Preparation, characterization, and pharmacokinetic evaluation of puerarin submicron emulsion.

A novel formulation of puerarin was studied. Puerarin submicron emulsion was prepared by complex phase inversion-high-pressure homogenization technology. Characterization, distribution of drug in emulsion, short-term stability, and pharmacokinetics of emulsion were evaluated. The mean diameter and zeta potential of puerarin emulsion were 188.14 nm and -29.45 mv, respectively. The distribution range of puerarin emulsion was very narrow. The concentration of puerarin in the interfacial surface, oil droplet, water, and liposome-micelles were 7.821, 1.079, 0.637 and 0.423 mg/mL, respectively. Puerarin submicron emulsion was stable for a period of 3 months. The area under the whole blood concentration-time curve of rabbits after intravenous administration of puerarin emulsion was 1.718-fold higher than that of rabbits of intravenous administration of puerarin (P < 0.05). And compared with the puerarin group, the elimination rate of puerarin emulsion group was significantly decreased (P < 0.05), and the biological half-life and the mean retention time of puerarin emulsion were markedly increased (P < 0.05).