Breviscapine proliposomes were prepared by ethanol injection-homogenization-lyophilization method. On contact with 5% glucose, the proliposomes were rapidly converted into a liposomal dispersion, in which a certain amount of breviscapine was entrapped by the liposomes. The entrapment efficiency measured by reverse dialysis method was 77.89 +/- 0.28%. The particle size, polydispersity index, and zeta potential of breviscapine liposomes were 504.83 +/- 52.88 nm (by intensity), 0.17 +/- 0.02, and -(20.31 +/- 1.03) mV, respectively (mean +/- SD, n = 3). In mimic-biomembrane model experiment, breviscapine was distributed not only to n-octanol and buffer phase but also to interfacial phase. After bolus administration, the elimination phase (t(1/2(beta)) = 66.386) of liposomal formulation in plasma was 4.8 times longer than that of solution formulation (t(1/2(beta)) = 13.695). The AUC and MRT values of liposomal formulation in heart were increased more than 11.7- and 3.2-fold versus solution formulation, respectively. These results were all beneficial to heart disease therapy.