Pharmacokinetics and biodistribution of surface modification polymeric nanoparticles

被引：78

作者：

Liu, Mingxing ^{[1
,2
]}

Li, Huifang ^{[2
,3
]}

Luo, Guoan ^{[2
]}

Liu, Qingfei ^{[2
]}

Wang, Yiming ^{[2
]}

机构：

[1] Hubei Univ Technol, Coll Bioengn, Dept Pharm, Wuhan 430068, Peoples R China

[2] Tsinghua Univ, Dept Chem, Beijing 100084, Peoples R China

[3] Jiangxi Univ Tradit Chinese Med, Dept Pharm, Nanchang 330006, Peoples R China

来源：

ARCHIVES OF PHARMACAL RESEARCH | 2008年 / 31卷 / 04期

关键词：

breviscapine; poly(D; L-lactic acid); nanoparticles; poloxamer; 188; pharmacokinetics; biodistribution;

D O I：

10.1007/s12272-001-1191-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The objective of this study is to investigate the pharmacokinetics and biodistribution of free breviscapine (BVP) and coated BVP-loaded poly (D, L-lactic acid) nanoparticles (BVP-PLA-NPs) in rats after i.v. administration. Coated BVP-PLA-NPs were prepared by the spontaneous emulsification solvent diffusion method and characterized. The BVP content in the NPs, the biological samples and in vitro release was measured by the high-performance liquid chromatography (HPLC). The mean sizes of coated BVP-PLA-NPs were 177 and 319 nm with a narrow distribution and smooth sphere shapes, entrapment efficiency of 86.9% and 93.1%, respectively. Drug release profiles in phosphate buffer and plasma exhibited a biphasic release phenomenon. After i.v. administration of free BVP and NPs suspensions in rats, area under plasma concentration-time curve and elimination t(1/2) were increased 9.3-fold and 10.9-fold for 177 nm of NPs, and 4.4-fold and 17.1-fold for 319 nm of NPs compared with that of free BVP, respectively. NPs were mainly distributed in liver, spleen, heart and brain. In addition, NPs could penetrate blood brain barrier (131313) and the particle size had some effect on pharmacokinetics and biodistribution. Coated BVP-PLA-NPs could effectively avoid the capture by the reticuloendothelial system and prolong the half-life of BVP. Moreover, these NPs could penetrate 131313 and enhance the accumulation of BVP in brain.

引用

页码：547 / 554

页数：8