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Ortner, A; Wernig, K; Kaisler, R; Edetsberger, M; Hajos, F; Köhler, G; Mosgoeller, W; Zimmer, A.
VPAC receptor mediated tumor cell targeting by protamine based nanoparticles.
J Drug Target. 2010; 18(6):457-467 Doi: 10.3109/10611860903508796
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Führende Autor*innen der Med Uni Graz
Ortner Anna
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Abstract:
The receptors for vasoactive intestinal peptide (VIP), VPAC1-, VPAC2-, and PAC1-receptor are overexpressed by various tumor cells. VIP can target these receptors and transport conjugates into the cell. However, the use of VIP for tumor cell targeting is hampered by the peptides short half-lives due to enzymatic degradation. Because protamine-based nanoparticles (proticles) protect the peptide and serve as peptide depot, we explored the potential of proticles as carrier for VIP-conjugated molecules. The VIP-loaded proticles were stable as shown by Fluorescence Correlation Spectroscopy. With Confocal Laser Scanning Microscopy, we observed VIP-loaded proticles to specifically target the tumor cells. The cell binding triggered the substance release and conjugate internalization of VIP-Cy3 in vitro and ex vivo by human tumors. We observed VIP releasing proticle depots distributed in rat tissue and human tumors. Our findings warrant further studies to explore the proticles potential to enable peptide-mediated targeting for in vivo and clinical applications.
Find related publications in this database (using NLM MeSH Indexing)
Animals -
Arteries - drug effects
Cell Line, Tumor -
Drug Stability -
Humans -
Immunohistochemistry -
Nanoparticles - chemistry
Neoplasms - metabolism
Particle Size -
Protamines - chemistry
Rats -
Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I - biosynthesis
Receptors, Vasoactive Intestinal Peptide, Type II - biosynthesis
Receptors, Vasoactive Intestinal Polypeptide, Type I - biosynthesis
Spectrometry, Fluorescence -
Vasoactive Intestinal Peptide - administration and dosage
Vasodilation - drug effects

Find related publications in this database (Keywords)
Tumor cell targeting
nanoparticles
proticles
vasoactive intestinal peptide
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