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@article{82733b430ebe4c5cb2c37458743bc99e,
title = "Positron emission tomography evaluation of somatostatin receptor targeted (64)Cu-TATE-liposomes in a human neuroendocrine carcinoma mouse model.",
keywords = "Liposomes, Octreotate, Somatostatin, Positron emission tomography, Targeting ligand, Nanoparticles",
publisher = "Elsevier BV",
author = "Petersen, {Anncatrine Luisa} and Tina Binderup and Jølck, {Rasmus Irming} and Palle Rasmussen and Henriksen, {Jonas Rosager} and Pfeifer, {Andreas Klaus} and Andreas Kjær and Andresen, {Thomas Lars}",
year = "2012",
doi = "10.1016/j.jconrel.2011.12.038",
volume = "160",
number = "2",
pages = "254--263",
journal = "Journal of Controlled Release",
issn = "0168-3659",

}

RIS

TY - JOUR

T1 - Positron emission tomography evaluation of somatostatin receptor targeted (64)Cu-TATE-liposomes in a human neuroendocrine carcinoma mouse model.

A1 - Petersen,Anncatrine Luisa

A1 - Binderup,Tina

A1 - Jølck,Rasmus Irming

A1 - Rasmussen,Palle

A1 - Henriksen,Jonas Rosager

A1 - Pfeifer,Andreas Klaus

A1 - Kjær,Andreas

A1 - Andresen,Thomas Lars

AU - Petersen,Anncatrine Luisa

AU - Binderup,Tina

AU - Jølck,Rasmus Irming

AU - Rasmussen,Palle

AU - Henriksen,Jonas Rosager

AU - Pfeifer,Andreas Klaus

AU - Kjær,Andreas

AU - Andresen,Thomas Lars

PB - Elsevier BV

PY - 2012

Y1 - 2012

N2 - Targeted therapeutic and diagnostic nanocarriers functionalized with antibodies, peptides or other targeting ligands that recognize over-expressed receptors or antigens on tumor cells have potential in the diagnosis and therapy of cancer. Somatostatin receptors (SSTRs) are over-expressed in a variety of cancers, particularly neuroendocrine tumors (NETs) and can be targeted with somatostatin peptide analogs such as octreotate (TATE). In the present study we investigate liposomes that target SSTR in a NET xenograft mouse model (NCI-H727) by use of TATE. TATE was covalently attached to the distal end of DSPE-PEG(2000) on PEGylated liposomes with an encapsulated positron emitter (64)Cu that can be utilized for positron emission tomography (PET) imaging. The biodistribution and pharmacokinetics of the (64)Cu-loaded PEGylated liposomes with and without TATE was investigated and their ability to image NETs was evaluated using PET. Additionally, the liposome accumulation and imaging capability was compared with free radiolabelled TATE peptide administered as (64)Cu-DOTA-TATE. The presence of TATE on the liposomes resulted in a significantly faster initial blood clearance in comparison to control-liposomes without TATE. PEGylated liposomes with or without TATE accumulated at significantly higher quantities in NETs (5.1±0.3 and 5.8±0.2 %ID/g, respectively) than the free peptide (64)Cu-DOTA-TATE (1.4±0.3 %ID/g) 24h post-injection. Importantly, (64)Cu-loaded PEGylated liposomes with TATE showed significantly higher tumor-to-muscle (T/M) ratio (12.7±1.0) than the control-liposomes without TATE (8.9±0.9) and the (64)Cu-DOTA-TATE free peptide (7.2±0.3). The higher T/M ratio of the PEGylated liposomes with TATE suggests some advantage of active targeting of NETs, although no absolute benefit in tumor accumulation over the non-targeted liposomes was observed. Collectively, these data showed that (64)Cu-loaded PEGylated liposomes with TATE conjugated to the surface could be promising new imaging agents for visualizing tumor tissue and especially NETs using PET.

AB - Targeted therapeutic and diagnostic nanocarriers functionalized with antibodies, peptides or other targeting ligands that recognize over-expressed receptors or antigens on tumor cells have potential in the diagnosis and therapy of cancer. Somatostatin receptors (SSTRs) are over-expressed in a variety of cancers, particularly neuroendocrine tumors (NETs) and can be targeted with somatostatin peptide analogs such as octreotate (TATE). In the present study we investigate liposomes that target SSTR in a NET xenograft mouse model (NCI-H727) by use of TATE. TATE was covalently attached to the distal end of DSPE-PEG(2000) on PEGylated liposomes with an encapsulated positron emitter (64)Cu that can be utilized for positron emission tomography (PET) imaging. The biodistribution and pharmacokinetics of the (64)Cu-loaded PEGylated liposomes with and without TATE was investigated and their ability to image NETs was evaluated using PET. Additionally, the liposome accumulation and imaging capability was compared with free radiolabelled TATE peptide administered as (64)Cu-DOTA-TATE. The presence of TATE on the liposomes resulted in a significantly faster initial blood clearance in comparison to control-liposomes without TATE. PEGylated liposomes with or without TATE accumulated at significantly higher quantities in NETs (5.1±0.3 and 5.8±0.2 %ID/g, respectively) than the free peptide (64)Cu-DOTA-TATE (1.4±0.3 %ID/g) 24h post-injection. Importantly, (64)Cu-loaded PEGylated liposomes with TATE showed significantly higher tumor-to-muscle (T/M) ratio (12.7±1.0) than the control-liposomes without TATE (8.9±0.9) and the (64)Cu-DOTA-TATE free peptide (7.2±0.3). The higher T/M ratio of the PEGylated liposomes with TATE suggests some advantage of active targeting of NETs, although no absolute benefit in tumor accumulation over the non-targeted liposomes was observed. Collectively, these data showed that (64)Cu-loaded PEGylated liposomes with TATE conjugated to the surface could be promising new imaging agents for visualizing tumor tissue and especially NETs using PET.

KW - Liposomes

KW - Octreotate

KW - Somatostatin

KW - Positron emission tomography

KW - Targeting ligand

KW - Nanoparticles

U2 - 10.1016/j.jconrel.2011.12.038

DO - 10.1016/j.jconrel.2011.12.038

JO - Journal of Controlled Release

JF - Journal of Controlled Release

SN - 0168-3659

IS - 2

VL - 160

SP - 254

EP - 263

ER -