Biodistribution and radiation dosimetry of radioiodinated hypericin as a cancer therapeutic

International Journal of Oncology
Marlein Miranda ConaYicheng Ni

Abstract

Iodine-131‑labeled monoiodohypericin (131I‑Hyp) is a necrosis avid compound used as a complementary anticancer agent. Herein, the biodistribution in rats with re-perfused partial liver infarction (RPLI) was used to estimate its human internal radiation dosimetry. Iodine-123‑labeled monoiodohypericin (123I-Hyp) as a safer surrogate for 131I-Hyp was prepared with iodogen as oxidant. Determination of radiochemical yield and purification was performed by high performance liquid chromatography (HPLC). To control aggregation, the formulation was macroscopically and microscopically examined. Biodistribution of 123I-Hyp was studied in RPLI rats (n=18) at 4, 24 and 48 h post-injection. Tissue gamma counting (TGC), autoradiography and histology were performed. Dosimetry of 131I-Hyp in hepatic necrosis and in normal human organs was estimated using biodistribution data of 123I-Hyp, the Organ Level Internal Dose Assessment/Exponential Modeling (OLINDA/EXM®), a sphere model and male and female phantoms. A radiochemical yield of 95% was achieved in labeling of 123I-Hyp with a radiochemical purity of 99% after HPLC purification. In the Hyp added formulation, no macroscopic but minimal microscopic aggregation was observed. By TGC, selective ac...Continue Reading

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