Determinants for in vivo antitumor effect of angiogenesis inhibitor SU5416 formulated in PEGylated emulsion

Ken-ichi Ogawara, Shigeki Abe, Keita Un, Yuta Yoshizawa, Toshikiro Kimura, Kazutaka Higaki

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4 Citations (Scopus)


Angiogenesis, the sprouting of capillaries from preexisting ones, is essential for the sustained growth of solid tumors. In this study, we used SU5416, a hydrophobic molecule with potent tyrosine kinase inhibitor of type 2 receptor for vascular endothelial growth factor (VEGF), as PEGylated emulsion (SU5416-PE), and evaluated the antitumor potency of this formulation in Lewis lung cancer (LLC), Colon-26 (C26), and B16BL6 melanoma (B16) tumor-bearing mice. Intravenous injection of SU5416-PE into tumor-bearing mice significantly suppressed the growth of C26 and B16 tumors, but had no effect on the growth of LLC tumors. MTT assay revealed that SU5416 inhibited the proliferation of human umbilical vein endothelial cells in a concentration-dependent manner but did not show such an inhibitory effect on all types of tumor cells examined, demonstrating the specificity of SU5416 for endothelial cells. Considering that VEGF levels within C26 and B16 tumors were found to be about 10-fold and 20-fold higher than that in LLC tumors, respectively, it was suggested that SU5416-PE would inhibit angiogenesis in certain types of tumor tissue such as C26 and B16 where VEGF plays a major role for promoting angiogenesis, leading to the suppression of in vivo tumor growth.

Original languageEnglish
Pages (from-to)2464-2469
Number of pages6
JournalJournal of Pharmaceutical Sciences
Issue number8
Publication statusPublished - Aug 2014


  • angiogenesis
  • cancer
  • drug delivery
  • emulsion
  • endothelial
  • solubility
  • vascular endothelial growth factor

ASJC Scopus subject areas

  • Pharmaceutical Science


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