[Preparation of Baicalein Liposome-Lyophilized Powder and Its Pharmacokinetics Study]

To prepare baicalein liposome-lyophilized powder, and to investigate the particle size distribution, encapsulation efficiency, stability, in vitro release and in vivo pharmacokirietics in rats. METHODs: Baicalein liposome was prepared by the ethanol injection, the encapsulation efficiency was measured by column chromatography, glucose, lactose and mannitol were selected as lyoprotectants. Pharmacokinetics study in rats was carried out by oral administration and analysis of rats pharmacokinetic parameters.

The baicalein liposomes were spherical, the mean diameter was (93.1 ± 11.2) nm, PDI was 0.258, the encapsulation efficiency was (83.9 ± 0.4)%. In vitro release test results showed that it had a significant slow-release effect, freeze-dried mannitol for the best protective agent. The pharmacokinetic parameters of baicalein liposomes and solution were as follows: AUC(0 --> 24 (129.04 ± 12.73) μg/mL x h and (73.31 ± 9.34) μg/mL x h; C(max) (15.07 ± 3.13) μg/mL and (9.38 ± 2.42) μg/mL; T(max) 1 and 1.5 h.

Baicalein liposome has the higher entrapment efficiency and the smaller particle size. In vitro studies show that baicalein liposome has a slow-release effect and can significantly improve the bioavailability in rats.