Abstract: OBJECTIVE To prepare borneol modified puerarin liposomes(BO-Pue-Lips) with optimization, and evaluate the concentration in brain of the drug liposomes in rats. METHODS The BO-Pue-Lips were prepared with the thin-film rehydration method and were optimized through orthogonal test according to entrapment efficiency and drug loading of BO-Pue-Lips. Using puerarin(Pue) suspension and borneol puerarin(BO-Pue) suspension as control, the concentration in brain of BO-Pue-Lips after intravenous administration in rats were studied. RESULTS The optimal conditions for preparation of BO-Pue-Lips were Pue-soybean phospholipids(1︰10), cholesterol-soybean phospholipids(1︰4), and the hydration temperature was 40 ℃. The mean particle size of the resulted BO-Pue-Lips was (112.97±0.89)nm and Zeta potential was (-7.48±0.49)mV, the average entrapment efficiency and drug-loading was (73.47±1.75)% and (5.55±0.13)%, respectively. The profiles of release in vitro was expressed well by Weibull equation. Results of distribution in brain showed that T_1/2of Pue, BO-Pue and BO-Pue-Lips were (0.61±0.22)h, (0.55±0.27)h and (1.80±0.17)h, AUC_0→twere (68.59±1.09)μg·h·g^-1, (72.70±2.63)μg·h·g^-1and (137.68±10.17)μg·h·g^-1, CL were (0.29±0.01)L·h^-1·kg^-1, (0.27±0.02)L·h^-1·kg^-1and (0.13±0.01)L·h^-1·kg^-1, MRT were (0.93±0.05)h, (0.97±0.02)h and (1.80±0.05)h. CONCLUSION An optimized liposomes drug delivery system is obtained by thin-film rehydration method. The preparation and preparation process are selected and optimized. The liposomes after intravenous administration might increase the concentration, prolong circulation time and have a good targeting efficiency in brain.