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Covalent core-radio...
Covalent core-radiolabeling of polymeric micelles with125I/211At for theranostic radiotherapy
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Sporer, E. (författare)
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Poulie, C. B. M. (författare)
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- Bäck, Tom, 1964 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kliniska vetenskaper, Avdelningen för medicinsk strålningsvetenskap,Institute of Clinical Sciences, Department of Medical Radiation Sciences
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- Lindegren, Sture, 1960 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kliniska vetenskaper, Avdelningen för medicinsk strålningsvetenskap,Institute of Clinical Sciences, Department of Medical Radiation Sciences
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Jensen, H. (författare)
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Kempen, P. J. (författare)
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Kjaer, A. (författare)
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Herth, M. M. (författare)
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Jensen, A. I. (författare)
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(creator_code:org_t)
- Ivyspring International Publisher, 2022
- 2022
- Engelska.
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Ingår i: Nanotheranostics. - : Ivyspring International Publisher. - 2206-7418. ; 6:4, s. 388-399
- Relaterad länk:
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https://gup.ub.gu.se...
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https://doi.org/10.7...
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Abstract
Ämnesord
Stäng
- 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).
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Radiologi och bildbehandling (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Radiology, Nuclear Medicine and Medical Imaging (hsv//eng)
Nyckelord
- alpha-therapy
- Astatine-211
- iodine-125
- PEG-PLGA
- polymeric micelles
- 2
- 5 dioxopyrrolidin 1 yl 3 iodobenzoate
- 2
- 5 dioxopyrrolidin 1 yl 3 (astato 211At) benzoate
- 2
- 5 dioxopyrrolidin 1 yl 3 (iodo iodine 125) benzoate
- 2
- 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
- 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
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
Hitta via bibliotek
Till lärosätets databas
- Av författaren/redakt...
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Sporer, E.
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Poulie, C. B. M.
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Bäck, Tom, 1964
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Lindegren, Sture ...
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Jensen, H.
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Kempen, P. J.
-
visa fler...
-
Kjaer, A.
-
Herth, M. M.
-
Jensen, A. I.
-
visa färre...
- Om ämnet
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- MEDICIN OCH HÄLSOVETENSKAP
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MEDICIN OCH HÄLS ...
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och Klinisk medicin
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och Radiologi och bi ...
- Artiklar i publikationen
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Nanotheranostics
- Av lärosätet
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Göteborgs universitet