PET imaging of liposomes labeled with an [¹⁸F]-fluorocholesteryl ether probe prepared by automated radiosynthesis

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

PET imaging of liposomes labeled with an [¹⁸F]-fluorocholesteryl ether probe prepared by automated radiosynthesis. / Jensen, Andreas Tue Ingemann; Binderup, Tina; Andresen, Thomas L; Kjær, Andreas; Rasmussen, Palle.

In: Journal of Liposome Research, Vol. 22, No. 4, 12.2012, p. 295-305.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Jensen, ATI, Binderup, T, Andresen, TL, Kjær, A & Rasmussen, P 2012, 'PET imaging of liposomes labeled with an [¹⁸F]-fluorocholesteryl ether probe prepared by automated radiosynthesis', Journal of Liposome Research, vol. 22, no. 4, pp. 295-305. https://doi.org/10.3109/08982104.2012.698418

APA

Jensen, A. T. I., Binderup, T., Andresen, T. L., Kjær, A., & Rasmussen, P. (2012). PET imaging of liposomes labeled with an [¹⁸F]-fluorocholesteryl ether probe prepared by automated radiosynthesis. Journal of Liposome Research, 22(4), 295-305. https://doi.org/10.3109/08982104.2012.698418

Vancouver

Jensen ATI, Binderup T, Andresen TL, Kjær A, Rasmussen P. PET imaging of liposomes labeled with an [¹⁸F]-fluorocholesteryl ether probe prepared by automated radiosynthesis. Journal of Liposome Research. 2012 Dec;22(4):295-305. https://doi.org/10.3109/08982104.2012.698418

Author

Jensen, Andreas Tue Ingemann ; Binderup, Tina ; Andresen, Thomas L ; Kjær, Andreas ; Rasmussen, Palle. / PET imaging of liposomes labeled with an [¹⁸F]-fluorocholesteryl ether probe prepared by automated radiosynthesis. In: Journal of Liposome Research. 2012 ; Vol. 22, No. 4. pp. 295-305.

Bibtex

@article{3596365d04be4a27a7f3412867ce531b,
title = "PET imaging of liposomes labeled with an [¹⁸F]-fluorocholesteryl ether probe prepared by automated radiosynthesis",
abstract = "A novel [¹⁸F]-labeled cholesteryl ether lipid probe was prepared by synthesis of the corresponding mesylate, which was [¹⁸F]-fluorinated by a [¹⁸F]KF, Kryptofix-222, K₂CO₃ procedure. Fluorination was done for 10 minutes at 165°C and took place with conversion between 3 and 17{\%}, depending on conditions. Radiolabelling of the probe and subsequent in situ purification on SEP-Paks were done on a custom-built, fully automatic synthesis robot. Long-circulating liposomes were prepared by hydration (magnetic stirring) of a lipid film containing the radiolabeled probe, followed by fully automated extrusion through 100-nm filters. The [¹⁸F]-labeled liposomes were injected into nude, tumor-bearing mice, and positron emission tomography (PET) scans were performed several times over 8 hours to investigate the in vivo biodistribution. Clear tumor accumulation, as well as hepatic and splenic uptake, was observed, corresponding to expected liposomal pharmacokinetics. The tumor accumulation 8 hours postinjection accounted for 2.25 ± 0.23 (mean ± standard error of the mean) percent of injected dose per gram ({\%}ID/g), and the tumor-to-muscle ratio reached 2.20 ± 0.24 after 8 hours, which is satisfactorily high for visualization of pathological lesions. Moreover, the blood concentration was still at a high level (13.9 ± 1.5 {\%}ID/g) at the end of the 8-hour time frame. The present work demonstrates the methodology for automated preparation of radiolabeled liposomes, and shows that [¹⁸F]-labeled liposomes could be suitable as a methodology for visualization of tumors and obtaining short-term pharmacokinetics in vivo.",
author = "Jensen, {Andreas Tue Ingemann} and Tina Binderup and Andresen, {Thomas L} and Andreas Kj{\ae}r and Palle Rasmussen",
year = "2012",
month = "12",
doi = "10.3109/08982104.2012.698418",
language = "English",
volume = "22",
pages = "295--305",
journal = "Journal of Liposome Research",
issn = "0898-2104",
publisher = "Taylor & Francis",
number = "4",

}

RIS

TY - JOUR

T1 - PET imaging of liposomes labeled with an [¹⁸F]-fluorocholesteryl ether probe prepared by automated radiosynthesis

AU - Jensen, Andreas Tue Ingemann

AU - Binderup, Tina

AU - Andresen, Thomas L

AU - Kjær, Andreas

AU - Rasmussen, Palle

PY - 2012/12

Y1 - 2012/12

N2 - A novel [¹⁸F]-labeled cholesteryl ether lipid probe was prepared by synthesis of the corresponding mesylate, which was [¹⁸F]-fluorinated by a [¹⁸F]KF, Kryptofix-222, K₂CO₃ procedure. Fluorination was done for 10 minutes at 165°C and took place with conversion between 3 and 17%, depending on conditions. Radiolabelling of the probe and subsequent in situ purification on SEP-Paks were done on a custom-built, fully automatic synthesis robot. Long-circulating liposomes were prepared by hydration (magnetic stirring) of a lipid film containing the radiolabeled probe, followed by fully automated extrusion through 100-nm filters. The [¹⁸F]-labeled liposomes were injected into nude, tumor-bearing mice, and positron emission tomography (PET) scans were performed several times over 8 hours to investigate the in vivo biodistribution. Clear tumor accumulation, as well as hepatic and splenic uptake, was observed, corresponding to expected liposomal pharmacokinetics. The tumor accumulation 8 hours postinjection accounted for 2.25 ± 0.23 (mean ± standard error of the mean) percent of injected dose per gram (%ID/g), and the tumor-to-muscle ratio reached 2.20 ± 0.24 after 8 hours, which is satisfactorily high for visualization of pathological lesions. Moreover, the blood concentration was still at a high level (13.9 ± 1.5 %ID/g) at the end of the 8-hour time frame. The present work demonstrates the methodology for automated preparation of radiolabeled liposomes, and shows that [¹⁸F]-labeled liposomes could be suitable as a methodology for visualization of tumors and obtaining short-term pharmacokinetics in vivo.

AB - A novel [¹⁸F]-labeled cholesteryl ether lipid probe was prepared by synthesis of the corresponding mesylate, which was [¹⁸F]-fluorinated by a [¹⁸F]KF, Kryptofix-222, K₂CO₃ procedure. Fluorination was done for 10 minutes at 165°C and took place with conversion between 3 and 17%, depending on conditions. Radiolabelling of the probe and subsequent in situ purification on SEP-Paks were done on a custom-built, fully automatic synthesis robot. Long-circulating liposomes were prepared by hydration (magnetic stirring) of a lipid film containing the radiolabeled probe, followed by fully automated extrusion through 100-nm filters. The [¹⁸F]-labeled liposomes were injected into nude, tumor-bearing mice, and positron emission tomography (PET) scans were performed several times over 8 hours to investigate the in vivo biodistribution. Clear tumor accumulation, as well as hepatic and splenic uptake, was observed, corresponding to expected liposomal pharmacokinetics. The tumor accumulation 8 hours postinjection accounted for 2.25 ± 0.23 (mean ± standard error of the mean) percent of injected dose per gram (%ID/g), and the tumor-to-muscle ratio reached 2.20 ± 0.24 after 8 hours, which is satisfactorily high for visualization of pathological lesions. Moreover, the blood concentration was still at a high level (13.9 ± 1.5 %ID/g) at the end of the 8-hour time frame. The present work demonstrates the methodology for automated preparation of radiolabeled liposomes, and shows that [¹⁸F]-labeled liposomes could be suitable as a methodology for visualization of tumors and obtaining short-term pharmacokinetics in vivo.

U2 - 10.3109/08982104.2012.698418

DO - 10.3109/08982104.2012.698418

M3 - Journal article

C2 - 22803638

VL - 22

SP - 295

EP - 305

JO - Journal of Liposome Research

JF - Journal of Liposome Research

SN - 0898-2104

IS - 4

ER -

ID: 45863431