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Necrosis affinity evaluation of 131I-hypericin in a rat model of induced necrosis.
- Source :
-
Journal of Drug Targeting . Jul2013, Vol. 21 Issue 6, p604-610. 7p. - Publication Year :
- 2013
-
Abstract
- Cancers are often with spontaneous or therapeutic necrosis that could be utilized as a generic target for developing new treatments. The purpose of this study was to investigate the biodistribution and pharmacokinetics of radioiodinated hypericin (Hyp), a naturally occurring compound, after intravenous (i.v.) injection in a rat model of liver and muscle necrosis ( n = 42), and evaluate its necrosis affinity. Hyp was labeled with 131I with labeling efficiency >99%. After incubating in solution/rat plasma for 8 days, radiochemical purity of 131I-Hyp remained 98.1 and 97.1%, respectively, indicating good in vitro stability. SPECT-CT images at 24 h after i.v. injection of 131I-Hyp in rats with induced liver and muscle necrosis showed obvious tracer absorption in necrotic tissues. Biodistribution studies revealed that the percentage of the injected dose per gram of tissue (%ID/g) evolved from 1.9 %ID/g at 6 h, through a maximum 3.0 %ID/g at 12 h, to 1.0 %ID/g at 192 h in necrotic liver. Pharmacokinetics studies revealed that the terminal elimination half-life, total body clearance and area under the curve of 131I-Hyp were 32.7 h, 9.2 L/h/kg and 1.6 MBq/L*h, respectively. These results demonstrated that 131I-Hyp features a long blood circulation in animals and persistent retention in necrotic tissues. Therefore, 131I-labeled Hyp could be a broad-spectrum anti-tumor agent with a cost much cheaper relative to the biological agents such as monoclonal antibodies. [ABSTRACT FROM AUTHOR]
- Subjects :
- *NECROSIS
*HYPERICIN
*GENERIC drugs
*DRUG development
*LABORATORY rats
*THERAPEUTICS
Subjects
Details
- Language :
- English
- ISSN :
- 1061186X
- Volume :
- 21
- Issue :
- 6
- Database :
- Academic Search Index
- Journal :
- Journal of Drug Targeting
- Publication Type :
- Academic Journal
- Accession number :
- 88802483
- Full Text :
- https://doi.org/10.3109/1061186X.2013.789034