Novel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical “apocynin”

Hend Mohamed Anter,1 Irhan Ibrahim Abu Hashim,1 Walaa Awadin,2 Mahasen Mohamed Meshali11Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Dakahlia 35516, Egypt; 2Department of Pathology, Faculty of Veterinary Medicine, Mansoura University, Mansoura, Dakahlia 35516, Egy...

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Autores principales:	Anter HM, Abu Hashim II, Awadin W, Meshali MM
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Apocynin Chitosan oligosaccharide Tripolyphosphate Nanoparticles Antiulcerogenic activity Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/6f69e7d6a2054d21870e97589b0d9e84
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spelling	oai:doaj.org-article:6f69e7d6a2054d21870e97589b0d9e842021-12-02T06:43:42ZNovel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical “apocynin”1178-2013https://doaj.org/article/6f69e7d6a2054d21870e97589b0d9e842019-07-01T00:00:00Zhttps://www.dovepress.com/novel-chitosan-oligosaccharide-based-nanoparticles-for-gastric-mucosal-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Hend Mohamed Anter,1 Irhan Ibrahim Abu Hashim,1 Walaa Awadin,2 Mahasen Mohamed Meshali11Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Dakahlia 35516, Egypt; 2Department of Pathology, Faculty of Veterinary Medicine, Mansoura University, Mansoura, Dakahlia 35516, EgyptBackground: Apocynin (APO) is a bioactive phytochemical with prominent anti-inflammatory and anti-oxidant activities. Designing a nano-delivery system targeted to potentiate the gastric antiulcerogenic activity of APO has not been investigated yet. Chitosan oligosaccharide (COS) is a low molecular weight chitosan and its oral nanoparticulate system for potentiating the antiulcerogenic activity of the loaded APO has been described here.Methods: COS-nanoparticles (NPs) loaded with APO (using tripolyphosphate [TPP] as a cross-linker) were prepared by ionic gelation method and fully characterized. The chosen formula was extensively evaluated regarding in vitro release profile, kinetic analysis, and stability at refrigerated and room temperatures. Ultimately, the in vivo antiulcerogenic activity against ketoprofen (KP)-induced gastric ulceration in rats was assessed by macroscopic parameters including Paul’s index and antiulcerogenic activity, histopathological examination, immunohistochemical (IHC) evaluation of cyclooxygenase-2 (COX-2) expression level in ulcerated gastric tissue, and biochemical measurement of oxidative stress markers and nitric oxide (NO) levels.Results: The selected NPs formula with COS (0.5 % w/v) and TPP (0.1% w/v) was the most appropriate one with drug entrapment efficiency percentage of 35.06%, particle size of 436.20 nm, zeta potential of +38.20 mV, and mucoadhesive strength of 51.22%. It exhibited a biphasic in vitro release pattern as well as high stability at refrigerated temperature for a 6-month storage period. APO-loaded COS-NPs provoked marvelous antiulcerogenic activity against KP-induced gastric ulceration in rats compared with free APO treated group, which was emphasized by histopathological, IHC, and biochemical studies.Conclusion: In conclusion, APO-loaded COS-NPs could be considered as a promising oral phytopharmaceutical nanoparticulate system for management of gastric ulceration.Keywords: apocynin, chitosan oligosaccharide, tripolyphosphate, nanoparticles, antiulcerogenic activityAnter HMAbu Hashim IIAwadin WMeshali MMDove Medical PressarticleApocyninChitosan oligosaccharideTripolyphosphateNanoparticlesAntiulcerogenic activityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 4911-4929 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Apocynin Chitosan oligosaccharide Tripolyphosphate Nanoparticles Antiulcerogenic activity Medicine (General) R5-920
spellingShingle	Apocynin Chitosan oligosaccharide Tripolyphosphate Nanoparticles Antiulcerogenic activity Medicine (General) R5-920 Anter HM Abu Hashim II Awadin W Meshali MM Novel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical “apocynin”
description	Hend Mohamed Anter,1 Irhan Ibrahim Abu Hashim,1 Walaa Awadin,2 Mahasen Mohamed Meshali11Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Dakahlia 35516, Egypt; 2Department of Pathology, Faculty of Veterinary Medicine, Mansoura University, Mansoura, Dakahlia 35516, EgyptBackground: Apocynin (APO) is a bioactive phytochemical with prominent anti-inflammatory and anti-oxidant activities. Designing a nano-delivery system targeted to potentiate the gastric antiulcerogenic activity of APO has not been investigated yet. Chitosan oligosaccharide (COS) is a low molecular weight chitosan and its oral nanoparticulate system for potentiating the antiulcerogenic activity of the loaded APO has been described here.Methods: COS-nanoparticles (NPs) loaded with APO (using tripolyphosphate [TPP] as a cross-linker) were prepared by ionic gelation method and fully characterized. The chosen formula was extensively evaluated regarding in vitro release profile, kinetic analysis, and stability at refrigerated and room temperatures. Ultimately, the in vivo antiulcerogenic activity against ketoprofen (KP)-induced gastric ulceration in rats was assessed by macroscopic parameters including Paul’s index and antiulcerogenic activity, histopathological examination, immunohistochemical (IHC) evaluation of cyclooxygenase-2 (COX-2) expression level in ulcerated gastric tissue, and biochemical measurement of oxidative stress markers and nitric oxide (NO) levels.Results: The selected NPs formula with COS (0.5 % w/v) and TPP (0.1% w/v) was the most appropriate one with drug entrapment efficiency percentage of 35.06%, particle size of 436.20 nm, zeta potential of +38.20 mV, and mucoadhesive strength of 51.22%. It exhibited a biphasic in vitro release pattern as well as high stability at refrigerated temperature for a 6-month storage period. APO-loaded COS-NPs provoked marvelous antiulcerogenic activity against KP-induced gastric ulceration in rats compared with free APO treated group, which was emphasized by histopathological, IHC, and biochemical studies.Conclusion: In conclusion, APO-loaded COS-NPs could be considered as a promising oral phytopharmaceutical nanoparticulate system for management of gastric ulceration.Keywords: apocynin, chitosan oligosaccharide, tripolyphosphate, nanoparticles, antiulcerogenic activity
format	article
author	Anter HM Abu Hashim II Awadin W Meshali MM
author_facet	Anter HM Abu Hashim II Awadin W Meshali MM
author_sort	Anter HM
title	Novel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical “apocynin”
title_short	Novel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical “apocynin”
title_full	Novel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical “apocynin”
title_fullStr	Novel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical “apocynin”
title_full_unstemmed	Novel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical “apocynin”
title_sort	novel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical “apocynin”
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/6f69e7d6a2054d21870e97589b0d9e84
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Novel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical &ldquo;apocynin&rdquo;

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Novel chitosan oligosaccharide-based nanoparticles for gastric mucosal administration of the phytochemical “apocynin”