Development of a 68 Ga-Fluorinated Porphyrin Complex as a Possible PET Imaging Agent
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ORIGINAL ARTICLE
Development of a 68Ga-Fluorinated Porphyrin Complex as a Possible PET Imaging Agent Yousef Fazaeli & Amir R. Jalilian & Mostafa M. Amini & Khosro Ardaneh & Ali Rahiminejad & Fatemeh Bolourinovin & Sedigheh Moradkhani & Abbas Majdabadi
Received: 11 July 2011 / Revised: 29 August 2011 / Accepted: 30 August 2011 / Published online: 16 December 2011 # Korean Society of Nuclear Medicine 2011
Abstract Aim Due to the interesting pharmacologic properties of porphyrins, the idea of developing a possible tumor imaging agent using PET by incorporating 68Ga into a suitable porphyrin ligand was investigated. Methods 68Ga-labeled 5,10,15,20-tetrakis(pentafluoro-13 phenyl) porphyrin (68Ga-TFPP) was prepared using freshly eluted [68Ga]GaCl3 obtained from a 68Ge/68Ga generator developed in-house and 5,10,15,20-tetrakis(pentafluorophenyl)porphyrin (H2TFPP) for 60 min at 100°C. Results The complex was prepared with high radiochemical purity (>99% ITLC, >99% HPLC, specific activity: 13–14 GBq/mmol). Stability of the complex was checked in the final formulation and in human serum for 5 h. The partition coefficient was calculated for the compound (log P = 0.62). The biodistribution of the labeled compound in vital organs of Swiss mice bearing fibrosarcoma tumors was studied Y. Fazaeli : K. Ardaneh : A. Rahiminejad : F. Bolourinovin : S. Moradkhani : A. Majdabadi Nuclear Medicine Research Group, Agricultural, Medical and Industrial Research School (AMIRS), Nuclear Science and Technology Research Institute (NSTRI), P.O.Box: 31485-498, Karaj, Iran A. R. Jalilian (*) Radiopharmaceutical Research and Development Lab, Nuclear Science and Technology Research Institute (NSTRI), P.O. Box:14395-836, Tehran, Iran e-mail: [email protected] M. M. Amini Department of Chemistry, Shahid Beheshti University, G.C., P.O. Box 19396–4716, Tehran, Iran
using scarification studies and SPECT imaging up to 1 h. The complex was mostly washed out from the circulation through kidneys and liver. The tumor-to-muscle ratio 1 h post injection was 5.13. Conclusion The radiolabeled porphyrin complex demonstrated potential for further imaging studies in other tumor models. Keywords Porphyrins . Ga-68 . Fibrosarcoma . Biodistribution . Co-incidence
Introduction Porphyrins are the focus of much attention because of their ability to mimic other chemicals in the human body, their ability to accumulate in many kinds of cancer cells, as well as their magnetic and optical properties. Photofrin has currently been approved for general use by licensing authorities for treatment of solid tumors and cancers. It makes use of photodynamic therapy (PDT), which uses a photochemical effect induced by light for treatment. Recently, meso-tetra (3-hydroxyphenyl)porphyrin was developed as one of the best tumor localizers and has also shown a favorable tissue distribution. These features make it useful in cancer medicine and photodynamic therapy [1, 2]. Various metal-porphyrin complexes have shown interesting tumor-avid activity in vitro and in vivo and have found their
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