Targeting properties of peptide-modified radiolabeled liposomal nanoparticles

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...

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Veröffentlicht in:	Nanomedicine 2012, Vol.8 (1), p.112-118
Hauptverfasser:	Helbok, Anna, MSc, Rangger, Christine, MSc, von Guggenberg, Elisabeth, PhD, Saba-Lepek, Matthias, PhD, Radolf, Thorsten, Ing, Thurner, Gudrun, MSc, Andreae, Fritz, PhD, Prassl, Ruth, PhD, Decristoforo, Clemens, PhD
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Cell Line, Tumor Drug Delivery Systems Inhibitory Concentration 50 Internal Medicine Iridium Radioisotopes Liposome Liposomes - administration & dosage Liposomes - chemistry Mice Mice, Nude Micelle Micelles Nanoparticles - administration & dosage Nanoparticles - therapeutic use Neuroendocrine tumors Octreotide - administration & dosage Octreotide - analogs & derivatives Octreotide - therapeutic use Pancreatic Neoplasms - drug therapy Pentetic Acid - chemistry Phosphatidylethanolamines - chemistry Polyethylene Glycols - chemistry Radiolabeling Rats Rats, Inbred Lew Targeting Tissue Distribution Tomography, Emission-Computed, Single-Photon Transplantation, Heterologous
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Zusammenfassung:	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 IC50 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 (
ISSN:	1549-9634 1549-9642
DOI:	10.1016/j.nano.2011.04.012