Increased brain uptake of venlafaxine loaded solid lipid nanoparticles by overcoming the efflux function and expression of P-gp

doi:10.1007/s12272-014-0539-6

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	Increased brain uptake of venlafaxine loaded solid lipid nanoparticles by overcoming the efflux function and expression of P-gp
	Zhou, Y; Zhang, GQ; Rao, Z; Yang, Y; Zhou, Q; Qin, HY; Wei, YH; Wu, XA; Wu, XA (reprint author), Lanzhou Univ, Dept Pharm, Hosp 1, Lanzhou 730000, Peoples R China.
刊名	ARCHIVES OF PHARMACAL RESEARCH
	2015-07
卷号	38 期号:7 页码:1325-1335
关键词	P-glycoprotein Blood-brain barrier Solid lipid nanoparticles Venlafaxine
ISSN号	0253-6269
DOI	10.1007/s12272-014-0539-6
文献子类	Article
英文摘要	Venlafaxine (VLX) could be pumped out of the brain by P-glycoprotein (P-gp). Moreover, the expression of P-gp distributed in blood-brain barrier could be significantly induced by VLX. Thus, P-gp could be considered as the nature barrier for delivering of VLX to the brain. The aim of this study was to investigate whether the efflux function and increased expression of P-gp could be reversed by utilizing solid lipid nanoparticles (SLN). VLX solid lipid nanoparticles (VLX - SLN) were prepared and evaluated. Pharmacokinetics and brain distribution of VLX in different formulations were conducted after oral or intravenous administration. P-gp efflux function to VLX was evaluated by the brain uptake amount of VLX, while P-gp expression was investigated by Western blotting. Results indicated that the entrapment, mean size and zata potential of VLX - SLN was 74.9 +/- A 3.0 %, 186.3 +/- A 69.26 nm and -22.8 +/- A 7.78 mv, respectively. After vein injection of VLX formulations, the brain uptake amount of VLX from VLX - SLN was significantly higher than that of VLX solution, VLX solution with empty SLN (VLX+ empty SLN) and VLX solution with Verapamil (VLX + Ver), respectively. Furthermore, the protein mass of P-gp in VLX - SLN treated group was the lowest among all the investigated groups. These results indicated that SLN could overcome P-gp and achieve brain target by intravenous administration.
学科主题	Pharmacology & Pharmacy
出版地	SEOUL
语种	英语
WOS记录号	WOS:000358046200006
内容类型	期刊论文
源URL	[http://ir.lzu.edu.cn/handle/262010/178583]
专题	第一临床医学院_期刊论文
通讯作者	Wu, XA (reprint author), Lanzhou Univ, Dept Pharm, Hosp 1, Lanzhou 730000, Peoples R China.
推荐引用方式 GB/T 7714	Zhou, Y,Zhang, GQ,Rao, Z,et al. Increased brain uptake of venlafaxine loaded solid lipid nanoparticles by overcoming the efflux function and expression of P-gp[J]. ARCHIVES OF PHARMACAL RESEARCH,2015,38(7):1325-1335.
APA	Zhou, Y.,Zhang, GQ.,Rao, Z.,Yang, Y.,Zhou, Q.,...&Wu, XA .(2015).Increased brain uptake of venlafaxine loaded solid lipid nanoparticles by overcoming the efflux function and expression of P-gp.ARCHIVES OF PHARMACAL RESEARCH,38(7),1325-1335.
MLA	Zhou, Y,et al."Increased brain uptake of venlafaxine loaded solid lipid nanoparticles by overcoming the efflux function and expression of P-gp".ARCHIVES OF PHARMACAL RESEARCH 38.7(2015):1325-1335.