Biodistribution and Dosimetry of Free 211At, 125I- and 131I- in Rats

Overview

Journal Cancer Biother Radiopharm

Specialties Oncology
Pharmacology
Radiology

Date 2013 Jun 25

PMID 23789969

Citations 38

Authors

Johan Spetz

Nils Rudqvist

Eva Forssell-Aronsson

Affiliations

Soon will be listed here.

Abstract

131I is widely used for therapy in the clinic and 125I and 131I, and increasingly 211At, are often used in experimental studies. It is important to know the biodistribution and dosimetry for these radionuclides to determine potential risk organs when using radiopharmaceuticals containing these radionuclides. The purpose of this study was to investigate the biodistribution of 125I-, 131I-, and free 211At in rats and to determine absorbed doses to various organs and tissues. Male Sprague Dawley rats were injected simultaneously with 0.1-0.3 MBq 125I- and 0.1-0.3 MBq 131I-, or 0.05-0.2 MBq 211At and sacrificed 1 hour to 7 days after injection. The activities and activity concentrations in organs and tissues were determined and mean absorbed doses were calculated. The biodistribution of 125I- was similar to that of 131I- but the biodistribution of free 211At was different compared to 125I- and 131I-. The activity concentration of radioiodine was higher compared with 211At in the thyroid and lower in all extrathyroidal tissues. The mean absorbed dose per unit injected activity was highest to the thyroid. 131I gave the highest absorbed dose to the thyroid, and 211At gave the highest absorbed dose to all other tissues studied.

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References

Garg P, Harrison C, Zalutsky M . Comparative tissue distribution in mice of the alpha-emitter 211At and 131I as labels of a monoclonal antibody and F(ab')2 fragment. Cancer Res. 1990; 50(12):3514-20. View

Lundh C, Lindencrona U, Schmitt A, Nilsson M, Forssell-Aronsson E . Biodistribution of free 211At and 125I- in nude mice bearing tumors derived from anaplastic thyroid carcinoma cell lines. Cancer Biother Radiopharm. 2007; 21(6):591-600. DOI: 10.1089/cbr.2006.21.591. View

Hamilton J, SOLEY M . A Comparison of the Metabolism of Iodine and of Element 85 (Eka-Iodine). Proc Natl Acad Sci U S A. 1940; 26(8):483-9. PMC: 1078214. DOI: 10.1073/pnas.26.8.483. View

Uusijarvi H, Bernhardt P, Forssell-Aronsson E . Translation of dosimetric results of preclinical radionuclide therapy to clinical situations: influence of photon irradiation. Cancer Biother Radiopharm. 2007; 22(2):268-74. DOI: 10.1089/cbr.2006.317. View

Dohan O, De la Vieja A, Paroder V, Riedel C, Artani M, Reed M . The sodium/iodide Symporter (NIS): characterization, regulation, and medical significance. Endocr Rev. 2003; 24(1):48-77. DOI: 10.1210/er.2001-0029. View

Brown I . Astatine-211: its possible applications in cancer therapy. Int J Rad Appl Instrum A. 1986; 37(8):789-98. DOI: 10.1016/0883-2889(86)90273-x. View

Endo S, Nitta Y, Ohtaki M, Takada J, Stepanenko V, Komatsu K . Estimation of dose absorbed fraction for 131I-beta rays in rat thyroid. J Radiat Res. 1998; 39(3):223-30. DOI: 10.1269/jrr.39.223. View

Lee H, BLAUFOX M . Blood volume in the rat. J Nucl Med. 1985; 26(1):72-6. View

Harrison A, Royle L . Determination of absorbed dose to blood, kidneys, testes and thyroid in mice injected with 211At and comparison of testes mass and sperm number in x-irradiated and 211At treated mice. Health Phys. 1984; 46(2):377-83. DOI: 10.1097/00004032-198402000-00013. View

10.

Spitzweg C, Joba W, Eisenmenger W, Heufelder A . Analysis of human sodium iodide symporter gene expression in extrathyroidal tissues and cloning of its complementary deoxyribonucleic acids from salivary gland, mammary gland, and gastric mucosa. J Clin Endocrinol Metab. 1998; 83(5):1746-51. DOI: 10.1210/jcem.83.5.4839. View

11.

Shellabarger C, Godwin J . Studies on the thyroidal uptake of astatine in the rat. J Clin Endocrinol Metab. 1954; 14(10):1149-60. DOI: 10.1210/jcem-14-10-1149. View

12.

Lindencrona U, Nilsson M, Forssell-Aronsson E . Similarities and differences between free 211At and 125I- transport in porcine thyroid epithelial cells cultured in bicameral chambers. Nucl Med Biol. 2001; 28(1):41-50. DOI: 10.1016/s0969-8051(00)00179-7. View

13.

Kleiber M . Body size and metabolic rate. Physiol Rev. 2010; 27(4):511-41. DOI: 10.1152/physrev.1947.27.4.511. View

14.

Hamilton J, ASLING C, GARRISON W, SCOTT K . The accumulation, metabolism and biological effects of astatine in rats and monkeys. Univ Calif Publ Pharmacol. 2014; 2(21):283-312. View

15.

Lindegren S, Back T, Jensen H . Dry-distillation of astatine-211 from irradiated bismuth targets: a time-saving procedure with high recovery yields. Appl Radiat Isot. 2001; 55(2):157-60. DOI: 10.1016/s0969-8043(01)00044-6. View

16.

Josefsson A, Forssell-Aronsson E . Microdosimetric analysis of 211At in thyroid models for man, rat and mouse. EJNMMI Res. 2012; 2(1):29. PMC: 3444346. DOI: 10.1186/2191-219X-2-29. View

17.

Cobb L, Harrison A, DUDLEY N, CARR T, Humphreys J . Relative concentration of astatine-211 and iodine-125 by human fetal thyroid and carcinoma of the thyroid in nude mice. Radiother Oncol. 1988; 13(3):203-9. DOI: 10.1016/0167-8140(88)90057-6. View

18.

Aronsson E, Gretarsdottir J, Jacobsson L, Back T, Hertzman S, Lindegren S . Therapy with 125I-labelled internalized and non-internalized monoclonal antibodies in nude mice with human colon carcinoma xenografts. Nucl Med Biol. 1993; 20(2):133-44. DOI: 10.1016/0969-8051(93)90105-4. View

19.

Larsen R, Slade S, Zalutsky M . Blocking [211At]astatide accumulation in normal tissues: preliminary evaluation of seven potential compounds. Nucl Med Biol. 1998; 25(4):351-7. DOI: 10.1016/s0969-8051(97)00230-8. View