Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin

Yuzhen Hou,1 Hui Wang,1 Fan Zhang,1 Fengyuan Sun,1 Meng Xin,1,2 Mengshuang Li,1,3 Jun Li,4 Xianggen Wu1 1Department of Pharmacy, College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, China; 2Department of Ophthalmology, Yantai Affiliated Hospital of Binzhou...

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Autores principales:	Hou Y, Wang H, Zhang F, Sun F, Xin M, Li M, Li J, Wu X
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Rebaudioside A Curcumin Self-nanomicellizing Micelle Solid dispersion Drug delivery Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/a863edc0276e431abbbfb4c582f9f2b9
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spelling	oai:doaj.org-article:a863edc0276e431abbbfb4c582f9f2b92021-12-02T03:29:29ZNovel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin1178-2013https://doaj.org/article/a863edc0276e431abbbfb4c582f9f2b92019-01-01T00:00:00Zhttps://www.dovepress.com/novel-self-nanomicellizing-solid-dispersion-based-on-rebaudioside-a-a--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Yuzhen Hou,1 Hui Wang,1 Fan Zhang,1 Fengyuan Sun,1 Meng Xin,1,2 Mengshuang Li,1,3 Jun Li,4 Xianggen Wu1 1Department of Pharmacy, College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, China; 2Department of Ophthalmology, Yantai Affiliated Hospital of Binzhou Medical University, Yantai 264100, China; 3Pharmacy Intravenous Admixture Services, Qingdao Women and Children’s Hospital, Qingdao 266034, China; 4Qingdao Eye Hospital, Shandong Eye Institute, Shandong Academy of Medical Sciences, Qingdao 266071, China Purpose: Rebaudioside A (RA) has nanocarrier characteristics that allow it to self-assemble into micelles in aqueous solutions. The purpose of this study was to determine if a self-nanomicellizing solid dispersion based on RA could be utilized as an oral nano-drug delivery system.Materials and methods: Curcumin (Cur) served as a model hydrophobic drug, and a Cur-loaded self-nanomicellizing solid dispersion based on RA (RA-Cur) was formulated. The properties of RA-Cur in the solid state and in aqueous solution were characterized. The antioxidant activity and mechanism of RA-Cur endocytosis were also investigated. The pharmacokinetics, biodistribution in the intestinal tract, and anti-inflammation properties were also evaluated in vivo.Results: RA-Cur could be easily fabricated, and it self-assembled into ultrasmall micelles (particle size ~4 nm) in a homogeneous distribution state (polydispersity index <0.2) when dissolved in water. Cur was readily encapsulated into RA micelles and this improved its water solubility (to 14.34±1.66 mg/mL), as well as its in vitro release and membrane permeability. The antioxidant activities of Cur in RA-Cur were also significantly improved. Biodistribution in the intestinal tract confirmed a significant enhancement of Cur absorption in the duodenum, jejunum, and ileum by encapsulation in RA-Cur, and the absorption of RA-Cur was governed by mixed transcytosis mechanisms. Pharmacokinetic tests of RA-Cur in rats revealed a dramatic 19.06-fold enhancement of oral bioavailability when compared to free Cur. More importantly, oral administration of RA-Cur could efficiently ameliorate ulcerative colitis in a mouse model induced by dextran sodium sulfate.Conclusion: Self-nanomicellizing solid dispersions based on RA have great potential as novel oral nano-drug delivery systems for hydrophobic drugs such as Cur. Keywords: rebaudioside A, curcumin, self-nanomicellizing, micelle, solid dispersion, drug deliveryHou YWang HZhang FSun FXin MLi MLi JWu XDove Medical PressarticleRebaudioside ACurcuminSelf-nanomicellizingMicelleSolid dispersionDrug deliveryMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 557-571 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Rebaudioside A Curcumin Self-nanomicellizing Micelle Solid dispersion Drug delivery Medicine (General) R5-920
spellingShingle	Rebaudioside A Curcumin Self-nanomicellizing Micelle Solid dispersion Drug delivery Medicine (General) R5-920 Hou Y Wang H Zhang F Sun F Xin M Li M Li J Wu X Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin
description	Yuzhen Hou,1 Hui Wang,1 Fan Zhang,1 Fengyuan Sun,1 Meng Xin,1,2 Mengshuang Li,1,3 Jun Li,4 Xianggen Wu1 1Department of Pharmacy, College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, China; 2Department of Ophthalmology, Yantai Affiliated Hospital of Binzhou Medical University, Yantai 264100, China; 3Pharmacy Intravenous Admixture Services, Qingdao Women and Children’s Hospital, Qingdao 266034, China; 4Qingdao Eye Hospital, Shandong Eye Institute, Shandong Academy of Medical Sciences, Qingdao 266071, China Purpose: Rebaudioside A (RA) has nanocarrier characteristics that allow it to self-assemble into micelles in aqueous solutions. The purpose of this study was to determine if a self-nanomicellizing solid dispersion based on RA could be utilized as an oral nano-drug delivery system.Materials and methods: Curcumin (Cur) served as a model hydrophobic drug, and a Cur-loaded self-nanomicellizing solid dispersion based on RA (RA-Cur) was formulated. The properties of RA-Cur in the solid state and in aqueous solution were characterized. The antioxidant activity and mechanism of RA-Cur endocytosis were also investigated. The pharmacokinetics, biodistribution in the intestinal tract, and anti-inflammation properties were also evaluated in vivo.Results: RA-Cur could be easily fabricated, and it self-assembled into ultrasmall micelles (particle size ~4 nm) in a homogeneous distribution state (polydispersity index <0.2) when dissolved in water. Cur was readily encapsulated into RA micelles and this improved its water solubility (to 14.34±1.66 mg/mL), as well as its in vitro release and membrane permeability. The antioxidant activities of Cur in RA-Cur were also significantly improved. Biodistribution in the intestinal tract confirmed a significant enhancement of Cur absorption in the duodenum, jejunum, and ileum by encapsulation in RA-Cur, and the absorption of RA-Cur was governed by mixed transcytosis mechanisms. Pharmacokinetic tests of RA-Cur in rats revealed a dramatic 19.06-fold enhancement of oral bioavailability when compared to free Cur. More importantly, oral administration of RA-Cur could efficiently ameliorate ulcerative colitis in a mouse model induced by dextran sodium sulfate.Conclusion: Self-nanomicellizing solid dispersions based on RA have great potential as novel oral nano-drug delivery systems for hydrophobic drugs such as Cur. Keywords: rebaudioside A, curcumin, self-nanomicellizing, micelle, solid dispersion, drug delivery
format	article
author	Hou Y Wang H Zhang F Sun F Xin M Li M Li J Wu X
author_facet	Hou Y Wang H Zhang F Sun F Xin M Li M Li J Wu X
author_sort	Hou Y
title	Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin
title_short	Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin
title_full	Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin
title_fullStr	Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin
title_full_unstemmed	Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin
title_sort	novel self-nanomicellizing solid dispersion based on rebaudioside a: a potential nanoplatform for oral delivery of curcumin
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/a863edc0276e431abbbfb4c582f9f2b9
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Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin

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