Abstract: OBJECTIVE To investigate the pharmacokinetical process of curcuminoids-loaded polyelectrolyte nanoparticles (CUR-PENPs) by i.v. administration in rats. METHODS CUR-PENPs were prepared and characterized. The rats were administrated through tail vein with curcuminoids (CUR) solution and CUR-PENPs. RESULTS CUR-PENPs were quasi-spherical shapes observed by TEM. The mean particle size， Zeta potential and drug loading were (243.0 ± 1.1)nm， (-28.13 ± 1.41)mV and 5.5%， respectively. After i.v. administration the area under concentration-time curve (AUC) of CUR-PENPs were 3.30-fold higher than those of CUR solution， the clearance (CL) of CUR-PENPs were 27.8% that of CUR solution. CONCLUSION The results indicate that CUR-PENPs may extend the retention time of CUR and improve the AUC when compared with CUR solution.