Self-assembled nanoparticles based on amphiphilic chitosan derivative and arginine for oral curcumin delivery

Mazhar Ali Raja, Shah Zeenat, Muhammad Arif, Chenguang Liu College of Marine Life Science, Ocean University of China, Qingdao, Shandong, People’s Republic of China Abstract: Curcumin (Cur) is a striking anticancer agent, but its low aqueous solubility, poor absorption, hasty metabolism,...

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Autores principales:	Raja MA, Zeenat S, Arif M, Liu C
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	Curcumin Acrylonitrile Arginine Chitosan Self-assembled Nanoparticles Cytotoxicity Cell uptake studies Oral bioavailability Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/afecb76deb034f7c9cbe365309159819
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spelling	oai:doaj.org-article:afecb76deb034f7c9cbe3653091598192021-12-02T05:10:44ZSelf-assembled nanoparticles based on amphiphilic chitosan derivative and arginine for oral curcumin delivery1178-2013https://doaj.org/article/afecb76deb034f7c9cbe3653091598192016-09-01T00:00:00Zhttps://www.dovepress.com/self-assembled-nanoparticles-based-on-amphiphilic-chitosan-derivative--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Mazhar Ali Raja, Shah Zeenat, Muhammad Arif, Chenguang Liu College of Marine Life Science, Ocean University of China, Qingdao, Shandong, People’s Republic of China Abstract: Curcumin (Cur) is a striking anticancer agent, but its low aqueous solubility, poor absorption, hasty metabolism, and elimination limit its oral bioavailability and consequently hinder its development as a drug. To redress these limitations, amphiphilic chitosan (CS) conjugate with improved mucoadhesion and solubility over a wider pH range was developed by modification with hydrophobic acrylonitrile (AN) and hydrophilic arginine (Arg); the synthesized conjugate (AN–CS–Arg), which was well characterized by Fourier transform infrared and 1H nuclear magnetic resonance spectroscopy. Results of critical aggregation concentration revealed that the AN–CS–Arg conjugate had low critical aggregation concentration and was prone to form self-assembled nanoparticles (NPs) in aqueous medium. Cur-encapsulated AN–CS–Arg NPs (AN–CS–Arg/Cur NPs) were developed by a simple sonication method and characterized for the physicochemical parameters such as zeta potential, particle size, and drug encapsulation. The results showed that zeta potential of the prepared NPs was 40.1±2.81 mV and the average size was ~218 nm. A considerable improvement in the aqueous solubility of Cur was observed after encapsulation into AN–CS–Arg/Cur NPs. With the increase in Cur concentration, loading efficiency increased but encapsulation efficiency decreased. The in vitro release profile exhibited sustained release pattern from the AN–CS–Arg/Cur NPs in typical biological buffers. The ex vivo mucoadhesion study revealed that AN–CS–Arg/Cur NPs had greater mucoadhesion than the control CS NPs. Compared with free Cur solution, AN–CS–Arg/Cur NPs showed stronger dose-dependent cytotoxicity against HT-29 cells. In addition, it was observed that cell uptake of AN–CS–Arg/Cur NPs was much higher compared with free Cur. Furthermore, the in vivo pharmacokinetic results in rats demonstrated that the AN–CS–Arg/Cur NPs could remarkably improve the oral bioavailability of Cur. Therefore, the developed AN–CS–Arg/Cur NPs might be a promising nano-candidate for oral delivery of Cur. Keywords: curcumin, self-assembled, nanoparticles, cytotoxicity, cell uptake studies, oral bioavailabilityRaja MAZeenat SArif MLiu CDove Medical PressarticleCurcuminAcrylonitrileArginineChitosanSelf-assembledNanoparticlesCytotoxicityCell uptake studiesOral bioavailabilityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 11, Pp 4397-4412 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Curcumin Acrylonitrile Arginine Chitosan Self-assembled Nanoparticles Cytotoxicity Cell uptake studies Oral bioavailability Medicine (General) R5-920
spellingShingle	Curcumin Acrylonitrile Arginine Chitosan Self-assembled Nanoparticles Cytotoxicity Cell uptake studies Oral bioavailability Medicine (General) R5-920 Raja MA Zeenat S Arif M Liu C Self-assembled nanoparticles based on amphiphilic chitosan derivative and arginine for oral curcumin delivery
description	Mazhar Ali Raja, Shah Zeenat, Muhammad Arif, Chenguang Liu College of Marine Life Science, Ocean University of China, Qingdao, Shandong, People’s Republic of China Abstract: Curcumin (Cur) is a striking anticancer agent, but its low aqueous solubility, poor absorption, hasty metabolism, and elimination limit its oral bioavailability and consequently hinder its development as a drug. To redress these limitations, amphiphilic chitosan (CS) conjugate with improved mucoadhesion and solubility over a wider pH range was developed by modification with hydrophobic acrylonitrile (AN) and hydrophilic arginine (Arg); the synthesized conjugate (AN–CS–Arg), which was well characterized by Fourier transform infrared and 1H nuclear magnetic resonance spectroscopy. Results of critical aggregation concentration revealed that the AN–CS–Arg conjugate had low critical aggregation concentration and was prone to form self-assembled nanoparticles (NPs) in aqueous medium. Cur-encapsulated AN–CS–Arg NPs (AN–CS–Arg/Cur NPs) were developed by a simple sonication method and characterized for the physicochemical parameters such as zeta potential, particle size, and drug encapsulation. The results showed that zeta potential of the prepared NPs was 40.1±2.81 mV and the average size was ~218 nm. A considerable improvement in the aqueous solubility of Cur was observed after encapsulation into AN–CS–Arg/Cur NPs. With the increase in Cur concentration, loading efficiency increased but encapsulation efficiency decreased. The in vitro release profile exhibited sustained release pattern from the AN–CS–Arg/Cur NPs in typical biological buffers. The ex vivo mucoadhesion study revealed that AN–CS–Arg/Cur NPs had greater mucoadhesion than the control CS NPs. Compared with free Cur solution, AN–CS–Arg/Cur NPs showed stronger dose-dependent cytotoxicity against HT-29 cells. In addition, it was observed that cell uptake of AN–CS–Arg/Cur NPs was much higher compared with free Cur. Furthermore, the in vivo pharmacokinetic results in rats demonstrated that the AN–CS–Arg/Cur NPs could remarkably improve the oral bioavailability of Cur. Therefore, the developed AN–CS–Arg/Cur NPs might be a promising nano-candidate for oral delivery of Cur. Keywords: curcumin, self-assembled, nanoparticles, cytotoxicity, cell uptake studies, oral bioavailability
format	article
author	Raja MA Zeenat S Arif M Liu C
author_facet	Raja MA Zeenat S Arif M Liu C
author_sort	Raja MA
title	Self-assembled nanoparticles based on amphiphilic chitosan derivative and arginine for oral curcumin delivery
title_short	Self-assembled nanoparticles based on amphiphilic chitosan derivative and arginine for oral curcumin delivery
title_full	Self-assembled nanoparticles based on amphiphilic chitosan derivative and arginine for oral curcumin delivery
title_fullStr	Self-assembled nanoparticles based on amphiphilic chitosan derivative and arginine for oral curcumin delivery
title_full_unstemmed	Self-assembled nanoparticles based on amphiphilic chitosan derivative and arginine for oral curcumin delivery
title_sort	self-assembled nanoparticles based on amphiphilic chitosan derivative and arginine for oral curcumin delivery
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/afecb76deb034f7c9cbe365309159819
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Self-assembled nanoparticles based on amphiphilic chitosan derivative and arginine for oral curcumin delivery

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