Self-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid

Chang-Shun Liu,1– 3 Li Chen,4 Yan-Nan Hu,1– 3 Jin-Lian Dai,4 Biao Ma,4 Qing-Fa Tang,1– 3 Xiao-Mei Tan1– 3 1School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, People’s Republic of China; 2Guangdong Provincial Key La...

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Autores principales:	Liu CS, Chen L, Hu YN, Dai JL, Ma B, Tang QF, Tan XM
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2020
Materias:	insomnia ferulic acid oral administration pharmacokinetics smedds Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/daa50f31db874dc2b0b3814e86fe0e92
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spelling	oai:doaj.org-article:daa50f31db874dc2b0b3814e86fe0e922021-12-02T08:15:40ZSelf-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid1178-2013https://doaj.org/article/daa50f31db874dc2b0b3814e86fe0e922020-03-01T00:00:00Zhttps://www.dovepress.com/self-microemulsifying-drug-delivery-system-for-improved-oral-delivery--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Chang-Shun Liu,1– 3 Li Chen,4 Yan-Nan Hu,1– 3 Jin-Lian Dai,4 Biao Ma,4 Qing-Fa Tang,1– 3 Xiao-Mei Tan1– 3 1School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, People’s Republic of China; 2Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Southern Medical University, Guangzhou 510515, People’s Republic of China; 3Guangdong Provincial Engineering Laboratory of Chinese Medicine Preparation Technology, Southern Medical University, Guangzhou 510515, People’s Republic of China; 4School of Pharmacy, Zunyi Medical University, Zunyi 563000, People’s Republic of ChinaCorrespondence: Li Chen; Xiao-Mei Tan Email zmu_cl@126.com; tanxm_smu@163.comPurpose: Ferulic acid (FA) is a natural compound which is used to treat insomnia. However, its use is limited because of its poor oral bioavailability caused by extremely rapid elimination. The current study aimed to develop a self-microemulsifying drug delivery system (SMEDDS) to improve the oral delivery of FA and to enhance its hypnotic efficacy.Methods: FA-SMEDDS was prepared, and its morphology and storage stability were characterized. The formulation was also subjected to pharmacokinetic and tissue distribution studies in rats. The hypnotic efficacy of FA-SMEDDS was evaluated in p-chlorophenylalanine-induced insomnia mice.Results: FA-loaded SMEDDS exhibited a small droplet size (15.24 nm) and good stability. Oral administration of FA-SMEDDS yielded relative bioavailability of 185.96%. In the kidney, SMEDDS decreased the distribution percentage of FA from 76.1% to 59.4% and significantly reduced its metabolic conversion, indicating a reduction in renal elimination. Interestingly, FA-SMEDDS showed a higher distribution in the brain and enhanced serotonin levels in the brain, which extended the sleep time by 2-fold in insomnia mice.Conclusion: This is the first study to show that FA-loaded SMEDDS decreased renal elimination, enhanced oral bioavailability, increased brain distribution, and improved hypnotic efficacy. Thus, we have demonstrated that SMEDDS is a promising carrier which can be employed to improve the oral delivery of FA and facilitate product development for the therapy of insomnia.Keywords: insomnia, ferulic acid, oral administration, pharmacokinetics, SMEDDSLiu CSChen LHu YNDai JLMa BTang QFTan XMDove Medical Pressarticleinsomniaferulic acidoral administrationpharmacokineticssmeddsMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 2059-2070 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	insomnia ferulic acid oral administration pharmacokinetics smedds Medicine (General) R5-920
spellingShingle	insomnia ferulic acid oral administration pharmacokinetics smedds Medicine (General) R5-920 Liu CS Chen L Hu YN Dai JL Ma B Tang QF Tan XM Self-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid
description	Chang-Shun Liu,1– 3 Li Chen,4 Yan-Nan Hu,1– 3 Jin-Lian Dai,4 Biao Ma,4 Qing-Fa Tang,1– 3 Xiao-Mei Tan1– 3 1School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, People’s Republic of China; 2Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Southern Medical University, Guangzhou 510515, People’s Republic of China; 3Guangdong Provincial Engineering Laboratory of Chinese Medicine Preparation Technology, Southern Medical University, Guangzhou 510515, People’s Republic of China; 4School of Pharmacy, Zunyi Medical University, Zunyi 563000, People’s Republic of ChinaCorrespondence: Li Chen; Xiao-Mei Tan Email zmu_cl@126.com; tanxm_smu@163.comPurpose: Ferulic acid (FA) is a natural compound which is used to treat insomnia. However, its use is limited because of its poor oral bioavailability caused by extremely rapid elimination. The current study aimed to develop a self-microemulsifying drug delivery system (SMEDDS) to improve the oral delivery of FA and to enhance its hypnotic efficacy.Methods: FA-SMEDDS was prepared, and its morphology and storage stability were characterized. The formulation was also subjected to pharmacokinetic and tissue distribution studies in rats. The hypnotic efficacy of FA-SMEDDS was evaluated in p-chlorophenylalanine-induced insomnia mice.Results: FA-loaded SMEDDS exhibited a small droplet size (15.24 nm) and good stability. Oral administration of FA-SMEDDS yielded relative bioavailability of 185.96%. In the kidney, SMEDDS decreased the distribution percentage of FA from 76.1% to 59.4% and significantly reduced its metabolic conversion, indicating a reduction in renal elimination. Interestingly, FA-SMEDDS showed a higher distribution in the brain and enhanced serotonin levels in the brain, which extended the sleep time by 2-fold in insomnia mice.Conclusion: This is the first study to show that FA-loaded SMEDDS decreased renal elimination, enhanced oral bioavailability, increased brain distribution, and improved hypnotic efficacy. Thus, we have demonstrated that SMEDDS is a promising carrier which can be employed to improve the oral delivery of FA and facilitate product development for the therapy of insomnia.Keywords: insomnia, ferulic acid, oral administration, pharmacokinetics, SMEDDS
format	article
author	Liu CS Chen L Hu YN Dai JL Ma B Tang QF Tan XM
author_facet	Liu CS Chen L Hu YN Dai JL Ma B Tang QF Tan XM
author_sort	Liu CS
title	Self-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid
title_short	Self-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid
title_full	Self-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid
title_fullStr	Self-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid
title_full_unstemmed	Self-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid
title_sort	self-microemulsifying drug delivery system for improved oral delivery and hypnotic efficacy of ferulic acid
publisher	Dove Medical Press
publishDate	2020
url	https://doaj.org/article/daa50f31db874dc2b0b3814e86fe0e92
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Self-Microemulsifying Drug Delivery System for Improved Oral Delivery and Hypnotic Efficacy of Ferulic Acid

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