution during the preclinical evaluation procedures. The co-ligand exchange labeling procedure was carried out at 100°C during 10 min, resulting in radiochemical purity >90%. The biodistribution scintigrams in normal Wistar rats showed rapid blood clearance after 15 min and predominant kidney accumulation after 4 h, in accordance with the data reported by other authors. Storage stability of the formulated small batch frozen kit (-20°C) was evaluated within 6 months, with radiolabeling yield ranging between 94,3% and 96,9%. We conclude that frozen kit can be a safe alternative to the freeze-dried for small batch in house production, and after the satisfactory preclinical evaluation, the “in house” prepared 99mTc-EDDA/ HYNIC-TOC can be introduced in clinical practice as specific targeting agent for somatostatin receptor scintigraphy. |
| Databáze: | Directory of Open Access Journals |
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