Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication

Marwa Ahmed Sallam,1 María Teresa Marín Boscá21Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Granada University, Granada, Spain Abstract: I...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Sallam MA, Marín Boscá MT
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/3f1e869e101e40d5b06b9f34057932fe
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:3f1e869e101e40d5b06b9f34057932fe
record_format	dspace
spelling	oai:doaj.org-article:3f1e869e101e40d5b06b9f34057932fe2021-12-02T04:33:06ZOptimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication1178-2013https://doaj.org/article/3f1e869e101e40d5b06b9f34057932fe2015-07-01T00:00:00Zhttp://www.dovepress.com/optimization-ex-vivo-permeation-and-stability-study-of-lipid-nanocarri-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Marwa Ahmed Sallam,1 María Teresa Marín Boscá21Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Granada University, Granada, Spain Abstract: In this study, an optimized nanodispersible oral dosage form (containing a lactate ester) was developed for cilostazol (CZL). CZL is a phosphodiesterase inhibitor used for intermittent claudication. We aimed to improve the dissolution rate and absorption of CZL giving it a better chance of oral bioavailability, and to evaluate its stability on storage. Suitable compositions of nanoemulsion preconcentrate formulations were screened via solubility and compatibility tests. Response surface methodology and a desirability approach were applied to optimize preconcentrates containing minimum amount of surfactant mixture, maximum amount of lipid, and possessing the smallest globule size, with the highest emulsification and dissolution rates and minimum risk of drug precipitation. As part of the optimization process, the main effect, interaction effects and quadratic effects of amounts of lipid, and surfactant/co-surfactant ratio on % transmittance, globule size, emulsification time, drug precipitation, and drug release were investigated. The optimized formulation consisting of 28.9% butyl lactate, 28.9% Capryol®, 27.82% Solubilisant Gamma® 2429, and 14.18% Transcutol® possessing a globule size of 60 nm was mixed with Aerosil® 200. This gave uniform free flowing granules, which were characterized for surface and powder properties. The self-nanoemulsifying granules (SNEGs) filled into hard gelatin capsules showed two- and threefold increase in CZL released compared with conventional tablet and pure drug, respectively. The amount of drug permeated using non-everted sac technique from the SNEGs was twofold higher than that permeated from the tablet suspension. The shelf life was 526 days at 25°C. Our study illustrated that the developed SNEGs, with bioenhancing ingredients, held great potential as a superior alternative to traditional oral formulations of CZL.Keywords: butyl lactate, preconcentrates, cilostazol, desirability, Solubilisant GammaSallam MAMarín Boscá MTDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 4459-4478 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Sallam MA Marín Boscá MT Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication
description	Marwa Ahmed Sallam,1 María Teresa Marín Boscá21Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Granada University, Granada, Spain Abstract: In this study, an optimized nanodispersible oral dosage form (containing a lactate ester) was developed for cilostazol (CZL). CZL is a phosphodiesterase inhibitor used for intermittent claudication. We aimed to improve the dissolution rate and absorption of CZL giving it a better chance of oral bioavailability, and to evaluate its stability on storage. Suitable compositions of nanoemulsion preconcentrate formulations were screened via solubility and compatibility tests. Response surface methodology and a desirability approach were applied to optimize preconcentrates containing minimum amount of surfactant mixture, maximum amount of lipid, and possessing the smallest globule size, with the highest emulsification and dissolution rates and minimum risk of drug precipitation. As part of the optimization process, the main effect, interaction effects and quadratic effects of amounts of lipid, and surfactant/co-surfactant ratio on % transmittance, globule size, emulsification time, drug precipitation, and drug release were investigated. The optimized formulation consisting of 28.9% butyl lactate, 28.9% Capryol®, 27.82% Solubilisant Gamma® 2429, and 14.18% Transcutol® possessing a globule size of 60 nm was mixed with Aerosil® 200. This gave uniform free flowing granules, which were characterized for surface and powder properties. The self-nanoemulsifying granules (SNEGs) filled into hard gelatin capsules showed two- and threefold increase in CZL released compared with conventional tablet and pure drug, respectively. The amount of drug permeated using non-everted sac technique from the SNEGs was twofold higher than that permeated from the tablet suspension. The shelf life was 526 days at 25°C. Our study illustrated that the developed SNEGs, with bioenhancing ingredients, held great potential as a superior alternative to traditional oral formulations of CZL.Keywords: butyl lactate, preconcentrates, cilostazol, desirability, Solubilisant Gamma
format	article
author	Sallam MA Marín Boscá MT
author_facet	Sallam MA Marín Boscá MT
author_sort	Sallam MA
title	Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication
title_short	Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication
title_full	Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication
title_fullStr	Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication
title_full_unstemmed	Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication
title_sort	optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/3f1e869e101e40d5b06b9f34057932fe
work_keys_str_mv	AT sallamma optimizationexvivopermeationandstabilitystudyoflipidnanocarrierloadedgelatincapsulesfortreatmentofintermittentclaudication AT mariacutenboscaacutemt optimizationexvivopermeationandstabilitystudyoflipidnanocarrierloadedgelatincapsulesfortreatmentofintermittentclaudication
_version_	1718401178325221376

Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication

Ejemplares similares