Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

Salma E El-Habashy, Ahmed N Allam, Amal H El-Kamel Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt Abstract: Nanoparticles (NPs) have long gained significant interest for their use in various drug formulations in order to increase bioavailability, prolong...

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Autores principales:	El-Habashy SE, Allam AN, El-Kamel AH
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	Piroxicam ethyl cellulose poloxamer ulcerogenic pharmacokinetics Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/171db9e98d2b4652aa3a11d1a2779eb1
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spelling	oai:doaj.org-article:171db9e98d2b4652aa3a11d1a2779eb12021-12-02T05:00:34ZEthyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation1178-2013https://doaj.org/article/171db9e98d2b4652aa3a11d1a2779eb12016-05-01T00:00:00Zhttps://www.dovepress.com/ethyl-cellulose-nanoparticles-as-a-platform-to-decrease-ulcerogenic-po-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Salma E El-Habashy, Ahmed N Allam, Amal H El-Kamel Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt Abstract: Nanoparticles (NPs) have long gained significant interest for their use in various drug formulations in order to increase bioavailability, prolong drug release, and decrease side effects of highly toxic drugs. The objective of this investigation was to evaluate the potential of ethyl cellulose-based NPs (EC-NPs) to modulate the release and reduce ulcerogenicity of piroxicam (PX) after oral administration. PX-loaded EC-NPs were prepared by solvent evaporation technique using different stabilizers at three concentration levels. Morphological examination of selected formulas confirmed the formation of spherical NPs with slightly porous surface. Formulation containing poloxamer-stabilized EC-NPs (P188/0.2), having a particle size of 240.26±29.24 nm, polydispersity index of 0.562±0.030, entrapment efficiency of 85.29%±1.57%, and modulated release of PX (88% after 12 hours), was selected as the optimum formulation. Differential scanning calorimetry demonstrated the presence of PX in an amorphous form in the NPs. Fourier-transform infrared spectroscopy revealed the possible formation of hydrogen bond and the absence of chemical interaction. In vivo study, evaluation of pharmacokinetic parameters, evaluation of gastric irritation potential, and histological examination were conducted after administration of the selected formulation. Time to reach maximum plasma concentration, tmax, of poloxamer-stabilized EC-NPs was significantly higher than that of Feldene® 20 mg capsules (P≤0.001). Encapsulation of the acidic, gastric offender PX into NPs managed to significantly suppress gastric ulceration potential in rats (P≤0.05) as compared to that of PX suspension. A reduction of 66% in mean ulcer index was observed. In conclusion, poloxamer-stabilized EC-NPs (P188/0.2) had a significant potential of offsetting deleterious side effects common in PX use. Keywords: polymeric nanoparticles, poloxamer, NSAIDs, pharmacokinetics, gastric irritation El-Habashy SEAllam ANEl-Kamel AHDove Medical PressarticlePiroxicamethyl cellulosepoloxamerulcerogenicpharmacokineticsMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 2369-2380 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Piroxicam ethyl cellulose poloxamer ulcerogenic pharmacokinetics Medicine (General) R5-920
spellingShingle	Piroxicam ethyl cellulose poloxamer ulcerogenic pharmacokinetics Medicine (General) R5-920 El-Habashy SE Allam AN El-Kamel AH Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation
description	Salma E El-Habashy, Ahmed N Allam, Amal H El-Kamel Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt Abstract: Nanoparticles (NPs) have long gained significant interest for their use in various drug formulations in order to increase bioavailability, prolong drug release, and decrease side effects of highly toxic drugs. The objective of this investigation was to evaluate the potential of ethyl cellulose-based NPs (EC-NPs) to modulate the release and reduce ulcerogenicity of piroxicam (PX) after oral administration. PX-loaded EC-NPs were prepared by solvent evaporation technique using different stabilizers at three concentration levels. Morphological examination of selected formulas confirmed the formation of spherical NPs with slightly porous surface. Formulation containing poloxamer-stabilized EC-NPs (P188/0.2), having a particle size of 240.26±29.24 nm, polydispersity index of 0.562±0.030, entrapment efficiency of 85.29%±1.57%, and modulated release of PX (88% after 12 hours), was selected as the optimum formulation. Differential scanning calorimetry demonstrated the presence of PX in an amorphous form in the NPs. Fourier-transform infrared spectroscopy revealed the possible formation of hydrogen bond and the absence of chemical interaction. In vivo study, evaluation of pharmacokinetic parameters, evaluation of gastric irritation potential, and histological examination were conducted after administration of the selected formulation. Time to reach maximum plasma concentration, tmax, of poloxamer-stabilized EC-NPs was significantly higher than that of Feldene® 20 mg capsules (P≤0.001). Encapsulation of the acidic, gastric offender PX into NPs managed to significantly suppress gastric ulceration potential in rats (P≤0.05) as compared to that of PX suspension. A reduction of 66% in mean ulcer index was observed. In conclusion, poloxamer-stabilized EC-NPs (P188/0.2) had a significant potential of offsetting deleterious side effects common in PX use. Keywords: polymeric nanoparticles, poloxamer, NSAIDs, pharmacokinetics, gastric irritation
format	article
author	El-Habashy SE Allam AN El-Kamel AH
author_facet	El-Habashy SE Allam AN El-Kamel AH
author_sort	El-Habashy SE
title	Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation
title_short	Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation
title_full	Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation
title_fullStr	Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation
title_full_unstemmed	Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation
title_sort	ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/171db9e98d2b4652aa3a11d1a2779eb1
work_keys_str_mv	AT elhabashyse ethylcellulosenanoparticlesasaplatformtodecreaseulcerogenicpotentialofpiroxicamformulationandinvitroinvivoevaluation AT allaman ethylcellulosenanoparticlesasaplatformtodecreaseulcerogenicpotentialofpiroxicamformulationandinvitroinvivoevaluation AT elkamelah ethylcellulosenanoparticlesasaplatformtodecreaseulcerogenicpotentialofpiroxicamformulationandinvitroinvivoevaluation
_version_	1718400815031386112

Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

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