Remote loading of liposomes with a 124I-radioiodinated compound and their in vivo evaluation by PET/CT in a murine tumor model

Research output: Contribution to journalJournal articlepeer-review

Standard

Remote loading of liposomes with a 124I-radioiodinated compound and their in vivo evaluation by PET/CT in a murine tumor model. / Engudar, Gokce; Schaarup-Jensen, Henrik; Fliedner, Frederikke P; Hansen, Anders E; Kempen, Paul; Jølck, Rasmus I; Kjaer, Andreas; Andresen, Thomas L; Clausen, Mads H; Jensen, Andreas I; Henriksen, Jonas R.

In: Theranostics, Vol. 8, No. 21, 2018, p. 5828-5841.

Research output: Contribution to journalJournal articlepeer-review

Harvard

Engudar, G, Schaarup-Jensen, H, Fliedner, FP, Hansen, AE, Kempen, P, Jølck, RI, Kjaer, A, Andresen, TL, Clausen, MH, Jensen, AI & Henriksen, JR 2018, 'Remote loading of liposomes with a 124I-radioiodinated compound and their in vivo evaluation by PET/CT in a murine tumor model', Theranostics, vol. 8, no. 21, pp. 5828-5841. https://doi.org/10.7150/thno.26706

APA

Engudar, G., Schaarup-Jensen, H., Fliedner, F. P., Hansen, A. E., Kempen, P., Jølck, R. I., Kjaer, A., Andresen, T. L., Clausen, M. H., Jensen, A. I., & Henriksen, J. R. (2018). Remote loading of liposomes with a 124I-radioiodinated compound and their in vivo evaluation by PET/CT in a murine tumor model. Theranostics, 8(21), 5828-5841. https://doi.org/10.7150/thno.26706

Vancouver

Engudar G, Schaarup-Jensen H, Fliedner FP, Hansen AE, Kempen P, Jølck RI et al. Remote loading of liposomes with a 124I-radioiodinated compound and their in vivo evaluation by PET/CT in a murine tumor model. Theranostics. 2018;8(21):5828-5841. https://doi.org/10.7150/thno.26706

Author

Engudar, Gokce ; Schaarup-Jensen, Henrik ; Fliedner, Frederikke P ; Hansen, Anders E ; Kempen, Paul ; Jølck, Rasmus I ; Kjaer, Andreas ; Andresen, Thomas L ; Clausen, Mads H ; Jensen, Andreas I ; Henriksen, Jonas R. / Remote loading of liposomes with a 124I-radioiodinated compound and their in vivo evaluation by PET/CT in a murine tumor model. In: Theranostics. 2018 ; Vol. 8, No. 21. pp. 5828-5841.

Bibtex

@article{113547d631a64faf9cac928c257e498b,
title = "Remote loading of liposomes with a 124I-radioiodinated compound and their in vivo evaluation by PET/CT in a murine tumor model",
abstract = "Long circulating liposomes entrapping iodinated and radioiodinated compounds offer a highly versatile theranostic platform. Here we report a new methodology for efficient and high-yield loading of such compounds into liposomes, enabling CT/SPECT/PET imaging and 131I-radiotherapy. Methods: The CT contrast agent diatrizoate was synthetically functionalized with a primary amine, which enabled its remote loading into PEGylated liposomes by either an ammonium sulfate- or a citrate-based pH transmembrane gradient. Further, the amino-diatrizoate was radiolabeled with either 124I (t1/2 = 4.18 days) for PET or 125I (t1/2 = 59.5 days) for SPECT, through an aromatic Finkelstein reaction. Results: Quantitative loading efficiencies (>99%) were achieved at optimized conditions. The 124I-labeled compound was remote-loaded into liposomes, with an overall radiolabeling efficiency of 77 ± 1%, and imaged in vivo in a CT26 murine colon cancer tumor model by PET/CT. A prolonged blood circulation half-life of 19.5 h was observed for the radiolabeled liposomes, whereas injections of the free compound were rapidly cleared. Lower accumulation was observed in the spleen, liver, kidney and tumor than what is usually seen for long-circulating liposomes. Conclusion: The lower accumulation was interpreted as release of the tracer from the liposomes within these organs after accumulation. These results may guide the design of systems for controlled release of remote loadable drugs from liposomes.",
author = "Gokce Engudar and Henrik Schaarup-Jensen and Fliedner, {Frederikke P} and Hansen, {Anders E} and Paul Kempen and J{\o}lck, {Rasmus I} and Andreas Kjaer and Andresen, {Thomas L} and Clausen, {Mads H} and Jensen, {Andreas I} and Henriksen, {Jonas R}",
year = "2018",
doi = "10.7150/thno.26706",
language = "English",
volume = "8",
pages = "5828--5841",
journal = "Theranostics",
issn = "1838-7640",
publisher = "Ivyspring International Publisher",
number = "21",

}

RIS

TY - JOUR

T1 - Remote loading of liposomes with a 124I-radioiodinated compound and their in vivo evaluation by PET/CT in a murine tumor model

AU - Engudar, Gokce

AU - Schaarup-Jensen, Henrik

AU - Fliedner, Frederikke P

AU - Hansen, Anders E

AU - Kempen, Paul

AU - Jølck, Rasmus I

AU - Kjaer, Andreas

AU - Andresen, Thomas L

AU - Clausen, Mads H

AU - Jensen, Andreas I

AU - Henriksen, Jonas R

PY - 2018

Y1 - 2018

N2 - Long circulating liposomes entrapping iodinated and radioiodinated compounds offer a highly versatile theranostic platform. Here we report a new methodology for efficient and high-yield loading of such compounds into liposomes, enabling CT/SPECT/PET imaging and 131I-radiotherapy. Methods: The CT contrast agent diatrizoate was synthetically functionalized with a primary amine, which enabled its remote loading into PEGylated liposomes by either an ammonium sulfate- or a citrate-based pH transmembrane gradient. Further, the amino-diatrizoate was radiolabeled with either 124I (t1/2 = 4.18 days) for PET or 125I (t1/2 = 59.5 days) for SPECT, through an aromatic Finkelstein reaction. Results: Quantitative loading efficiencies (>99%) were achieved at optimized conditions. The 124I-labeled compound was remote-loaded into liposomes, with an overall radiolabeling efficiency of 77 ± 1%, and imaged in vivo in a CT26 murine colon cancer tumor model by PET/CT. A prolonged blood circulation half-life of 19.5 h was observed for the radiolabeled liposomes, whereas injections of the free compound were rapidly cleared. Lower accumulation was observed in the spleen, liver, kidney and tumor than what is usually seen for long-circulating liposomes. Conclusion: The lower accumulation was interpreted as release of the tracer from the liposomes within these organs after accumulation. These results may guide the design of systems for controlled release of remote loadable drugs from liposomes.

AB - Long circulating liposomes entrapping iodinated and radioiodinated compounds offer a highly versatile theranostic platform. Here we report a new methodology for efficient and high-yield loading of such compounds into liposomes, enabling CT/SPECT/PET imaging and 131I-radiotherapy. Methods: The CT contrast agent diatrizoate was synthetically functionalized with a primary amine, which enabled its remote loading into PEGylated liposomes by either an ammonium sulfate- or a citrate-based pH transmembrane gradient. Further, the amino-diatrizoate was radiolabeled with either 124I (t1/2 = 4.18 days) for PET or 125I (t1/2 = 59.5 days) for SPECT, through an aromatic Finkelstein reaction. Results: Quantitative loading efficiencies (>99%) were achieved at optimized conditions. The 124I-labeled compound was remote-loaded into liposomes, with an overall radiolabeling efficiency of 77 ± 1%, and imaged in vivo in a CT26 murine colon cancer tumor model by PET/CT. A prolonged blood circulation half-life of 19.5 h was observed for the radiolabeled liposomes, whereas injections of the free compound were rapidly cleared. Lower accumulation was observed in the spleen, liver, kidney and tumor than what is usually seen for long-circulating liposomes. Conclusion: The lower accumulation was interpreted as release of the tracer from the liposomes within these organs after accumulation. These results may guide the design of systems for controlled release of remote loadable drugs from liposomes.

U2 - 10.7150/thno.26706

DO - 10.7150/thno.26706

M3 - Journal article

C2 - 30613265

VL - 8

SP - 5828

EP - 5841

JO - Theranostics

JF - Theranostics

SN - 1838-7640

IS - 21

ER -

ID: 218611807