Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers

Abdel-Rahim M El-Helw, Usama A FahmyDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaAbstract: The aim of this study is to prepare fluvastatin nanostructured lipid carriers (FLV-NLCs) in order to find an innovative way to allevi...

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Autores principales:	El-Helw AR, Fahmy UA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/6022330a73674e74b9dc6a234b617c83
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spelling	oai:doaj.org-article:6022330a73674e74b9dc6a234b617c832021-12-02T06:31:49ZImprovement of fluvastatin bioavailability by loading on nanostructured lipid carriers1178-2013https://doaj.org/article/6022330a73674e74b9dc6a234b617c832015-09-01T00:00:00Zhttps://www.dovepress.com/improvement-of-fluvastatin-bioavailability-by-loading-on-nanostructure-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Abdel-Rahim M El-Helw, Usama A FahmyDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaAbstract: The aim of this study is to prepare fluvastatin nanostructured lipid carriers (FLV-NLCs) in order to find an innovative way to alleviate FLV-associated disadvantages. The limitations include poor solubility and extensive first-pass metabolism, resulting in low (30%) bioavailability and short elimination half-life (1–3 hours). FLV-NLCs were prepared by hot emulsification–ultrasonication method. Ten runs were created by three-level factorial design (32) to optimize FLV-NLCs formulation process. In this study, two factors, four responses, and three-level factorial design were endorsed. The studied variables were lipid:oil ratio (X1) and sonication time (X2). However, the responses parameter determined the particle size (Y1, nm), entrapment efficiency percent (EE%, Y2), particles zeta potential (Y3), and 80% of the drug release after 24 hours (X4). Furthermore, stability and in vivo pharmacokinetics were studied in rats. The optimized consisted formula had an average particle size of 165 nm with 75.32% entrapment efficiency and 85.32% of drug released after 24 hours, demonstrating a sustaining drug release over 24 hours. An in vivo pharmacokinetic study revealed enhanced bioavailability by >2.64-fold, and the mean residence time was longer than that of FLV. We concluded that NLCs could be promising carriers for sustained/prolonged FLV release with enhanced oral bioavailability.Keywords: factorial design, nano-vesicles, hyperlipidemia, statinsEl-Helw ARFahmy UADove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 5797-5804 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 El-Helw AR Fahmy UA Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers
description	Abdel-Rahim M El-Helw, Usama A FahmyDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaAbstract: The aim of this study is to prepare fluvastatin nanostructured lipid carriers (FLV-NLCs) in order to find an innovative way to alleviate FLV-associated disadvantages. The limitations include poor solubility and extensive first-pass metabolism, resulting in low (30%) bioavailability and short elimination half-life (1–3 hours). FLV-NLCs were prepared by hot emulsification–ultrasonication method. Ten runs were created by three-level factorial design (32) to optimize FLV-NLCs formulation process. In this study, two factors, four responses, and three-level factorial design were endorsed. The studied variables were lipid:oil ratio (X1) and sonication time (X2). However, the responses parameter determined the particle size (Y1, nm), entrapment efficiency percent (EE%, Y2), particles zeta potential (Y3), and 80% of the drug release after 24 hours (X4). Furthermore, stability and in vivo pharmacokinetics were studied in rats. The optimized consisted formula had an average particle size of 165 nm with 75.32% entrapment efficiency and 85.32% of drug released after 24 hours, demonstrating a sustaining drug release over 24 hours. An in vivo pharmacokinetic study revealed enhanced bioavailability by >2.64-fold, and the mean residence time was longer than that of FLV. We concluded that NLCs could be promising carriers for sustained/prolonged FLV release with enhanced oral bioavailability.Keywords: factorial design, nano-vesicles, hyperlipidemia, statins
format	article
author	El-Helw AR Fahmy UA
author_facet	El-Helw AR Fahmy UA
author_sort	El-Helw AR
title	Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers
title_short	Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers
title_full	Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers
title_fullStr	Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers
title_full_unstemmed	Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers
title_sort	improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/6022330a73674e74b9dc6a234b617c83
work_keys_str_mv	AT elhelwar improvementoffluvastatinbioavailabilitybyloadingonnanostructuredlipidcarriers AT fahmyua improvementoffluvastatinbioavailabilitybyloadingonnanostructuredlipidcarriers
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Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers

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