Antiangiogenic cancer therapy using tumor vasculature-targeted liposomes encapsulating 3-(3,5-dimethyl-1H-pyrrol-2-ylmethylene)-1,3-dihydro-indol-2-one, SU5416.

Abstract	Previously, we identified angiogenic vessel-homing peptide Ala-Pro-Arg-Pro-Gly (APRPG), and showed that APRPG-modified liposomes could selectively target to tumor neovasculature. Here, we designed an APRPG-modified liposome encapsulating SU5416, an angiogenesis inhibitor, to overcome the solubility problem, and to enhance the antiangiogenic activity of SU5416. Liposomal SU5416 appeared to have the appropriate characteristics, such as particle size and stability in serum. It showed a significantly lower hemoglobin release than SU5416 dissolved in a Cremophor EL-containing solvent. Compared with peptide-unmodified liposomal SU5416, the APRPG-modified liposomal SU5416 significantly suppressed tumor growth and with no remarkable side effects. Thus, targeted delivery of antiangiogenic drugs with tumor vasculature-targeted liposomes may be useful for antiangiogenic cancer therapy.
Authors	Yasufumi Katanasaka, Tomoko Ida, Tomohiro Asai, Kosuke Shimizu, Fumiaki Koizumi, Noriyuki Maeda, Kazuhiko Baba, Naoto Oku
Journal	Cancer letters (Cancer Lett) Vol. 270 Issue 2 Pg. 260-8 (Nov 08 2008) ISSN: 1872-7980 [Electronic] Ireland
PMID	18555591 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Angiogenesis Inhibitors Indoles Lipids Liposomes Oligopeptides Pyrroles Vascular Endothelial Growth Factor A alanyl-prolyl-arginyl-prolyl-glycine Semaxinib
Topics	Angiogenesis Inhibitors (administration & dosage, chemistry, metabolism, pharmacology) Animals Cell Line, Tumor Cell Proliferation (drug effects) Colonic Neoplasms (blood supply, drug therapy, metabolism, pathology) Dose-Response Relationship, Drug Drug Compounding Drug Stability Endothelial Cells (drug effects, metabolism) Hemolysis (drug effects) Humans Indoles (administration & dosage, chemistry, metabolism, pharmacology) Lipids (chemistry) Liposomes Male Mice Mice, Inbred BALB C Oligopeptides (chemistry, metabolism) Particle Size Pyrroles (administration & dosage, chemistry, metabolism, pharmacology) Solubility Time Factors Vascular Endothelial Growth Factor A (metabolism)

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