Peptide-targeted PEG-liposomes in anti-angiogenic therapy

Peptides with the RGD amino acid sequence show affinity for the alpha(v)beta(3) integrin, an integrin which is over-expressed on angiogenic endothelium and involved in cell adhesion. A peptide with the sequence ATWLPPR has been demonstrated to show affinity for the vascular endothelial growth factor...

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Bibliographic Details
Published in:International journal of pharmaceutics 2003-03, Vol.254 (1), p.55-58
Main Authors: Janssen, A.P.C.A, Schiffelers, R.M, ten Hagen, T.L.M, Koning, G.A, Schraa, A.J, Kok, R.J, Storm, G, Molema, G
Format: Article
Language:English
Subjects:
Angiogenesis
Angiogenesis Inhibitors - administration & dosage
Angiogenesis Inhibitors - therapeutic use
Animals
Biological and medical sciences
Carcinoma, Lewis Lung - drug therapy
Carcinoma, Lewis Lung - metabolism
Cells, Cultured
Drug Carriers
Drug Delivery Systems
Endothelial cells
Endothelium, Vascular - drug effects
Endothelium, Vascular - metabolism
Flow Cytometry - instrumentation
Flow Cytometry - methods
General pharmacology
Humans
In Vitro Techniques
Liposomes
Liposomes - chemistry
Medical sciences
Mice
Microscopy, Confocal - instrumentation
Microscopy, Confocal - methods
Neovascularization, Pathologic - drug therapy
Oligopeptides - chemistry
Peptide Fragments - administration & dosage
Peptide Fragments - chemistry
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polyethylene Glycols - chemistry
Receptors, Vascular Endothelial Growth Factor - metabolism
RGD-peptides
Time Factors
Transplants
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Description
Summary:Peptides with the RGD amino acid sequence show affinity for the alpha(v)beta(3) integrin, an integrin which is over-expressed on angiogenic endothelium and involved in cell adhesion. A peptide with the sequence ATWLPPR has been demonstrated to show affinity for the vascular endothelial growth factor (VEGF) receptor, a receptor involved in the proliferation of endothelial cells. By coupling these peptides to liposomes, these liposomes can serve as a site-specific drug delivery system to tumor endothelial cells in order to inhibit angiogenesis. In the present study we demonstrate that the coupling of cyclic RGD-peptides or ATWLPPR-peptides to the surface of PEG-liposomes results in binding of these liposomes to endothelial cells in vitro. Subsequent studies with RGD-peptide targeted liposomes in vivo also demonstrate specific binding to the tumor endothelium.
ISSN:0378-5173
1873-3476
DOI:10.1016/S0378-5173(02)00682-8