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Targeting properties of peptide-modified radiolabeled liposomal nanoparticles.

Identifieur interne : 000A02 ( Main/Exploration ); précédent : 000A01; suivant : 000A03

Targeting properties of peptide-modified radiolabeled liposomal nanoparticles.

Auteurs : RBID : pubmed:21645641

English descriptors

Abstract

Radiolabeled PEGylated liposomal nanoparticles (NPs) open new possibilities for a variety of applications including diagnosis, drug delivery, targeted therapy, and monitoring treatment effects. Here we describe the characterization of liposomal NPs (liposomes and micelles) derivatized with the somatostatin analogue tyrosine-3-octreotide as a proof of concept for tumor targeting. NPs were radiolabeled with indium-111, and targeting properties were evaluated in vitro on rat pancreatic tumor cells (AR42J), demonstrating specific binding and IC(50) values in the low nanomolar range. Biodistribution studies were performed in Lewis rats and compared to single-photon emission computed tomography images. Moderate tumor uptake was found in xenografted nude mice (<2.5% ID/g tissue) as compared to control. Micelles and liposomes revealed comparable pharmacokinetics and targeting properties. This study provides insight into tumor-targeting characteristics of peptide-derivatized liposomal NPs and can serve as a basis for further improvement of these constructs.

DOI: 10.1016/j.nano.2011.04.012
PubMed: 21645641

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Le document en format XML

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<title xml:lang="en">Targeting properties of peptide-modified radiolabeled liposomal nanoparticles.</title>
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<name sortKey="Helbok, Anna" uniqKey="Helbok A">Anna Helbok</name>
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<nlm:affiliation>Clinical Department of Nuclear Medicine, Innsbruck Medical University, Austria.</nlm:affiliation>
<country xml:lang="fr">Autriche</country>
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<name sortKey="Rangger, Christine" uniqKey="Rangger C">Christine Rangger</name>
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<name sortKey="Von Guggenberg, Elisabeth" uniqKey="Von Guggenberg E">Elisabeth von Guggenberg</name>
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<name sortKey="Saba Lepek, Matthias" uniqKey="Saba Lepek M">Matthias Saba-Lepek</name>
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<name sortKey="Radolf, Thorsten" uniqKey="Radolf T">Thorsten Radolf</name>
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<name sortKey="Thurner, Gudrun" uniqKey="Thurner G">Gudrun Thurner</name>
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<name sortKey="Andreae, Fritz" uniqKey="Andreae F">Fritz Andreae</name>
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<name sortKey="Prassl, Ruth" uniqKey="Prassl R">Ruth Prassl</name>
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<name sortKey="Decristoforo, Clemens" uniqKey="Decristoforo C">Clemens Decristoforo</name>
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<div type="abstract" xml:lang="en">Radiolabeled PEGylated liposomal nanoparticles (NPs) open new possibilities for a variety of applications including diagnosis, drug delivery, targeted therapy, and monitoring treatment effects. Here we describe the characterization of liposomal NPs (liposomes and micelles) derivatized with the somatostatin analogue tyrosine-3-octreotide as a proof of concept for tumor targeting. NPs were radiolabeled with indium-111, and targeting properties were evaluated in vitro on rat pancreatic tumor cells (AR42J), demonstrating specific binding and IC(50) values in the low nanomolar range. Biodistribution studies were performed in Lewis rats and compared to single-photon emission computed tomography images. Moderate tumor uptake was found in xenografted nude mice (<2.5% ID/g tissue) as compared to control. Micelles and liposomes revealed comparable pharmacokinetics and targeting properties. This study provides insight into tumor-targeting characteristics of peptide-derivatized liposomal NPs and can serve as a basis for further improvement of these constructs.</div>
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<AbstractText Label="UNLABELLED">Radiolabeled PEGylated liposomal nanoparticles (NPs) open new possibilities for a variety of applications including diagnosis, drug delivery, targeted therapy, and monitoring treatment effects. Here we describe the characterization of liposomal NPs (liposomes and micelles) derivatized with the somatostatin analogue tyrosine-3-octreotide as a proof of concept for tumor targeting. NPs were radiolabeled with indium-111, and targeting properties were evaluated in vitro on rat pancreatic tumor cells (AR42J), demonstrating specific binding and IC(50) values in the low nanomolar range. Biodistribution studies were performed in Lewis rats and compared to single-photon emission computed tomography images. Moderate tumor uptake was found in xenografted nude mice (<2.5% ID/g tissue) as compared to control. Micelles and liposomes revealed comparable pharmacokinetics and targeting properties. This study provides insight into tumor-targeting characteristics of peptide-derivatized liposomal NPs and can serve as a basis for further improvement of these constructs.</AbstractText>
<AbstractText Label="FROM THE CLINICAL EDITOR" NlmCategory="UNASSIGNED">The authors investigated tumor-targeting characteristics of peptide-derivatized liposomal NPs. Similar radiolabeled PEGylated liposomal NPs open new possibilities for a variety of applications including diagnosis, drug delivery, targeted therapy, and treatment monitoring.</AbstractText>
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