Cyclic RGD peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects

Zhiwang Song, Yun Lin, Xia Zhang, Chan Feng, Yonglin Lu, Yong Gao, Chunyan Dong Department of Oncology, Shanghai East Hospital, Tongji University School of Medicine, Shanghai, People’s Republic of China Abstract: Apatinib is an oral tyrosine kinase inhibitor, which selectively targets va...

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Autores principales:	Song Z, Lin Y, Zhang X, Feng C, Lu Y, Gao Y, Dong C
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	Integrin αvβ3 c-RGD targeted oral therapy apatinib colorectal cancer Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/7ebf0ab17c864cc09c777b9020ce3472
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spelling	oai:doaj.org-article:7ebf0ab17c864cc09c777b9020ce34722021-12-02T06:31:50ZCyclic RGD peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects1178-2013https://doaj.org/article/7ebf0ab17c864cc09c777b9020ce34722017-03-01T00:00:00Zhttps://www.dovepress.com/cyclic-rgd-peptide-modified-liposomal-drug-delivery-system-for-targete-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Zhiwang Song, Yun Lin, Xia Zhang, Chan Feng, Yonglin Lu, Yong Gao, Chunyan Dong Department of Oncology, Shanghai East Hospital, Tongji University School of Medicine, Shanghai, People’s Republic of China 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 cancerSong ZLin YZhang XFeng CLu YGao YDong CDove Medical PressarticleIntegrin αvβ3c-RGDtargeted oral therapyapatinibcolorectal cancerMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 1941-1958 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Integrin αvβ3 c-RGD targeted oral therapy apatinib colorectal cancer Medicine (General) R5-920
spellingShingle	Integrin αvβ3 c-RGD targeted oral therapy apatinib colorectal cancer Medicine (General) R5-920 Song Z Lin Y Zhang X Feng C Lu Y Gao Y Dong C Cyclic RGD peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects
description	Zhiwang Song, Yun Lin, Xia Zhang, Chan Feng, Yonglin Lu, Yong Gao, Chunyan Dong Department of Oncology, Shanghai East Hospital, Tongji University School of Medicine, Shanghai, People’s Republic of China 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
format	article
author	Song Z Lin Y Zhang X Feng C Lu Y Gao Y Dong C
author_facet	Song Z Lin Y Zhang X Feng C Lu Y Gao Y Dong C
author_sort	Song Z
title	Cyclic RGD peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects
title_short	Cyclic RGD peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects
title_full	Cyclic RGD peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects
title_fullStr	Cyclic RGD peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects
title_full_unstemmed	Cyclic RGD peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects
title_sort	cyclic rgd peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/7ebf0ab17c864cc09c777b9020ce3472
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Cyclic RGD peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects

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