Development and evaluation of a 166holmium labelled porphyrin complex as a possible therapeutic agent View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2013-02

AUTHORS

Nassim Vahidfar, Amir R. Jalilian, Yousef Fazaeli, Ali Bahrami-Samani, Davood Beiki, Ali Khalaj

ABSTRACT

Porphyrins are interesting derivatives with low toxicity, tumor avidity and rapid wash-out suggested as potential radiopharmaceuticals in radiolabeled form. In this work, [166Ho] labeled 5,10,15,20-tetrakis(phenyl) porphyrin ([166Ho]-TPP) was prepared using [166Ho]HoCl3 and 5,10,15,20-tetrakis(phenyl)porphyrin (H2TPP) for 12 h at 50 °C (radiochemical purity: >95 ± 2 % ITLC, >99 ± 0.5 % HPLC, specific activity: 0.9–1.1 GBq/mmol). Stability of the complex was checked in final formulation and human serum for 48 h. The partition coefficient was calculated for the compound (log P = 2.01). The biodistribution of the labeled compound in vital organs of wild-type rats was studied using scarification studies and SPECT. A detailed comparative pharmacokinetic study performed for 166Ho cation and [166Ho]-TPP performed up to 24 h. The complex is mostly washed out from the circulation through kidneys and in less extends from the liver. The kidney:blood, kidney:liver and kidney:muscle ratios 4 h post injection were 14, 3.6 and 7.38 respectively. More... »

PAGES

979-986

References to SciGraph publications

  • 2005-08. Biodistribution and excretion of radioactivity after the administration of 166Ho-chitosan complex (DW-166HC) into the prostate of rat in EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
  • 2011-04. Preparation and preliminary evaluation of [67Ga]-tetra phenyl porphyrin complexes as possible imaging agents in JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
  • 2000-06. Treatment of Bowen’s disease with a specially designed radioactive skin patch in EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
  • 2010-04. Studies on the porphine labeled with 99mTc–pertechnetate in JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
  • 2005-05. Preparation of [66Ga]bleomycin complex as a possible PET radiopharmaceutical in JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
  • 1992. Synthesis and Properties of Tetrakis-Carborane-Carboxylate Esters of 2,4-BIS-(α,β-Dihydroxyethyl) Deuteroporphyrin IX in PROGRESS IN NEUTRON CAPTURE THERAPY FOR CANCER
  • 1979-03. The kinetics of incorporation of111In into m-tetraphenylporphine in JOURNAL OF RADIOANALYTICAL CHEMISTRY
  • Identifiers

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    http://scigraph.springernature.com/pub.10.1007/s10967-012-2034-1

    DOI

    http://dx.doi.org/10.1007/s10967-012-2034-1

    DIMENSIONS

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