Preparation, characterization and pharmacokinetics of dihydromyricetin phospholipids complex loaded by nanostructured lipid carriers / 中草药

ABSTRACT

Objective: To prepare dihydromyricetin (DMY) phospholipids complex (DMY-PC) and its nanostructured lipid carriers (DMY-PC-NLC), and carry out in vitro and in vivo evaluation. Methods: DMY-PC was prepared by solvent evaporation method. High pressure homogenization method was used to prepare DMY-PC-NLC. Orthogonal test was employed to optimize the ratio of solid/liquid lipid, dose of lipids materials, dose of DMY-PC and the concentration of emulsifier of poloxamer. The lyophilized powder of DMY-PC-NLC was prepared with 5% of mannitol as protective agent. The comparation of in vitro release and pharmacokinetics between DMY-PC and DMY-PC-NLC was also studied. Results: DMY was in an amorphous state in DMY-PC. The results of 1HNMR showed that the structure of DMY was not changed. The optimized prescription of DMY-PC-NLC determined by orthogonal test was as follow The ratio of solid/liquid lipid was 51, dose of lipids materials was 325 mg, dose of DMY-PC was 45 mg and the concentration of emulsifier of poloxamer was 0.9%. The average size, Zeta potential, entrapment efficiency and drug loading of DMY- PC-NLC was (197.25 ± 4.42) nm, (-18.2 ± 2.1) mV, (71.68 ± 1.36)% and (3.94 ± 0.24)%, respectively. The in vitro release model was accord with Weibull model and the equation was lnln(1-Mt/M∞)=0.700 1 lnt-1.954 1 (r = 0.971 4). The relative bioavailability of DMY-PC and DMY-PC-NLC were enhanced to 1.63 and 3.22 times compared to DMY, respectively. Conclusion: Compared with DMY-PC, the absorption was promoted by DMY-PC-NLC in further, and the bioavailability of DMY was enhanced effectively.