Design of cationic nanostructured heterolipid matrices for ocular delivery of methazolamide

John Youshia, Amany O Kamel, Abdelhameed El Shamy, Samar MansourPharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Ain Shams University, Cairo, EgyptAbstract: Solid lipid nanoparticles (SLNs) formulated from one type of lipid (homolipid) suffer from low drug encapsulation and dru...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Youshia J, Kamel AO, El Shamy A, Mansour S
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/51b6eaafd13041a7aa15a2abe82a7ba4
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:51b6eaafd13041a7aa15a2abe82a7ba4
record_format	dspace
spelling	oai:doaj.org-article:51b6eaafd13041a7aa15a2abe82a7ba42021-12-02T01:29:49ZDesign of cationic nanostructured heterolipid matrices for ocular delivery of methazolamide1176-91141178-2013https://doaj.org/article/51b6eaafd13041a7aa15a2abe82a7ba42012-05-01T00:00:00Zhttp://www.dovepress.com/design-of-cationic-nanostructured-heterolipid-matrices-for-ocular-deli-a9917https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013John Youshia, Amany O Kamel, Abdelhameed El Shamy, Samar MansourPharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Ain Shams University, Cairo, EgyptAbstract: Solid lipid nanoparticles (SLNs) formulated from one type of lipid (homolipid) suffer from low drug encapsulation and drug bursting due to crystallization of the lipid into the more ordered &beta; modification, which leads to decreased drug entrapment and faster drug release. This study assessed the feasibility of using nanostructured lipid matrices (NLMs) for ocular delivery of methazolamide-(MZA) adopting heterolipids composed of novel mixtures of Compritol&reg; and cetostearyl alcohol (CSA), and stabilized by Tween 80&reg;. The systems were prepared using the modified high shear homogenization followed by ultrasonication method, which avoids the use of organic solvents. A 32 full factorial design was constructed to study the influence of two independent variables, namely the ratio of CSA:Compritol and the concentration of Tween 80, each in three levels. The dependent variables were the entrapment efficiency percentages (EE%), mean particle size (PS), polydispersity index (PDI), and zeta potential (ZP). In vivo intraocular pressure (IOP) lowering activity for the selected formulae was compared to that of MZA solution. The results showed that increasing the ratio of CSA to Compritol increased the EE% and PS, while increasing the concentration of Tween 80, decreased PS with no significant effect on EE%. The ZP values of all formulae were positive, and greater than 30 mV. The best formula, composed of 4% CSA, 2% Compritol, 0.15% stearylamine, and 2% Tween 80, with EE% of 25.62%, PS of 207.1 nm, PDI of 0.243, and ZP of 41.50 mV, showed in vitro sustained release properties for 8 hours and lowered the intraocular pressure by 8.3 mmHg within 3 hours, with this drop in pressure lasting for 12 hours.Keywords: nanostructured lipid matrices, heterolipids, factorial design, cetostearyl alcohol, methazolamide, ocular deliveryYoushia JKamel AOEl Shamy AMansour SDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 2483-2496 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Youshia J Kamel AO El Shamy A Mansour S Design of cationic nanostructured heterolipid matrices for ocular delivery of methazolamide
description	John Youshia, Amany O Kamel, Abdelhameed El Shamy, Samar MansourPharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Ain Shams University, Cairo, EgyptAbstract: Solid lipid nanoparticles (SLNs) formulated from one type of lipid (homolipid) suffer from low drug encapsulation and drug bursting due to crystallization of the lipid into the more ordered &beta; modification, which leads to decreased drug entrapment and faster drug release. This study assessed the feasibility of using nanostructured lipid matrices (NLMs) for ocular delivery of methazolamide-(MZA) adopting heterolipids composed of novel mixtures of Compritol&reg; and cetostearyl alcohol (CSA), and stabilized by Tween 80&reg;. The systems were prepared using the modified high shear homogenization followed by ultrasonication method, which avoids the use of organic solvents. A 32 full factorial design was constructed to study the influence of two independent variables, namely the ratio of CSA:Compritol and the concentration of Tween 80, each in three levels. The dependent variables were the entrapment efficiency percentages (EE%), mean particle size (PS), polydispersity index (PDI), and zeta potential (ZP). In vivo intraocular pressure (IOP) lowering activity for the selected formulae was compared to that of MZA solution. The results showed that increasing the ratio of CSA to Compritol increased the EE% and PS, while increasing the concentration of Tween 80, decreased PS with no significant effect on EE%. The ZP values of all formulae were positive, and greater than 30 mV. The best formula, composed of 4% CSA, 2% Compritol, 0.15% stearylamine, and 2% Tween 80, with EE% of 25.62%, PS of 207.1 nm, PDI of 0.243, and ZP of 41.50 mV, showed in vitro sustained release properties for 8 hours and lowered the intraocular pressure by 8.3 mmHg within 3 hours, with this drop in pressure lasting for 12 hours.Keywords: nanostructured lipid matrices, heterolipids, factorial design, cetostearyl alcohol, methazolamide, ocular delivery
format	article
author	Youshia J Kamel AO El Shamy A Mansour S
author_facet	Youshia J Kamel AO El Shamy A Mansour S
author_sort	Youshia J
title	Design of cationic nanostructured heterolipid matrices for ocular delivery of methazolamide
title_short	Design of cationic nanostructured heterolipid matrices for ocular delivery of methazolamide
title_full	Design of cationic nanostructured heterolipid matrices for ocular delivery of methazolamide
title_fullStr	Design of cationic nanostructured heterolipid matrices for ocular delivery of methazolamide
title_full_unstemmed	Design of cationic nanostructured heterolipid matrices for ocular delivery of methazolamide
title_sort	design of cationic nanostructured heterolipid matrices for ocular delivery of methazolamide
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/51b6eaafd13041a7aa15a2abe82a7ba4
work_keys_str_mv	AT youshiaj designofcationicnanostructuredheterolipidmatricesforoculardeliveryofmethazolamide AT kamelao designofcationicnanostructuredheterolipidmatricesforoculardeliveryofmethazolamide AT elshamya designofcationicnanostructuredheterolipidmatricesforoculardeliveryofmethazolamide AT mansours designofcationicnanostructuredheterolipidmatricesforoculardeliveryofmethazolamide
_version_	1718403012092755968

Design of cationic nanostructured heterolipid matrices for ocular delivery of methazolamide

Ejemplares similares