Galactosylated chitosan-functionalized mesoporous silica nanoparticles for efficient colon cancer cell-targeted drug delivery

Targeted drug delivery to colon cancer cells can significantly enhance the therapeutic efficiency. Herein, we developed 5-fluorouracil (5-FU)-loaded amino-functionalized mesoporous silica nanoparticle (MSN-NH2)-based galactosylated chitosans (GCs), which are galactose receptor-mediated materials for...

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Main Authors: Wei Liu, Yongchao Zhu, Fan Wang, Xue Li, Xiaojing Liu, Jingjing Pang, Weisan Pan
Format: Article
Language:English
Published: The Royal Society 2018-01-01
Series:Royal Society Open Science
Subjects:
Online Access:https://royalsocietypublishing.org/doi/pdf/10.1098/rsos.181027
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author Wei Liu
Yongchao Zhu
Fan Wang
Xue Li
Xiaojing Liu
Jingjing Pang
Weisan Pan
author_facet Wei Liu
Yongchao Zhu
Fan Wang
Xue Li
Xiaojing Liu
Jingjing Pang
Weisan Pan
author_sort Wei Liu
collection DOAJ
description Targeted drug delivery to colon cancer cells can significantly enhance the therapeutic efficiency. Herein, we developed 5-fluorouracil (5-FU)-loaded amino-functionalized mesoporous silica nanoparticle (MSN-NH2)-based galactosylated chitosans (GCs), which are galactose receptor-mediated materials for colon-specific drug delivery systems. Both unmodified and functionalized nanoparticles were characterized by scanning electron microscopy, transmission electron microscopy, X-ray diffraction, Fourier transform infrared spectroscopy, nitrogen sorption and dynamic light scattering. Drug loading capacity and drug release properties were determined by ultraviolet spectrophotometry. 5-FU@MSN-NH2/GC showed high loading capacity and possessed much higher cytotoxicity on human colon cancer cells (SW620 cells) than 5-FU@MSN-NH2 and free 5-FU. But, MSN-NH2/GC did not show significant cytotoxicity. Subsequently, 5-FU@MSN-NH2/GC anti-cancer activity on SW620 cells in vitro was confirmed by cell apoptosis. These results are consistent with the cellular uptake test in which MSN-NH2/GC could specifically recognize and bind to cancer cells by the galectin-receptor recognition. But, it is found that pre-addition of galactose in the medium, leading to competitive binding to the galectin receptor of SW620 cells, resulted in a decrease in the binding of MSN-NH2/GC to the galectin receptor. The results demonstrated the inorganic–organic nanocomposite could be used as a promising drug delivery carrier for the targeted delivery of drug into galectin-positive colon cancer cells to improve therapeutic index while reducing side effects.
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spelling doaj.art-55437e7a55f749499819f617c22458942022-12-21T19:32:07ZengThe Royal SocietyRoyal Society Open Science2054-57032018-01-0151210.1098/rsos.181027181027Galactosylated chitosan-functionalized mesoporous silica nanoparticles for efficient colon cancer cell-targeted drug deliveryWei LiuYongchao ZhuFan WangXue LiXiaojing LiuJingjing PangWeisan PanTargeted drug delivery to colon cancer cells can significantly enhance the therapeutic efficiency. Herein, we developed 5-fluorouracil (5-FU)-loaded amino-functionalized mesoporous silica nanoparticle (MSN-NH2)-based galactosylated chitosans (GCs), which are galactose receptor-mediated materials for colon-specific drug delivery systems. Both unmodified and functionalized nanoparticles were characterized by scanning electron microscopy, transmission electron microscopy, X-ray diffraction, Fourier transform infrared spectroscopy, nitrogen sorption and dynamic light scattering. Drug loading capacity and drug release properties were determined by ultraviolet spectrophotometry. 5-FU@MSN-NH2/GC showed high loading capacity and possessed much higher cytotoxicity on human colon cancer cells (SW620 cells) than 5-FU@MSN-NH2 and free 5-FU. But, MSN-NH2/GC did not show significant cytotoxicity. Subsequently, 5-FU@MSN-NH2/GC anti-cancer activity on SW620 cells in vitro was confirmed by cell apoptosis. These results are consistent with the cellular uptake test in which MSN-NH2/GC could specifically recognize and bind to cancer cells by the galectin-receptor recognition. But, it is found that pre-addition of galactose in the medium, leading to competitive binding to the galectin receptor of SW620 cells, resulted in a decrease in the binding of MSN-NH2/GC to the galectin receptor. The results demonstrated the inorganic–organic nanocomposite could be used as a promising drug delivery carrier for the targeted delivery of drug into galectin-positive colon cancer cells to improve therapeutic index while reducing side effects.https://royalsocietypublishing.org/doi/pdf/10.1098/rsos.181027galactosylated chitosan5-fluorouracilmesoporous silicacolon cancer
spellingShingle Wei Liu
Yongchao Zhu
Fan Wang
Xue Li
Xiaojing Liu
Jingjing Pang
Weisan Pan
Galactosylated chitosan-functionalized mesoporous silica nanoparticles for efficient colon cancer cell-targeted drug delivery
Royal Society Open Science
galactosylated chitosan
5-fluorouracil
mesoporous silica
colon cancer
title Galactosylated chitosan-functionalized mesoporous silica nanoparticles for efficient colon cancer cell-targeted drug delivery
title_full Galactosylated chitosan-functionalized mesoporous silica nanoparticles for efficient colon cancer cell-targeted drug delivery
title_fullStr Galactosylated chitosan-functionalized mesoporous silica nanoparticles for efficient colon cancer cell-targeted drug delivery
title_full_unstemmed Galactosylated chitosan-functionalized mesoporous silica nanoparticles for efficient colon cancer cell-targeted drug delivery
title_short Galactosylated chitosan-functionalized mesoporous silica nanoparticles for efficient colon cancer cell-targeted drug delivery
title_sort galactosylated chitosan functionalized mesoporous silica nanoparticles for efficient colon cancer cell targeted drug delivery
topic galactosylated chitosan
5-fluorouracil
mesoporous silica
colon cancer
url https://royalsocietypublishing.org/doi/pdf/10.1098/rsos.181027
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AT fanwang galactosylatedchitosanfunctionalizedmesoporoussilicananoparticlesforefficientcoloncancercelltargeteddrugdelivery
AT xueli galactosylatedchitosanfunctionalizedmesoporoussilicananoparticlesforefficientcoloncancercelltargeteddrugdelivery
AT xiaojingliu galactosylatedchitosanfunctionalizedmesoporoussilicananoparticlesforefficientcoloncancercelltargeteddrugdelivery
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