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KMID : 1145520180040010003
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Journal of Radiopharmaceuticals and Molecular Probes
2018 Volume.4 No. 1 p.3 ~ p.10
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Direct radio-iodination of folic acid for targeting folate receptor-positive tumors
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Huynh Phuong Tu
Lee Woong-Hee
Ha Yeong-Su
Yoo Jeong-Soo
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Abstract
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The folate receptor (FR) is a promising cell membrane-associated target for nuclear imaging of various cancers (via imaging FR-α) and potentially also inflammatory diseases (via imaging FR-β), through the use of folic acid-based radioconjugates. However, there have been several drawbacks of previously reported radioconjugates, such as a short half-life of the radiolabel (68Ga t1/2 68 min), a complex and time-consuming multistep radiosynthesis, and a high renal uptake of radiolabeled folate derivatives. The goal of this study was to develop an imaging probe by directly labeling folate with radioactive iodine without using an extra prosthetic group. The radiolabeling of folate was optimized using various labeling conditions and the labeled tracers were isolated by high-performance liquid chromatography. The in vitro stability of labeled folate was checked in phosphate-buffered saline and serum. The tumor-targeting efficacy of the probe was also evaluated by biodistribution studies using a murine 4T1 tumor model.
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KEYWORD
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Folic acid, radioiodination, tumor targeting
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