Mechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride

Osama Abdelhakim Aly Ahmed,1,2 Ahmed Samir Zidan,1,3 Maan Khayat4 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt; 3D...

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Autores principales:	Ahmed OAA, Zidan AS, Khayat M
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	Glimepiride Zein Nanoparticles Quality by design In-situ implants Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/fc2dd3d8823d4b7dab4619bd4002aa7f
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spelling	oai:doaj.org-article:fc2dd3d8823d4b7dab4619bd4002aa7f2021-12-02T02:10:26ZMechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride1178-2013https://doaj.org/article/fc2dd3d8823d4b7dab4619bd4002aa7f2016-02-01T00:00:00Zhttps://www.dovepress.com/mechanistic-analysis-of-zein-nanoparticlesplga-triblock-in-situ-formin-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Osama Abdelhakim Aly Ahmed,1,2 Ahmed Samir Zidan,1,3 Maan Khayat4 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt; 4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia Objectives: The study aims at applying pharmaceutical nanotechnology and D-optimal fractional factorial design to screen and optimize the high-risk variables affecting the performance of a complex drug delivery system consisting of glimepiride–Zein nanoparticles and inclusion of the optimized formula with thermoresponsive triblock copolymers in in situ gel. Methods: Sixteen nanoparticle formulations were prepared by liquid–liquid phase separation method according to the D-optimal fractional factorial design encompassing five variables at two levels. The responses investigated were glimepiride entrapment capacity (EC), particle size and size distribution, zeta potential, and in vitro drug release from the prepared nanoparticles. Furthermore, the feasibility of embedding the optimized Zein-based glimepiride nanoparticles within thermoresponsive triblock copolymers poly(lactide-co-glycolide)-block-poly(ethylene glycol)-block-poly(lactide-co-glycolide) in in situ gel was evaluated for controlling glimepiride release rate. Results: Through the systematic optimization phase, improvement of glimepiride EC of 33.6%, nanoparticle size of 120.9 nm with a skewness value of 0.2, zeta potential of 11.1 mV, and sustained release features of 3.3% and 17.3% drug released after 2 and 24 hours, respectively, were obtained. These desirability functions were obtained at Zein and glimepiride loadings of 50 and 75 mg, respectively, utilizing didodecyldimethylammonium bromide as a stabilizer at 0.1% and 90% ethanol as a common solvent. Moreover, incorporating this optimized formulation in triblock copolymers-based in situ gel demonstrated pseudoplastic behavior with reduction of drug release rate as the concentration of polymer increased. Conclusion: This approach to control the release of glimepiride using Zein nanoparticles/triblock copolymers-based in situ gel forming intramuscular implants could be useful for improving diabetes treatment effectiveness. Keywords: glimepiride, Zein, nanoparticles, quality by design, in situ implantsAhmed OAAZidan ASKhayat MDove Medical PressarticleGlimepirideZeinNanoparticlesQuality by designIn-situ implantsMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss Issue 1, Pp 543-555 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Glimepiride Zein Nanoparticles Quality by design In-situ implants Medicine (General) R5-920
spellingShingle	Glimepiride Zein Nanoparticles Quality by design In-situ implants Medicine (General) R5-920 Ahmed OAA Zidan AS Khayat M Mechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride
description	Osama Abdelhakim Aly Ahmed,1,2 Ahmed Samir Zidan,1,3 Maan Khayat4 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt; 4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia Objectives: The study aims at applying pharmaceutical nanotechnology and D-optimal fractional factorial design to screen and optimize the high-risk variables affecting the performance of a complex drug delivery system consisting of glimepiride–Zein nanoparticles and inclusion of the optimized formula with thermoresponsive triblock copolymers in in situ gel. Methods: Sixteen nanoparticle formulations were prepared by liquid–liquid phase separation method according to the D-optimal fractional factorial design encompassing five variables at two levels. The responses investigated were glimepiride entrapment capacity (EC), particle size and size distribution, zeta potential, and in vitro drug release from the prepared nanoparticles. Furthermore, the feasibility of embedding the optimized Zein-based glimepiride nanoparticles within thermoresponsive triblock copolymers poly(lactide-co-glycolide)-block-poly(ethylene glycol)-block-poly(lactide-co-glycolide) in in situ gel was evaluated for controlling glimepiride release rate. Results: Through the systematic optimization phase, improvement of glimepiride EC of 33.6%, nanoparticle size of 120.9 nm with a skewness value of 0.2, zeta potential of 11.1 mV, and sustained release features of 3.3% and 17.3% drug released after 2 and 24 hours, respectively, were obtained. These desirability functions were obtained at Zein and glimepiride loadings of 50 and 75 mg, respectively, utilizing didodecyldimethylammonium bromide as a stabilizer at 0.1% and 90% ethanol as a common solvent. Moreover, incorporating this optimized formulation in triblock copolymers-based in situ gel demonstrated pseudoplastic behavior with reduction of drug release rate as the concentration of polymer increased. Conclusion: This approach to control the release of glimepiride using Zein nanoparticles/triblock copolymers-based in situ gel forming intramuscular implants could be useful for improving diabetes treatment effectiveness. Keywords: glimepiride, Zein, nanoparticles, quality by design, in situ implants
format	article
author	Ahmed OAA Zidan AS Khayat M
author_facet	Ahmed OAA Zidan AS Khayat M
author_sort	Ahmed OAA
title	Mechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride
title_short	Mechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride
title_full	Mechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride
title_fullStr	Mechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride
title_full_unstemmed	Mechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride
title_sort	mechanistic analysis of zein nanoparticles/plga triblock in situ forming implants for glimepiride
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/fc2dd3d8823d4b7dab4619bd4002aa7f
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Mechanistic analysis of Zein nanoparticles/PLGA triblock in situ forming implants for glimepiride

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