Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Ahmed O Elzoghby,1 Maged W Helmy,2 Wael M Samy,1,3 Nazik A Elgindy11Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmacology and Toxicology, Faculty of Pharmacy, Pharos University, Alexandria, Egypt; 3Department of Pharmaceutics an...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Elzoghby AO, Helmy MW, Samy WM, Elgindy NA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/b96c3423df2347019d27dae1fc6e2b26
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:b96c3423df2347019d27dae1fc6e2b26
record_format	dspace
spelling	oai:doaj.org-article:b96c3423df2347019d27dae1fc6e2b262021-12-02T02:11:16ZNovel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics1176-91141178-2013https://doaj.org/article/b96c3423df2347019d27dae1fc6e2b262013-05-01T00:00:00Zhttp://www.dovepress.com/novel-ionically-crosslinked-casein-nanoparticles-for-flutamide-deliver-a12943https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Ahmed O Elzoghby,1 Maged W Helmy,2 Wael M Samy,1,3 Nazik A Elgindy11Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmacology and Toxicology, Faculty of Pharmacy, Pharos University, Alexandria, Egypt; 3Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, LebanonAbstract: A novel particulate delivery matrix based on ionically crosslinked casein (CAS) nanoparticles was developed for controlled release of the poorly soluble anticancer drug flutamide (FLT). Nanoparticles were fabricated via oil-in-water emulsification then stabilized by ionic crosslinking of the positively charged CAS molecules below their isoelectric point, with the polyanionic crosslinker sodium tripolyphosphate. With the optimal preparation conditions, the drug loading and incorporation efficiency achieved were 8.73% and 64.55%, respectively. The nanoparticles exhibited a spherical shape with a size below 100 nm and a positive zeta potential (+7.54 to +17.3 mV). FLT was molecularly dispersed inside the nanoparticle protein matrix, as revealed by thermal analysis. The biodegradability of CAS nanoparticles in trypsin solution could be easily modulated by varying the sodium tripolyphosphate crosslinking density. A sustained release of FLT from CAS nanoparticles for up to 4 days was observed, depending on the crosslinking density. After intravenous administration of FLT-CAS nanoparticles into rats, CAS nanoparticles exhibited a longer circulation time and a markedly delayed blood clearance of FLT, with the half-life of FLT extended from 0.88 hours to 14.64 hours, compared with drug cosolvent. The results offer a promising method for tailoring biodegradable, drug-loaded CAS nanoparticles as controlled, long-circulating drug delivery systems of hydrophobic anticancer drugs in aqueous vehicles.Keywords: casein nanoparticles, ionic crosslinking, biodegradability, controlled release, in vivo pharmacokineticsElzoghby AOHelmy MWSamy WMElgindy NADove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 1721-1732 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Elzoghby AO Helmy MW Samy WM Elgindy NA Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics
description	Ahmed O Elzoghby,1 Maged W Helmy,2 Wael M Samy,1,3 Nazik A Elgindy11Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmacology and Toxicology, Faculty of Pharmacy, Pharos University, Alexandria, Egypt; 3Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, LebanonAbstract: A novel particulate delivery matrix based on ionically crosslinked casein (CAS) nanoparticles was developed for controlled release of the poorly soluble anticancer drug flutamide (FLT). Nanoparticles were fabricated via oil-in-water emulsification then stabilized by ionic crosslinking of the positively charged CAS molecules below their isoelectric point, with the polyanionic crosslinker sodium tripolyphosphate. With the optimal preparation conditions, the drug loading and incorporation efficiency achieved were 8.73% and 64.55%, respectively. The nanoparticles exhibited a spherical shape with a size below 100 nm and a positive zeta potential (+7.54 to +17.3 mV). FLT was molecularly dispersed inside the nanoparticle protein matrix, as revealed by thermal analysis. The biodegradability of CAS nanoparticles in trypsin solution could be easily modulated by varying the sodium tripolyphosphate crosslinking density. A sustained release of FLT from CAS nanoparticles for up to 4 days was observed, depending on the crosslinking density. After intravenous administration of FLT-CAS nanoparticles into rats, CAS nanoparticles exhibited a longer circulation time and a markedly delayed blood clearance of FLT, with the half-life of FLT extended from 0.88 hours to 14.64 hours, compared with drug cosolvent. The results offer a promising method for tailoring biodegradable, drug-loaded CAS nanoparticles as controlled, long-circulating drug delivery systems of hydrophobic anticancer drugs in aqueous vehicles.Keywords: casein nanoparticles, ionic crosslinking, biodegradability, controlled release, in vivo pharmacokinetics
format	article
author	Elzoghby AO Helmy MW Samy WM Elgindy NA
author_facet	Elzoghby AO Helmy MW Samy WM Elgindy NA
author_sort	Elzoghby AO
title	Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics
title_short	Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics
title_full	Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics
title_fullStr	Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics
title_full_unstemmed	Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics
title_sort	novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/b96c3423df2347019d27dae1fc6e2b26
work_keys_str_mv	AT elzoghbyao novelionicallycrosslinkedcaseinnanoparticlesforflutamidedeliveryformulationcharacterizationandinvivopharmacokinetics AT helmymw novelionicallycrosslinkedcaseinnanoparticlesforflutamidedeliveryformulationcharacterizationandinvivopharmacokinetics AT samywm novelionicallycrosslinkedcaseinnanoparticlesforflutamidedeliveryformulationcharacterizationandinvivopharmacokinetics AT elgindyna novelionicallycrosslinkedcaseinnanoparticlesforflutamidedeliveryformulationcharacterizationandinvivopharmacokinetics
_version_	1718402673406902272

Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Ejemplares similares