Pharmacokinetics and tissue distribution of piperine lipid nanospheres.

摘要

The purpose of this study was to estimate the pharmacokinetic parameters and tissue distribution of positively charged stearylamine (LN-P-SA) and pegylated lipid nanospheres (LN-P-PEG) of piperine in BALB/c mice. Lipid nanospheres of piperine (LN-P), LN-P-PEG and LN-P-SA were prepared by homogenization followed by ultrasonication. The pharmacokinetics and tissue distribution of different lipid nanosphere formulations (piperine, LN-P, LN-P-PEG and LN-P-SA) were studied in male BALB/c mice. The pharmacokinetic parameters of LN-P-PEG and LN-P-SA were: AUC(0-24): 372.1 +/- 71.6 and 162.2 +/- 36.4 microg h(-1) ml(-1), clearance 13 +/- 2.5 and 32 +/- 7.5 ml h(-1), Cmax: 24.7 +/- 1.5 and 22.3 +/- 1.0 microg ml(-1), Vd: 0.45 +/- 0.02 and 0.66 +/- 0.06 l Kg(-1)). Pharmacokinetics of piperine in lipid nanospheres showed a biexponential decline with significantly high AUC, a lower rate of clearance and a smaller volume of distribution than piperine.