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

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

Keywords: :

• Blood-brain barrier
• nanoparticles
• doxorubicin
• polysorbate 80

Abbreviations
BBB	=	blood-brain barrier
CNS	=	central nervous system
RES	=	reticuloendothelial system
NP	=	Nanoparticles
PBCA	=	poly(butyl cyanoacrylate)
DOX	=	doxorubicin
PS	=	polysorbate 80
Pgp	=	P-glycoprotein efflux system

Abbreviations
BBB	=	blood-brain barrier
CNS	=	central nervous system
RES	=	reticuloendothelial system
NP	=	Nanoparticles
PBCA	=	poly(butyl cyanoacrylate)
DOX	=	doxorubicin
PS	=	polysorbate 80
Pgp	=	P-glycoprotein efflux system