preparation of a 153sm-5,10,15,20-tetrakis(4-methoxyphenyl) porphyrin complex as a possible therapeutic agent
نویسندگان
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.
منابع مشابه
Preparation of a 153Sm-5,10,15,20-tetrakis(4-methoxyphenyl) porphyrin complex as a possible therapeutic agent
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 ...
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عنوان ژورنال:
iranian journal of nuclear medicineناشر: tehran university of medical sciences
ISSN 1681-2824
دوره 23
شماره 2 2015
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