Radioiodinated Hypericin: Its Biodistribution, Necrosis Avidity and Therapeutic Efficacy are Influenced by Formulation |
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Authors: | Marlein Miranda Cona Yeranddy Aguiar Alpizar Junjie Li Matthias Bauwens Yuanbo Feng Ziping Sun Jian Zhang Feng Chen Karel Talavera Peter de Witte Alfons Verbruggen Raymond Oyen Yicheng Ni |
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Institution: | 1. Department of Imaging & Pathology, Faculty of Medicine Biomedical Sciences Group, KU Leuven, Herestraat 49, Leuven, Belgium 2. Molecular Small Animal Imaging Centre/MoSAIC, Faculty of Medicine Biomedical Sciences Group, KU Leuven, Herestraat 49, Leuven, Belgium 3. Laboratory of Ion Channel Research, Department of Cellular and Molecular Medicine, KU Leuven Herestraat 49, Leuven, Belgium 4. Faculty of Pharmaceutical Sciences, Biomedical Sciences Group, KU Leuven, Herestraat 49, Leuven, Belgium 5. Radiopharmacy Laboratory, Shandong Academy of Medical Sciences, Jinan, 250062, China 6. Laboratory of Translational Medicine, Jiangsu Academy of Traditional Chinese Medicine, Nanjing, 210028, China 7. Theragnostic Laboratory, Radiology, KU Leuven, UZ Gathuisberg Herestraat 49, 3000, Leuven, Belgium
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Abstract: | Purpose To study whether formulation influences biodistribution, necrosis avidity and tumoricidal effects of the radioiodinated hypericin, a necrosis avid agent for a dual-targeting anticancer radiotherapy. Methods Iodine-123- and 131-labeled hypericin (123I-Hyp and 131I-Hyp) were prepared with Iodogen as oxidant, and formulated in dimethyl sulfoxide (DMSO)/PEG400 (polyethylene glycol 400)/water (25/60/15, v/v/v) or DMSO/saline (20:80, v/v). The formulations with excessive Hyp were optically characterized. Biodistribution, necrosis avidity and tumoricidal effects were studied in rats (n?=?42) without and with reperfused liver infarction and implanted rhabdomyosarcomas (R1). To induce tumor necrosis, R1-rats were pre-treated with a vascular disrupting agent. Magnetic resonance imaging, tissue-gamma counting, autoradiography and histology were used. Results The two formulations differed significantly in fluorescence and precipitation. 123I-Hyp/Hyp in DMSO/PEG400/water exhibited high uptake in necrosis but lower concentration in the lung, spleen and liver (p?<?0.01). Tumor volumes of 0.9?±?0.3 cm3 with high radioactivity (3.1?±?0.3% ID/g) were detected 6 days post-treatment. By contrast, 131I-Hyp/Hypin DMSO/saline showed low uptake in necrosis but high retention in the spleen and liver (p?<?0.01). Tumor volumes reached 2.6?±?0.7 cm3 with low tracer accumulation (0.1?±?0.04%ID/g). Conclusions The formulation of radioiodinated hypericin/hypericin appears crucial for its physical property, biodistribution, necrosis avidity and tumoricidal effects. |
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