Supersaturated polymeric micelles for oral silybin delivery: the role of the Soluplus-PVPVA complex

doi:10.1016/j.apsb.2018.09.004

	Supersaturated polymeric micelles for oral silybin delivery: the role of the Soluplus-PVPVA complex
	Zhu, Chunliu 1,3; Gong, Shuang 2,3; Ding, Jinsong 2; Yu, Miaorong 3; Ahmad, Ejaj 3; Feng, Yi 1; Gan, Yong 3
刊名	ACTA PHARMACEUTICA SINICA B
	2019
卷号	9 期号:1 页码:107-117
关键词	Silybin Soluplus PVPVA Complex Supersaturated drug delivery system Oral bioavailability
ISSN号	2211-3835
DOI	10.1016/j.apsb.2018.09.004
通讯作者	Feng, Yi(fengyi@vip.sina.com) ; Gan, Yong(ygan@mail.shcnc.ac.cn)
英文摘要	Increasing the degree of supersaturation of drugs and maintaining their proper stability are very important in improving the oral bioavailability of poorly soluble drugs by a supersaturated drug delivery system (SDDS). In this study, we reported a complex system of Soluplus-Copovidone (Soluplus-PVPVA) loaded with the model drug silybin (SLB) that could not only maintain the stability of a supersaturated solution but also effectively promote oral absorption. The antiprecipitation effect of the polymers on SLB was observed using the solvent-shift method. In addition, the effects of the polymers on absorption were detected by cellular uptake and transport experiments. The mechanisms by which the Soluplus-PVPVA complex promotes oral absorption were explored by dynamic light scattering, transmission electron microscopy, fluorescence spectra and isothermal titration calorimetry analyses. Furthermore, a pharmacokinetic study in rats was used to demonstrate the advantages of the Soluplus-PVPVA complex. The results showed that Soluplus and PVPVA spontaneously formed complexes in aqueous solution via the adsorption of PVPVA on the hydrophilichydrophobic interface of the Soluplus micelle, and the Soluplus-PVPVA complex significantly increased the absorption of SLB. In conclusion, the Soluplus-PVPVA complex is a potential SDDS for improving the bioavailability of hydrophobic drugs. (C) 2019 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
资助项目	National Natural Science Foundation of China[81573378] ; National Natural Science Foundation of China[81773651] ; Shanghai Science and Technology Innovation Action Plan for Basic Research, China[17430741500]
WOS关键词	SOLUBILITY-PERMEABILITY INTERPLAY ; WATER-SOLUBLE DRUGS ; MEMBRANE-TRANSPORT ; FORMULATION DESIGN ; IN-VITRO ; SYSTEM ; BIOAVAILABILITY ; ABSORPTION ; IMPACT ; DISSOLUTION
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
WOS记录号	WOS:000457201700010
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/290611]
专题	中国科学院上海药物研究所
通讯作者	Feng, Yi; Gan, Yong
作者单位	1.Shanghai Univ Tradit Chinese Med, Engn Res Ctr Modern Preparat Technol Tradit Chine, Shanghai 201203, Peoples R China 2.Cent S Univ, Xiangya Sch Pharmaceut Sci, Changsha 410000, Hunan, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Zhu, Chunliu,Gong, Shuang,Ding, Jinsong,et al. Supersaturated polymeric micelles for oral silybin delivery: the role of the Soluplus-PVPVA complex[J]. ACTA PHARMACEUTICA SINICA B,2019,9(1):107-117.
APA	Zhu, Chunliu.,Gong, Shuang.,Ding, Jinsong.,Yu, Miaorong.,Ahmad, Ejaj.,...&Gan, Yong.(2019).Supersaturated polymeric micelles for oral silybin delivery: the role of the Soluplus-PVPVA complex.ACTA PHARMACEUTICA SINICA B,9(1),107-117.
MLA	Zhu, Chunliu,et al."Supersaturated polymeric micelles for oral silybin delivery: the role of the Soluplus-PVPVA complex".ACTA PHARMACEUTICA SINICA B 9.1(2019):107-117.