Body distribution of polysorbate-80 and doxorubicin-loaded [14C]poly(butyl cyanoacrylate) nanoparticles after i.v. administration in rats

被引:72
作者
Ambruosi, A
Yamamoto, H
Kreuter, J
机构
[1] Univ Frankfurt, Inst Pharmazeut Technol, D-60439 Frankfurt, Germany
[2] Gifu Pharmaceut Univ, Lab Pharmaceut Engn, Gifu 5028585, Japan
关键词
blood-brain barrier; nanoparticles; doxorubicin; polysorbate; 80;
D O I
10.1080/10611860500411043
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Previously it was shown that poly(butyl cyanoacrylate) (PBCA) nanoparticles coated with polysorbate 80 are able to cross the blood-brain barrier (BBB) after i.v. administration. The objective of the present study was to investigate the influence of polysorbate 80 and doxorubicin-loading on the body distribution in rats. The biodistribution profile and brain concentration of C-14-radiolabeled PBCA nanoparticles, polysorbate 80 coated C-14-PBCA nanoparticles, and doxorubicin-loaded C-14-PBCA nanoparticles were determined by radioactivity counting after i.v. administration in rats. The C-14-PBCA nanoparticles showed a significant accumulation in the organs of the reticuloendothelial system (RES). Polysorbate 80 coating of the C-14-PBCA nanoparticles decreased this accumulation to about 40% after 1 h post injection. The brain concentration was increased about 2-fold after polysorbate 80-coating at this time point. The presence of doxorubicin in this preparation, however, decreased the brain concentration to levels similar to uncoated particles, probably caused by the positive charge of this compound. After longer time periods after injection the differences between the three preparations decreased.
引用
收藏
页码:535 / 542
页数:8
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