Labeling of biotin with [166Dy]Dy/166Ho as a stable in vivo generator system
| Autor: | F. Monroy-Guzmán, Guillermina Ferro-Flores, Martha Pedraza-López, C. Arteaga de Murphy, Laura Meléndez-Alafort, J. I. Tendilla, R Jiménez-Varela |
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| Rok vydání: | 2003 |
| Předmět: |
Biodistribution
Biotin Pharmaceutical Science High-performance liquid chromatography Holmium Mice chemistry.chemical_compound Drug Stability In vivo Dysprosium Animals Tissue Distribution Chromatography High Pressure Liquid Radioisotopes Mice Inbred BALB C biology Radiochemistry Pentetic Acid In vitro Dilution chemistry Isotope Labeling Injections Intravenous biology.protein Agarose Female Chromatography Thin Layer Radiopharmaceuticals Nuclear chemistry Avidin |
| Zdroj: | International Journal of Pharmaceutics. 255:129-138 |
| ISSN: | 0378-5173 |
| DOI: | 10.1016/s0378-5173(03)00052-8 |
| Popis: | The aim of this work was to synthesize [ 166 Dy ] Dy / 166 Ho -DTPA-Biotin to evaluate its potential as a new radiopharmaceutical for targeted radiotherapy. Dysprosium-166 ( 166 Dy ) was obtained by neutron irradiation of enriched 164 Dy 2 O 3 in a Triga Mark III reactor. The labeling was carried out in aqueous media at pH 8.0 by addition of [ 166 Dy ] DyCl 3 to diethylenetriaminepentaacetic-α,ω-bis(biocytinamide) (DTPA-Biotin). Radiochemical purity was determined by high-performance liquid chromatography (HPLC) and TLC. The biological integrity of labeled biotin was studied evaluating its avidity for avidin in an agarose column and by size-exclusion HPLC analysis of the radiolabeled DTPA-Biotin with and without the addition of avidin. Stability studies against dilution were carried out by diluting the radiocomplex solution with saline solution and with human serum at 37 °C for 24 h. The [ 166 Dy ] Dy / 166 Ho -labeled biotin was obtained with a 99.1±0.6% radiochemical purity. In vitro studies demonstrated that [ 166 Dy ] Dy / 166 Ho -DTPA-Biotin is stable after dilution in saline and in human serum and no translocation of the daughter nucleus occurs subsequent to β− decay of 166 Dy that could produce release of 166 Ho 3+ . Avidity of labeled biotin for avidin was not affected by the labeling procedure. Biodistribution studies in normal mice showed that the [ 166 Dy ] Dy / 166 Ho -DTPA-Biotin has a high renal clearance. In conclusion, the radiolabeled biotin prepared in this investigation has adequate properties to work as a stable in vivo generator system for targeted radiotherapy. |
| Databáze: | OpenAIRE |
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