Distribution of liposomal bifendate in liver following intravenous injection in mice.

摘要

The purpose of this study was to develop and study the behaviors of bifendate (DDB) liposome in vivo. DDB liposome was prepared by the rotary evaporationextrusion method. The particle size, zeta-potential, encapsulation efficiency (EE), and in vitro drug release from liposome were determined and the in vivo studies were tested in mice and rats. The concentrations of DDB in plasma and liver at different sampling time points were determined by RP-HPLC. The liver concentration-time curves of DDB liposome and free drug solution in mice were determined, and the pharmacokinetic parameters in rats and mice were calculated and compared by statistical analysis. The average liposome diameter was 323 +/- 29 nm (n = 3) and the EE was 91.52 +/- 2.38%. There were significantly different parameters of k10 and area under the plasma concentrationtime curve (AUC(0-T)) between liposome and solution. The mean residence time (MRT(0-T)) in plasma of liposomal formulation was 3.72 times longer than that of solution. Compared with solution, DDB liposome delivered about 2.57 times higher DDB into liver. Thus, an optimum intravenous liposome formulation for DDB could be developed as an alternative to the commercial DDB preparations.