Thiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation

Shahrooz Saremi1,4, Fatemeh Atyabi1,2, Seyedeh Parinaz Akhlaghi1, Seyed Nasser Ostad3, Rassoul Dinarvand1,21Department of Pharmaceutics, 2Nanotechnology Research Centre, 3Department of Toxicology and Pharmacology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; 4R&a...

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Autores principales:	Shahrooz Saremi, Fatemeh Atyabi, Seyedeh Parinaz Akhlaghi, et al
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/a71015c418c24a7ab519ecaf82fbfe4f
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spelling	oai:doaj.org-article:a71015c418c24a7ab519ecaf82fbfe4f2021-12-02T07:37:02ZThiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation1176-91141178-2013https://doaj.org/article/a71015c418c24a7ab519ecaf82fbfe4f2011-01-01T00:00:00Zhttp://www.dovepress.com/thiolated-chitosan-nanoparticles-for-enhancing-oral-absorption-of-doce-a6049https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Shahrooz Saremi1,4, Fatemeh Atyabi1,2, Seyedeh Parinaz Akhlaghi1, Seyed Nasser Ostad3, Rassoul Dinarvand1,21Department of Pharmaceutics, 2Nanotechnology Research Centre, 3Department of Toxicology and Pharmacology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; 4R&amp;D Department, Osvah Pharmaceutical Co., Tehran, IranAbstract: The aim of this study was to prepare and evaluate mucoadhesive core-shell nanoparticles based on copolymerization of thiolated chitosan coated on poly methyl methacrylate cores as a carrier for oral delivery of docetaxel. Docetaxel-loaded nanoparticles with various concentrations were prepared via a radical emulsion polymerization method using cerium ammonium nitrate as an initiator. The physicochemical properties of the obtained nanoparticles were characterized by: dynamic light-scattering analysis for their mean size, size distribution, and zeta potential; scanning electron microscopy and transmission electron microscopy for surface morphology; and differential scanning calorimetry analysis for confirmation of molecular dispersity of docetaxel in the nanoparticles. Nanoparticles were spherical with mean diameter below 200 nm, polydispersity of below 0.15, and positive zeta potential values. The entrapment efficiency of the nanoparticles was approximately 90%. In vitro release studies showed a sustained release characteristic for 10 days after a burst release at the beginning. Ex vivo studies showed a significant increase in the transportation of docetaxel from intestinal membrane of rat when formulated as nanoparticles. Cellular uptake of nanoparticles was investigated using fluoresceinamine-loaded nanoparticles. Docetaxel nanoparticles showed a high cytotoxicity effect in the Caco-2 and MCF-7 cell lines after 72 hours. It can be concluded that by combining the advantages of both thiolated polymers and colloidal particles, these nanoparticles can be proposed as a drug carrier system for mucosal delivery of hydrophobic drugs.Keywords: poly methyl methacrylate, mucoadhesive, cytotoxicity Shahrooz SaremiFatemeh AtyabiSeyedeh Parinaz Akhlaghiet alDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 119-128 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Shahrooz Saremi Fatemeh Atyabi Seyedeh Parinaz Akhlaghi et al Thiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation
description	Shahrooz Saremi1,4, Fatemeh Atyabi1,2, Seyedeh Parinaz Akhlaghi1, Seyed Nasser Ostad3, Rassoul Dinarvand1,21Department of Pharmaceutics, 2Nanotechnology Research Centre, 3Department of Toxicology and Pharmacology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; 4R&amp;D Department, Osvah Pharmaceutical Co., Tehran, IranAbstract: The aim of this study was to prepare and evaluate mucoadhesive core-shell nanoparticles based on copolymerization of thiolated chitosan coated on poly methyl methacrylate cores as a carrier for oral delivery of docetaxel. Docetaxel-loaded nanoparticles with various concentrations were prepared via a radical emulsion polymerization method using cerium ammonium nitrate as an initiator. The physicochemical properties of the obtained nanoparticles were characterized by: dynamic light-scattering analysis for their mean size, size distribution, and zeta potential; scanning electron microscopy and transmission electron microscopy for surface morphology; and differential scanning calorimetry analysis for confirmation of molecular dispersity of docetaxel in the nanoparticles. Nanoparticles were spherical with mean diameter below 200 nm, polydispersity of below 0.15, and positive zeta potential values. The entrapment efficiency of the nanoparticles was approximately 90%. In vitro release studies showed a sustained release characteristic for 10 days after a burst release at the beginning. Ex vivo studies showed a significant increase in the transportation of docetaxel from intestinal membrane of rat when formulated as nanoparticles. Cellular uptake of nanoparticles was investigated using fluoresceinamine-loaded nanoparticles. Docetaxel nanoparticles showed a high cytotoxicity effect in the Caco-2 and MCF-7 cell lines after 72 hours. It can be concluded that by combining the advantages of both thiolated polymers and colloidal particles, these nanoparticles can be proposed as a drug carrier system for mucosal delivery of hydrophobic drugs.Keywords: poly methyl methacrylate, mucoadhesive, cytotoxicity
format	article
author	Shahrooz Saremi Fatemeh Atyabi Seyedeh Parinaz Akhlaghi et al
author_facet	Shahrooz Saremi Fatemeh Atyabi Seyedeh Parinaz Akhlaghi et al
author_sort	Shahrooz Saremi
title	Thiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation
title_short	Thiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation
title_full	Thiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation
title_fullStr	Thiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation
title_full_unstemmed	Thiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation
title_sort	thiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/a71015c418c24a7ab519ecaf82fbfe4f
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Thiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation

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