Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation

Myoung-Ki Baek,1,* Jong-Hwa Lee,2,* Young-Ho Cho,3 Hak-Hyung Kim,4 Gye-Won Lee3 1Life Science R&amp;D Park, SK Biopharmaceuticals Co, LTD, Daejeon, Republic of Korea; 2Toxicology Center, Korea Institute of Toxicology, Daejeon, Republic of Korea; 3Department of Pharmaceutical Engineering, Kon...

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Autores principales:	Baek MK, Lee JH, Cho YH, Kim HH, Lee GW
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/0c389c5119554a35a9d426d47e07e673
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spelling	oai:doaj.org-article:0c389c5119554a35a9d426d47e07e6732021-12-02T02:30:32ZSelf-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation1176-91141178-2013https://doaj.org/article/0c389c5119554a35a9d426d47e07e6732013-01-01T00:00:00Zhttp://www.dovepress.com/self-microemulsifying-drug-delivery-system-for-improved-oral-bioavail-a11879https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Myoung-Ki Baek,1,* Jong-Hwa Lee,2,* Young-Ho Cho,3 Hak-Hyung Kim,4 Gye-Won Lee3 1Life Science R&amp;D Park, SK Biopharmaceuticals Co, LTD, Daejeon, Republic of Korea; 2Toxicology Center, Korea Institute of Toxicology, Daejeon, Republic of Korea; 3Department of Pharmaceutical Engineering, Konyang University, Nonsan, Republic of Korea; 4R&amp;D Center, Pharvis Korea Pharm, Ansan, Republic of Korea *These authors contributed equally to this workAbstract: The purpose of the present investigation was to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) for improving the oral absorption of a pranlukast hemihydrate (PLH), a very poorly water-soluble drug. An efficient self-microemulsifying vehicle for PLH was selected and optimized using solubility testing and phase diagram construction. The formulations were characterized by assessing self-emulsification performance, droplet size analysis, in vitro drug release characteristics and formulation stability studies. Optimized formulations for in vitro dissolution and bioavailability assessment were Triethylcitrate (TEC; 10%), Tween 20 (50%), Span 20 (25%), triethanolamine (5%), and benzyl alcohol (10%). The SMEDDS readily released the lipid phase to form a fine oil-in-water microemulsion with a narrow distribution size. Saturated solubilities of PLH from SMEDDS in water, pH 4.0 and 6.8, were over 150 times greater than that of plain PLH. The release of 100% PLH from SMEDDS was considerably greater compared to only 1.12% in simulated intestinal fluid (pH 6.8) from plain PLH after 2 hours. The PLH suspension with 0.5% sodium carboxymethylcellulose or 3% PLH-loaded SMEDDS was administrated at a dose of 40 mg/kg as PLH to fasted rats. The absorption of PLH from SMEDDS resulted in about a threefold increase in bioavailability compared with plain PLH aqueous suspension. Our studies illustrated that the potential use of the new SMEDDS can be used as a possible alternative to oral delivery of a poorly water-soluble drug such as PLH.Keywords: pranlukast hemihydrates, PLH, SMEDDS, bioavailability, solubilityBaek MKLee JHCho YHKim HHLee GWDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 167-176 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Baek MK Lee JH Cho YH Kim HH Lee GW Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation
description	Myoung-Ki Baek,1,* Jong-Hwa Lee,2,* Young-Ho Cho,3 Hak-Hyung Kim,4 Gye-Won Lee3 1Life Science R&amp;D Park, SK Biopharmaceuticals Co, LTD, Daejeon, Republic of Korea; 2Toxicology Center, Korea Institute of Toxicology, Daejeon, Republic of Korea; 3Department of Pharmaceutical Engineering, Konyang University, Nonsan, Republic of Korea; 4R&amp;D Center, Pharvis Korea Pharm, Ansan, Republic of Korea *These authors contributed equally to this workAbstract: The purpose of the present investigation was to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) for improving the oral absorption of a pranlukast hemihydrate (PLH), a very poorly water-soluble drug. An efficient self-microemulsifying vehicle for PLH was selected and optimized using solubility testing and phase diagram construction. The formulations were characterized by assessing self-emulsification performance, droplet size analysis, in vitro drug release characteristics and formulation stability studies. Optimized formulations for in vitro dissolution and bioavailability assessment were Triethylcitrate (TEC; 10%), Tween 20 (50%), Span 20 (25%), triethanolamine (5%), and benzyl alcohol (10%). The SMEDDS readily released the lipid phase to form a fine oil-in-water microemulsion with a narrow distribution size. Saturated solubilities of PLH from SMEDDS in water, pH 4.0 and 6.8, were over 150 times greater than that of plain PLH. The release of 100% PLH from SMEDDS was considerably greater compared to only 1.12% in simulated intestinal fluid (pH 6.8) from plain PLH after 2 hours. The PLH suspension with 0.5% sodium carboxymethylcellulose or 3% PLH-loaded SMEDDS was administrated at a dose of 40 mg/kg as PLH to fasted rats. The absorption of PLH from SMEDDS resulted in about a threefold increase in bioavailability compared with plain PLH aqueous suspension. Our studies illustrated that the potential use of the new SMEDDS can be used as a possible alternative to oral delivery of a poorly water-soluble drug such as PLH.Keywords: pranlukast hemihydrates, PLH, SMEDDS, bioavailability, solubility
format	article
author	Baek MK Lee JH Cho YH Kim HH Lee GW
author_facet	Baek MK Lee JH Cho YH Kim HH Lee GW
author_sort	Baek MK
title	Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation
title_short	Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation
title_full	Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation
title_fullStr	Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation
title_full_unstemmed	Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation
title_sort	self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/0c389c5119554a35a9d426d47e07e673
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Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation

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