التفاصيل البيبلوغرافية
| العنوان: |
Covalent core-radiolabeling of polymeric micelles with125I/211At for theranostic radiotherapy |
| المؤلفون: |
Sporer, E., Poulie, C. B. M., Bäck, Tom, 1964, Lindegren, Sture, 1960, Jensen, H., Kempen, P. J., Kjaer, A., Herth, M. M., Jensen, A. I. |
| المصدر: |
Nanotheranostics. 6(4):388-399 |
| مصطلحات موضوعية: |
Radiology, Nuclear Medicine and Medical Imaging, Radiologi och bildbehandling, alpha-therapy, Astatine-211, iodine-125, PEG-PLGA, polymeric micelles, 5 dioxopyrrolidin 1 yl 3 iodobenzoate, 5 dioxopyrrolidin 1 yl 3 (astato 211At) benzoate, 5 dioxopyrrolidin 1 yl 3 (iodo iodine 125) benzoate, 5 dioxopyrrolidin 1 yl 3 (trimethylstannyl) benzoate, 3 (astato astatine 211) benzamide n (polyethylene glycol poly(lactic co glycolic acid), 3 (iodo iodine 125) benzamide n (polyethylene glycol poly(lactic co glycolic acid), 3 (trimethylstannyl)benzamide n (polyethylene glycol poly(lactic co glycolic acid), aluminum, astatine 211, bismuth, germanium, iodine 125, macrogol, n chlorosuccinimide, n iodosuccinimide, n dimethylformamide, polyglactin, polymer, sodium iodide, succinimidyl stannyl enzoate, tosylchloramide sodium, unclassified drug, adult, animal experiment, animal model, animal tissue, Article, biodistribution, bond strength, carbon nuclear magnetic resonance, chromatography, circulation, clinical evaluation, controlled study, covalent bond, drug stability, dry distillation, female, high performance liquid chromatography, hydrophophicity, incubation time, lipophilicity, macrophage activation, micelle, mouse, nonhuman, particle size, photon correlation spectroscopy, polymeric micelle, positron emission tomography, proton nuclear magnetic resonance, purification, radiochemical conversion, radiochemical stability, radiochemistry, radiohalogenation, radioiodination, radiolabeling, theranostic nanomedicine, theranostic radiotherapy, thin layer chromatography, transmission electron microscopy, zeta potential |
| الوصف: |
Astatine-211 (211At) is one of the most promising α-emitters for targeted alpha therapy, especially of cancer metastases. However, the lack of a stable isotope, frequent in vivo deastatination, and limited radiochemical knowledge makes it challenging to apply. Here, we report a new strategy for radiolabeling the lipophilic core of polymeric micelles (PMs) with covalently bound211At. The PMs were radiolabeled via either an indirect synthon-based method or directly on the amphipathic block copolymer. The radiochemistry was optimized with iodine-125 (125I) and then adapted for211At, enabling the use of both elements as a potential theranostic pair. PMs that were core-radiolabeled with both125I or211At were prepared and characterized, based on a PEG(5k)-PLGA(10k) co-polymer. The stability of the radiolabeled PMs was evaluated in mouse serum for 21 h, showing radiochemical stability above 85%. After in vivo evaluation of the211At-labeled PMs, 4-5 % ID/g of the211At could still be detected in the blood, showing a promising in vivo stability of the PMs. Further,211At-labeled PMs accumulated in the spleen (20-30 %ID/g) and the liver (2.5-5.5 %ID/g), along with some detection of211At in the thyroid (3.5-9 %ID/g). This led to the hypothesis that deastatination takes place in the liver, whereas good stability of the211At core-radiolabel was observed in the blood. © The author(s). |
| الوصول الحر: |
https://gup.ub.gu.se/publication/322039Test |
| قاعدة البيانات: |
SwePub |
