supersaturatedpolymericmicellesfororalsilybindeliverytheroleofthesolupluspvpvacomplex

doi:10.1016/j.apsb.2018.09.004

	supersaturatedpolymericmicellesfororalsilybindeliverytheroleofthesolupluspvpvacomplex
	Zhu Chunliu 2; Gong Shuang 1; Ding Jinsong 1; Yu Miaorong 3; Ahmad Ejaj 3; Feng Yi 2; Gan Yong 3
刊名	actapharmaceuticasinicab
	2019
卷号	9 期号:1 页码:107
关键词	SOLUBILITY-PERMEABILITY INTERPLAY WATER-SOLUBLE DRUGS MEMBRANE-TRANSPORT FORMULATION DESIGN IN-VITRO SYSTEM BIOAVAILABILITY ABSORPTION IMPACT DISSOLUTION Silybin Soluplus PVPVA Complex Supersaturated drug delivery system Oral bioavailability
ISSN号	2211-3835
DOI	10.1016/j.apsb.2018.09.004
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] ; [Shanghai Science and Technology Innovation Action Plan for Basic Research, China]
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/286546]
专题	中国科学院上海药物研究所
作者单位	1.中南大学 2.上海中医药大学 3.中国科学院上海药物研究所
推荐引用方式 GB/T 7714	Zhu Chunliu,Gong Shuang,Ding Jinsong,et al. supersaturatedpolymericmicellesfororalsilybindeliverytheroleofthesolupluspvpvacomplex[J]. actapharmaceuticasinicab,2019,9(1):107.
APA	Zhu Chunliu.,Gong Shuang.,Ding Jinsong.,Yu Miaorong.,Ahmad Ejaj.,...&Gan Yong.(2019).supersaturatedpolymericmicellesfororalsilybindeliverytheroleofthesolupluspvpvacomplex.actapharmaceuticasinicab,9(1),107.
MLA	Zhu Chunliu,et al."supersaturatedpolymericmicellesfororalsilybindeliverytheroleofthesolupluspvpvacomplex".actapharmaceuticasinicab 9.1(2019):107.