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

Author： Ambruosi Alessandra Yamamoto Hiromitsu Kreuter Jörg

Publisher： Informa Healthcare

ISSN： 1061-186X

Source： Journal of Drug Targeting, Vol.13, Iss.10, 2005-01, pp. : 535-542

Disclaimer: Any content in publications that violate the sovereignty, the constitution or regulations of the PRC is not accepted or approved by CNPIEC.

Previous Menu Next

Abstract

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 14 C-radiolabeled PBCA nanoparticles, polysorbate 80 coated 14 C-PBCA nanoparticles, and doxorubicin-loaded 14 C-PBCA nanoparticles were determined by radioactivity counting after i.v. administration in rats. The 14 C-PBCA nanoparticles showed a significant accumulation in the organs of the reticuloendothelial system (RES). Polysorbate 80 coating of the 14 C-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.