Optimized zein nanospheres for improved oral bioavailability of atorvastatin

Fahima M Hashem,1 Majid M Al-Sawahli,2 Mohamed Nasr,1 Osama AA Ahmed3,4 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, 2Holding Company for Biological Products and Vaccines, Giza, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Facu...

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Autores principales:	Hashem FM, Al-Sawahli MM, Nasr M, Ahmed OA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/693e85a0d6024f68b04938429605a990
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spelling	oai:doaj.org-article:693e85a0d6024f68b04938429605a9902021-12-02T04:28:17ZOptimized zein nanospheres for improved oral bioavailability of atorvastatin1178-2013https://doaj.org/article/693e85a0d6024f68b04938429605a9902015-06-01T00:00:00Zhttp://www.dovepress.com/optimized-zein-nanospheres-for-improved-oral-bioavailability-of-atorva-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Fahima M Hashem,1 Majid M Al-Sawahli,2 Mohamed Nasr,1 Osama AA Ahmed3,4 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, 2Holding Company for Biological Products and Vaccines, Giza, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; 4Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt Background: This work focuses on the development of atorvastatin utilizing zein, a natural, safe, and biocompatible polymer, as a nanosized formulation in order to overcome the poor oral bioavailability (12%) of the drug. Methods: Twelve experimental runs of atorvastatin–zein nanosphere formula were formulated by a liquid–liquid phase separation method according to custom fractional factorial design to optimize the formulation variables. The factors studied were: weight % of zein to atorvastatin (X1), pH (X2), and stirring time (X3). Levels for each formulation variable were designed. The selected dependent variables were: mean particle size (Y1), zeta potential (Y2), drug loading efficiency (Y3), drug encapsulation efficiency (Y4), and yield (Y5). The optimized formulation was assayed for compatibility using an X-ray diffraction assay. In vitro diffusion of the optimized formulation was carried out. A pharmacokinetic study was also done to compare the plasma profile of the atorvastatin–zein nanosphere formulation versus atorvastatin oral suspension and the commercially available tablet. Results: The optimized atorvastatin–zein formulation had a mean particle size of 183 nm, a loading efficiency of 14.86%, and an encapsulation efficiency of 29.71%. The in vitro dissolution assay displayed an initial burst effect, with a cumulative amount of atorvastatin released of 41.76% and 82.3% after 12 and 48 hours, respectively. In Wistar albino rats, the bioavailability of atorvastatin from the optimized atorvastatin–zein formulation was 3-fold greater than that from the atorvastatin suspension and the commercially available tablet. Conclusion: The atorvastatin–zein nanosphere formulation improved the oral delivery and pharmacokinetic profile of atorvastatin by enhancing its oral bioavailability. Keywords: nanoparticles, optimization, experimental design, fractional factorial designHashem FMAl-Sawahli MMNasr MAhmed OADove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 4059-4069 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Hashem FM Al-Sawahli MM Nasr M Ahmed OA Optimized zein nanospheres for improved oral bioavailability of atorvastatin
description	Fahima M Hashem,1 Majid M Al-Sawahli,2 Mohamed Nasr,1 Osama AA Ahmed3,4 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, 2Holding Company for Biological Products and Vaccines, Giza, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; 4Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt Background: This work focuses on the development of atorvastatin utilizing zein, a natural, safe, and biocompatible polymer, as a nanosized formulation in order to overcome the poor oral bioavailability (12%) of the drug. Methods: Twelve experimental runs of atorvastatin–zein nanosphere formula were formulated by a liquid–liquid phase separation method according to custom fractional factorial design to optimize the formulation variables. The factors studied were: weight % of zein to atorvastatin (X1), pH (X2), and stirring time (X3). Levels for each formulation variable were designed. The selected dependent variables were: mean particle size (Y1), zeta potential (Y2), drug loading efficiency (Y3), drug encapsulation efficiency (Y4), and yield (Y5). The optimized formulation was assayed for compatibility using an X-ray diffraction assay. In vitro diffusion of the optimized formulation was carried out. A pharmacokinetic study was also done to compare the plasma profile of the atorvastatin–zein nanosphere formulation versus atorvastatin oral suspension and the commercially available tablet. Results: The optimized atorvastatin–zein formulation had a mean particle size of 183 nm, a loading efficiency of 14.86%, and an encapsulation efficiency of 29.71%. The in vitro dissolution assay displayed an initial burst effect, with a cumulative amount of atorvastatin released of 41.76% and 82.3% after 12 and 48 hours, respectively. In Wistar albino rats, the bioavailability of atorvastatin from the optimized atorvastatin–zein formulation was 3-fold greater than that from the atorvastatin suspension and the commercially available tablet. Conclusion: The atorvastatin–zein nanosphere formulation improved the oral delivery and pharmacokinetic profile of atorvastatin by enhancing its oral bioavailability. Keywords: nanoparticles, optimization, experimental design, fractional factorial design
format	article
author	Hashem FM Al-Sawahli MM Nasr M Ahmed OA
author_facet	Hashem FM Al-Sawahli MM Nasr M Ahmed OA
author_sort	Hashem FM
title	Optimized zein nanospheres for improved oral bioavailability of atorvastatin
title_short	Optimized zein nanospheres for improved oral bioavailability of atorvastatin
title_full	Optimized zein nanospheres for improved oral bioavailability of atorvastatin
title_fullStr	Optimized zein nanospheres for improved oral bioavailability of atorvastatin
title_full_unstemmed	Optimized zein nanospheres for improved oral bioavailability of atorvastatin
title_sort	optimized zein nanospheres for improved oral bioavailability of atorvastatin
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/693e85a0d6024f68b04938429605a990
work_keys_str_mv	AT hashemfm optimizedzeinnanospheresforimprovedoralbioavailabilityofatorvastatin AT alsawahlimm optimizedzeinnanospheresforimprovedoralbioavailabilityofatorvastatin AT nasrm optimizedzeinnanospheresforimprovedoralbioavailabilityofatorvastatin AT ahmedoa optimizedzeinnanospheresforimprovedoralbioavailabilityofatorvastatin
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Optimized zein nanospheres for improved oral bioavailability of atorvastatin

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