Preparation of a 153Sm-5,10,15,20-tetrakis(4-methoxyphenyl) porphyrin complex as a possible therapeutic agent
- سال انتشار: 1394
- محل انتشار: مجله پزشکی هسته ای ایران، دوره: 23، شماره: 2
- کد COI اختصاصی: JR_IRJNM-23-2_002
- زبان مقاله: انگلیسی
- تعداد مشاهده: 356
نویسندگان
Department of Radiopharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
Radiopharmacy Research Group, Radiation Application Research School, Nuclear Science and Technology Research Institute, Tehran, Iran
Radiopharmacy Research Group, Radiation Application Research School, Nuclear Science and Technology Research Institute, Tehran, Iran
Radiopharmacy Research Group, Radiation Application Research School, Nuclear Science and Technology Research Institute, Tehran, Iran
چکیده
Introduction: Porphyrins are interesting derivatives with low toxicity, tumor avidity and rapid wash-out suggested as potential radiopharmaceuticals in radiolabeled form. In this work we report, synthesis, radiolabeling, quality control, stability, partition coefficient determination and biodistribution studies of 153Sm-5,10,15,20-tetrakis(4-methoxyphenyl) porphyrin (153Sm-4-MPP) in wild-type rats. Methods: [153Sm]-4MPP was prepared using [153Sm]SmCl3 and 5,10,15,20-tetrakis(4-methoxyphenyl) porphyrin (H2-4MPP) for 18 h at 80-90°C. Stability of the complex was checked in final formulation and in presence of human serum for 24 h. The biodistribution of the labeled compound in vital organs of wild-type rats was studied. A detailed comparative pharmacokinetic study performed for 153Sm cation and [153Sm]-4-MPP up to 24h. Results: The radiochemical purity of [153Sm]-4MPP was reported > 97±2% and > 99±0.5% by ITLC and HPLC, respectively. The specific activity was 220-230 MBq/mmol. The calculated partition coefficient for the compound was (log P=-1.09). The complex is mostly cleared from the circulation through kidneys and liver. The kidney:blood and kidney:muscle ratios 24 h post injection were 14.75 and 42.4, respectively. kidney/liver ratio was almost constant at all time intervals (0.6). Conclusion: [153Sm]-4MPP was prepared at the optimized conditions and suitable characteristics. Further investigations such as biological studies of this agent on tumor-bearing models are needed.کلیدواژه ها
Porphyrins, quality control, Sm-15, Biodistributionاطلاعات بیشتر در مورد COI
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