Anti-Colorectal Cancer Effect via Application of Polyethylene Glycol Modified Liposomal Apatinib.

Metastatic colorectal cancer is a stumbling block in colorectal cancer management due to limited treatment approaches and unfavorable prognosis. Angiogenesis is essential in tumor development and metastasis. Vascular endothelial growth factor receptor (VEGFR) targeted anti-angiogenesis drugs have gain inspiring achievements in cancer treatment. Apatinib is a novel small molecular VEGFR-2 tyrosine kinase targeted drug with poor water-solubility, showing anti-tumor ability in some solid tumors. In this study, PEG modified liposomal Apatinib (Apatinib-Lipo/PEG) was synthesized and applied for colorectal cancer treatment. Results showed that Apatinib-Lipo/PEG could attenuate proliferation and induce apoptosis of CT26 cells. Moreover, Apatinib-Lipo/PEG significantly reduced tumor growth in colorectal peritoneal model as well as subcutaneous model without obvious toxicity. The anti-tumor mechanisms included inhibiting tumor proliferation, promoting tumor apoptosis and suppressing tumor angiogenesis. Thereafter, the application of Apatinib-Lipo/PEG would be very promising in colorectal cancer treatment.