Preparation of Cationic Amphiphilic Nanoparticles with Modified Chitosan Derivatives for Doxorubicin Delivery

Polymeric micelle-like nanoparticles have demonstrated effectiveness for the delivery of some poorly soluble or hydrophobic anticancer drugs. In this study, a hydrophobic moiety, deoxycholic acid (DCA) was first bonded on a polysaccharide, chitosan (CS), for the preparation of amphiphilic chitosan (...

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Autores principales: Xiudong Liu, Huofei Zhou, Weiting Yu, Xin Xiong, Rumen Krastev, Xiaojun Ma
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Publicado: MDPI AG 2021
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spelling oai:doaj.org-article:d7dc7d719a53461d936425a5b8d3c25b2021-11-25T18:15:39ZPreparation of Cationic Amphiphilic Nanoparticles with Modified Chitosan Derivatives for Doxorubicin Delivery10.3390/ma142270101996-1944https://doaj.org/article/d7dc7d719a53461d936425a5b8d3c25b2021-11-01T00:00:00Zhttps://www.mdpi.com/1996-1944/14/22/7010https://doaj.org/toc/1996-1944Polymeric micelle-like nanoparticles have demonstrated effectiveness for the delivery of some poorly soluble or hydrophobic anticancer drugs. In this study, a hydrophobic moiety, deoxycholic acid (DCA) was first bonded on a polysaccharide, chitosan (CS), for the preparation of amphiphilic chitosan (CS-DCA), which was further modified with a cationic glycidyltrimethylammounium chloride (GTMAC) to form a novel soluble chitosan derivative (HT-CS-DCA). The cationic amphiphilic HT-CS-DCA was easily self-assembled to micelle-like nanoparticles about 200 nm with narrow size distribution (PDI 0.08–0.18). The zeta potential of nanoparticles was in the range of 14 to 24 mV, indicating higher positive charges. Then, doxorubicin (DOX), an anticancer drug with poor solubility, was entrapped into HT-CS-DCA nanoparticles. The DOX release test was performed in PBS (pH 7.4) at 37 °C, and the results showed that there was no significant burst release in the first two hours, and the cumulative release increased steadily and slowly in the following hours. HT-CS-DCA nanoparticles loaded with DOX could easily enter into MCF-7 cells, as observed by a confocal microscope. As a result, DOX-loaded HT-CS-DCA nanoparticles demonstrated a significant inhibition activity on MCF-7 growth without obvious cellular toxicity in comparison with blank nanoparticles. Therefore, the anticancer efficacy of these cationic HT-CS-DCA nanoparticles showed great promise for the delivery of DOX in cancer therapy.Xiudong LiuHuofei ZhouWeiting YuXin XiongRumen KrastevXiaojun MaMDPI AGarticlecationic amphiphilic chitosanself-assembled nanoparticlesdoxorubicindrug deliveryTechnologyTElectrical engineering. Electronics. Nuclear engineeringTK1-9971Engineering (General). Civil engineering (General)TA1-2040MicroscopyQH201-278.5Descriptive and experimental mechanicsQC120-168.85ENMaterials, Vol 14, Iss 7010, p 7010 (2021)
institution DOAJ
collection DOAJ
language EN
topic cationic amphiphilic chitosan
self-assembled nanoparticles
doxorubicin
drug delivery
Technology
T
Electrical engineering. Electronics. Nuclear engineering
TK1-9971
Engineering (General). Civil engineering (General)
TA1-2040
Microscopy
QH201-278.5
Descriptive and experimental mechanics
QC120-168.85
spellingShingle cationic amphiphilic chitosan
self-assembled nanoparticles
doxorubicin
drug delivery
Technology
T
Electrical engineering. Electronics. Nuclear engineering
TK1-9971
Engineering (General). Civil engineering (General)
TA1-2040
Microscopy
QH201-278.5
Descriptive and experimental mechanics
QC120-168.85
Xiudong Liu
Huofei Zhou
Weiting Yu
Xin Xiong
Rumen Krastev
Xiaojun Ma
Preparation of Cationic Amphiphilic Nanoparticles with Modified Chitosan Derivatives for Doxorubicin Delivery
description Polymeric micelle-like nanoparticles have demonstrated effectiveness for the delivery of some poorly soluble or hydrophobic anticancer drugs. In this study, a hydrophobic moiety, deoxycholic acid (DCA) was first bonded on a polysaccharide, chitosan (CS), for the preparation of amphiphilic chitosan (CS-DCA), which was further modified with a cationic glycidyltrimethylammounium chloride (GTMAC) to form a novel soluble chitosan derivative (HT-CS-DCA). The cationic amphiphilic HT-CS-DCA was easily self-assembled to micelle-like nanoparticles about 200 nm with narrow size distribution (PDI 0.08–0.18). The zeta potential of nanoparticles was in the range of 14 to 24 mV, indicating higher positive charges. Then, doxorubicin (DOX), an anticancer drug with poor solubility, was entrapped into HT-CS-DCA nanoparticles. The DOX release test was performed in PBS (pH 7.4) at 37 °C, and the results showed that there was no significant burst release in the first two hours, and the cumulative release increased steadily and slowly in the following hours. HT-CS-DCA nanoparticles loaded with DOX could easily enter into MCF-7 cells, as observed by a confocal microscope. As a result, DOX-loaded HT-CS-DCA nanoparticles demonstrated a significant inhibition activity on MCF-7 growth without obvious cellular toxicity in comparison with blank nanoparticles. Therefore, the anticancer efficacy of these cationic HT-CS-DCA nanoparticles showed great promise for the delivery of DOX in cancer therapy.
format article
author Xiudong Liu
Huofei Zhou
Weiting Yu
Xin Xiong
Rumen Krastev
Xiaojun Ma
author_facet Xiudong Liu
Huofei Zhou
Weiting Yu
Xin Xiong
Rumen Krastev
Xiaojun Ma
author_sort Xiudong Liu
title Preparation of Cationic Amphiphilic Nanoparticles with Modified Chitosan Derivatives for Doxorubicin Delivery
title_short Preparation of Cationic Amphiphilic Nanoparticles with Modified Chitosan Derivatives for Doxorubicin Delivery
title_full Preparation of Cationic Amphiphilic Nanoparticles with Modified Chitosan Derivatives for Doxorubicin Delivery
title_fullStr Preparation of Cationic Amphiphilic Nanoparticles with Modified Chitosan Derivatives for Doxorubicin Delivery
title_full_unstemmed Preparation of Cationic Amphiphilic Nanoparticles with Modified Chitosan Derivatives for Doxorubicin Delivery
title_sort preparation of cationic amphiphilic nanoparticles with modified chitosan derivatives for doxorubicin delivery
publisher MDPI AG
publishDate 2021
url https://doaj.org/article/d7dc7d719a53461d936425a5b8d3c25b
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AT huofeizhou preparationofcationicamphiphilicnanoparticleswithmodifiedchitosanderivativesfordoxorubicindelivery
AT weitingyu preparationofcationicamphiphilicnanoparticleswithmodifiedchitosanderivativesfordoxorubicindelivery
AT xinxiong preparationofcationicamphiphilicnanoparticleswithmodifiedchitosanderivativesfordoxorubicindelivery
AT rumenkrastev preparationofcationicamphiphilicnanoparticleswithmodifiedchitosanderivativesfordoxorubicindelivery
AT xiaojunma preparationofcationicamphiphilicnanoparticleswithmodifiedchitosanderivativesfordoxorubicindelivery
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