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Authors Song Z, Lin Y, Zhang X, Feng C, Lu Y, Gao Y, Dong C
Received 24 October 2016
Accepted for publication 31 January 2017
Published 10 March 2017 Volume 2017:12 Pages 1941—1958
DOI https://doi.org/10.2147/IJN.S125573
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Akshita Wason
Peer reviewer comments 2
Editor who approved publication: Dr Lei Yang
Abstract: Apatinib is an oral tyrosine kinase inhibitor, which selectively targets
vascular endothelial growth factor receptor 2 and has the potential to treat
many tumors therapeutically. Cyclic arginylglycylaspartic acid (cRGD)- and
polyethylene glycol (PEG)-modified liposomes (cRGD-Lipo-PEG) were constructed
to act as a targeted delivery system for the delivery of apatinib to the human
colonic cancer cell line, HCT116. These cRGD-modified liposomes specifically
recognized integrin αvβ3 and exhibited greater uptake
efficiency with respect to delivering liposomes into HCT116 cells when compared
to nontargeted liposomes (Lipo-PEG), as well as greater death of tumor cells
and apoptosis. The mechanism by which cRGD-Lipo-PEG targets cells was
elucidated further with competition assays. To determine the anticancer
efficacy in vivo, nude mice were implanted with HCT116 xenografts and treated
with apatinib-loaded liposomes or free apatinib intravenously or via
intragastric administration. The active and passive targeting of cRGD-Lipo-PEG
led to significant tumor treatment targeting ability, better inhibition of
tumor growth, and less toxicity when compared with treatments using uncombined
apatinib. The results presented strongly support the case for cRGD-Lipo-PEG
representing a targeted delivery system for apatinib in the treatment of colonic
cancer.
Keywords: integrin αvβ3, cRGD, targeted oral therapy, apatinib, colorectal
cancer