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Article

Biological Distribution of Orally Administered [123I]MIBG for Estimating Gastrointestinal Tract Absorption

1
Faculty of Health Sciences, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, 5-11-80 Kodatsuno, Kanazawa 920-0942, Japan
2
Department of Radioisotope Medicine, Atomic Bomb Disease Institute, Nagasaki University, 1-12-4 Sakamoto, Nagasaki 852-8523, Japan
3
Faculty of Pharmaceutical Sciences, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kakuma, Kanazawa 920-1192, Japan
4
Department of Molecular Imaging and Theranostics, Institute for Quantum Medical Science Quantum Life and Medical Science Directorate, National Institutes for Quantum Science and Technology (QST), 4-9-1 Anagawa, Inage, Chiba 263-8555, Japan
5
Department of Radiological Sciences, Ibaraki Prefectural University of Health Sciences, 4669-2 Ami, Inashiki, Ibaraki 300-0394, Japan
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Faculty of Pharmacy, Takasaki University of Health and Welfare, 60 Nakaorui-machi, Takasaki 370-0033, Japan
7
Biomedical Imaging Research Center, University of Fukui, 23-3 Matsuokashimoaizuki, Eiheiji, Fukui 910-1193, Japan
*
Author to whom correspondence should be addressed.
Academic Editor: Emanuela Fabiola Craparo
Pharmaceutics 2022, 14(1), 61; https://doi.org/10.3390/pharmaceutics14010061
Received: 30 November 2021 / Revised: 21 December 2021 / Accepted: 24 December 2021 / Published: 28 December 2021
(This article belongs to the Special Issue Recent Advances in Radiopharmaceutics)
Gastrointestinal tract absorption of cationic anticancer drugs and medicines was estimated using whole-body imaging following oral [123I]MIBG administration. [123I]MIBG was added to cultures of human embryonic kidney (HEK)293 cells expressing human organic anion transporting polypeptide (OATP)2B1, carnitine/organic cation transporter (OCTN)1 and OCTN2, and organic cation transporter (OCT)1, OCT2, and OCT3 with and without cimetidine (an OCTN and OCT inhibitor) and L-carnitine (an OCTN inhibitor). Biodistribution analyses and single-photon emission computed tomography (SPECT) imaging in normal and dextran sodium sulfate (DSS)-induced experimental colitis mice were conducted using [123I]MIBG with and without cimetidine. [123I]MIBG uptake was significantly higher in HEK293/OCTN1, 2, and OCT1-3 cells than in mock cells. Uptake via OCTN was inhibited by L-carnitine, whereas OCT-mediated uptake was inhibited by cimetidine. Biodistribution analyses and SPECT imaging studies showed significantly lower accumulation of [123I]MIBG in the blood, heart, liver, and bladder in DSS-induced experimental colitis mice and mice with cimetidine loading compared with normal mice, whereas significantly higher accumulation in the stomach and kidney was observed after [123I]MIBG injection. [123I]MIBG imaging after oral administration can be used to estimate gastrointestinal absorption in the small intestine via OCTN and/or OCT by measuring radioactivity in the heart, liver, and bladder. View Full-Text
Keywords: [123I]MIBG; SPECT; imaging; drug transporters; gastrointestinal tract absorption [123I]MIBG; SPECT; imaging; drug transporters; gastrointestinal tract absorption
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MDPI and ACS Style

Kobayashi, M.; Mizutani, A.; Muranaka, Y.; Nishi, K.; Komori, H.; Nishii, R.; Shikano, N.; Nakanishi, T.; Tamai, I.; Kawai, K. Biological Distribution of Orally Administered [123I]MIBG for Estimating Gastrointestinal Tract Absorption. Pharmaceutics 2022, 14, 61. https://doi.org/10.3390/pharmaceutics14010061

AMA Style

Kobayashi M, Mizutani A, Muranaka Y, Nishi K, Komori H, Nishii R, Shikano N, Nakanishi T, Tamai I, Kawai K. Biological Distribution of Orally Administered [123I]MIBG for Estimating Gastrointestinal Tract Absorption. Pharmaceutics. 2022; 14(1):61. https://doi.org/10.3390/pharmaceutics14010061

Chicago/Turabian Style

Kobayashi, Masato, Asuka Mizutani, Yuka Muranaka, Kodai Nishi, Hisakazu Komori, Ryuichi Nishii, Naoto Shikano, Takeo Nakanishi, Ikumi Tamai, and Keiichi Kawai. 2022. "Biological Distribution of Orally Administered [123I]MIBG for Estimating Gastrointestinal Tract Absorption" Pharmaceutics 14, no. 1: 61. https://doi.org/10.3390/pharmaceutics14010061

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