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Helbok, A; Rangger, C; von Guggenberg, E; Saba-Lepek, M; Radolf, T; Thurner, G; Andreae, F; Prassl, R; Decristoforo, C.
Targeting properties of peptide-modified radiolabeled liposomal nanoparticles
NANOMED-NANOTECHNOL. 2012; 8(1): 112-118.
Doi: 10.1016/j.nano.2011.04.012
Web of Science
PubMed
FullText
FullText_MUG
- Co-authors Med Uni Graz
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Prassl Ruth
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- 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. FROM THE CLINICAL EDITOR: 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.
- Find related publications in this database (using NLM MeSH Indexing)
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Animals -
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Cell Line, Tumor -
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Drug Delivery Systems -
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Inhibitory Concentration 50 -
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Iridium Radioisotopes -
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Liposomes - administration and dosage Liposomes - chemistry
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Mice -
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Mice, Nude -
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Micelles -
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Nanoparticles - administration and dosage Nanoparticles - therapeutic use
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Octreotide - administration and dosage Octreotide - analogs and derivatives Octreotide - therapeutic use
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Pancreatic Neoplasms - drug therapy
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Pentetic Acid - chemistry
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Phosphatidylethanolamines - chemistry
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Polyethylene Glycols - chemistry
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Rats -
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Rats, Inbred Lew -
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Tissue Distribution -
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Tomography, Emission-Computed, Single-Photon -
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Transplantation, Heterologous -
- Find related publications in this database (Keywords)
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Liposome
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Micelle
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Radiolabeling
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Targeting
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Neuroendocrine tumors