Covalent core-radiolabeling of polymeric micelles with125I/211At for theranostic radiotherapy

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Covalent core-radiolabeling of polymeric micelles with125I/211At for theranostic radiotherapy. / Sporer, Emanuel; Poulie, Christian B.M.; Bäck, Tom; Lindegren, Sture; Jensen, Holger; Kempen, Paul J.; Kjaer, Andreas; Herth, Matthias M.; Jensen, Andreas I.

In: Nanotheranostics, Vol. 6, No. 4, 2022, p. 388-399.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Sporer, E, Poulie, CBM, Bäck, T, Lindegren, S, Jensen, H, Kempen, PJ, Kjaer, A, Herth, MM & Jensen, AI 2022, 'Covalent core-radiolabeling of polymeric micelles with125I/211At for theranostic radiotherapy', Nanotheranostics, vol. 6, no. 4, pp. 388-399. https://doi.org/10.7150/ntno.71906

APA

Sporer, E., Poulie, C. B. M., Bäck, T., Lindegren, S., Jensen, H., Kempen, P. J., Kjaer, A., Herth, M. M., & Jensen, A. I. (2022). Covalent core-radiolabeling of polymeric micelles with125I/211At for theranostic radiotherapy. Nanotheranostics, 6(4), 388-399. https://doi.org/10.7150/ntno.71906

Vancouver

Sporer E, Poulie CBM, Bäck T, Lindegren S, Jensen H, Kempen PJ et al. Covalent core-radiolabeling of polymeric micelles with125I/211At for theranostic radiotherapy. Nanotheranostics. 2022;6(4):388-399. https://doi.org/10.7150/ntno.71906

Author

Sporer, Emanuel ; Poulie, Christian B.M. ; Bäck, Tom ; Lindegren, Sture ; Jensen, Holger ; Kempen, Paul J. ; Kjaer, Andreas ; Herth, Matthias M. ; Jensen, Andreas I. / Covalent core-radiolabeling of polymeric micelles with125I/211At for theranostic radiotherapy. In: Nanotheranostics. 2022 ; Vol. 6, No. 4. pp. 388-399.

Bibtex

@article{c1c8aeea42504a8a91df32d3ef63f1e3,
title = "Covalent core-radiolabeling of polymeric micelles with125I/211At for theranostic radiotherapy",
abstract = "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.",
keywords = "alpha-therapy, Astatine-211, iodine-125, PEG-PLGA, polymeric micelles",
author = "Emanuel Sporer and Poulie, {Christian B.M.} and Tom B{\"a}ck and Sture Lindegren and Holger Jensen and Kempen, {Paul J.} and Andreas Kjaer and Herth, {Matthias M.} and Jensen, {Andreas I.}",
note = "Publisher Copyright: {\textcopyright} The author(s).",
year = "2022",
doi = "10.7150/ntno.71906",
language = "English",
volume = "6",
pages = "388--399",
journal = "Nanotheranostics",
issn = "2206-7418",
publisher = "Ivyspring International Publisher",
number = "4",

}

RIS

TY - JOUR

T1 - Covalent core-radiolabeling of polymeric micelles with125I/211At for theranostic radiotherapy

AU - Sporer, Emanuel

AU - Poulie, Christian B.M.

AU - Bäck, Tom

AU - Lindegren, Sture

AU - Jensen, Holger

AU - Kempen, Paul J.

AU - Kjaer, Andreas

AU - Herth, Matthias M.

AU - Jensen, Andreas I.

N1 - Publisher Copyright: © The author(s).

PY - 2022

Y1 - 2022

N2 - 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.

AB - 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.

KW - alpha-therapy

KW - Astatine-211

KW - iodine-125

KW - PEG-PLGA

KW - polymeric micelles

UR - http://www.scopus.com/inward/record.url?scp=85134598082&partnerID=8YFLogxK

U2 - 10.7150/ntno.71906

DO - 10.7150/ntno.71906

M3 - Journal article

C2 - 35912139

AN - SCOPUS:85134598082

VL - 6

SP - 388

EP - 399

JO - Nanotheranostics

JF - Nanotheranostics

SN - 2206-7418

IS - 4

ER -

ID: 317513769