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Paper Information

Journal:   IRANIAN JOURNAL OF NUCLEAR MEDICINE   SUMMER 2015 , Volume 23 , Number 2 (SERIAL NUMBER 44); Page(s) 65 To 72.
 
Paper: 

PREPARATION OF A 153SM-5, 10, 15, 20-TETRAKIS (4-METHOXYPHENYL) PORPHYRIN COMPLEX AS A POSSIBLE THERAPEUTIC AGENT

 
 
Author(s): 
 
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Abstract: 

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 80-90oC. 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.

 
Keyword(s): PORPHYRINS, QUALITY CONTROL, SM-15, BIODISTRIBUTION
 
 
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