Preparation, characterization, and biodistribution of breviscapine proliposomes in heart

Abstract

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(β) = 66.386) of liposomal formulation in plasma was 4.8 times longer than that of solution formulation (t_1/2(β) = 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.

Keywords:

• Breviscapine
• proliposomes
• reverse dialysis
• mimic-biomembrane
• biodistribution in heart

Acknowledgments

This work was partly supported by “211 project” and “985 project” university grant from Southeast University awarded to Dr. Xiong Fei (Nos. 4007031040 and 9207032444), National Basic Research Program of China (Nos. 2006CB933206 and 2006CB705602), and National Natural Science Foundation of China (Nos. 60725101 and 30772663).

Declaration of interest: The authors report no conflicts of interest.