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Taxifolin flavanone alcohol compounds, is the main active ingredient of Chinese medicine orientale, soil Fuling, widespread in the citrus, grapes and other fruits. Pharmacology studies have shown that taxifolin has significant anti-oxidation, anti-tumor effects. However, because of the small water-soluble, low bioavailability, irregular oral absorption, it largely limits its clinical application. This experiment will Taxifolin made of solid lipid nanoparticles and liposomes, and both a preliminary study in mice pharmacokinetic characteristics, and to lay the foundation for the further development of Taxifolin. Preparation of solid lipid nanoparticles Taxifolin and liposomes Taxifolin, using solvent injection method, optimization of solid lipid nanoparticles Taxifolin prescription by Star Dot Design - response surface methodology (RSM-CCD) through a single factors experimental screening Taxifolin liposomes prescription dosage. Three batches were prepared according to the optimized formulation and preparation of the the taxifolin solid lipid nanoparticles and liposomes results show solid lipid nanoparticles mean encapsulation efficiency of 80.9 ± 3.5%, drug loading of 13.9 ± 2.0%, dynamic laser scattering instrument, nanoparticles average particle size of 125.0 ± 1.5nm, zeta potential -24.3 ± 6.1mV, transmission electron microscopy shows that nanoparticles cylindrical the whole uniform spherical particles; the liposomes Taxifolin encapsulation efficiency 68.1 ± 4.5%, and an average particle size of 166.4 ± 2.9 nm, the zeta potential -32.3 ± 4.9mV, transmission and scanning electron microscopy showed that the particles are rounded uniform. Establishment of mouse plasma Taxifolin HPLC analysis method. Taxifolin solution agent for the control, the study mice were intravenously injected the taxifolin solid lipid nanoparticles suspension, the pharmacokinetics of liposome suspension Taxifolin process and calculate the pharmacokinetic parameters. Preparations Taxifolin the mice plasma pharmacokinetics meets three-compartment model. The plasma pharmacokinetic parameters (each blood collection point n = 3): the solution dose group: AUC (0 - ∞) 15.745mg / L * h, t1/2β0.021h Cmax of 31.02mg / L, the Tmax 0.083h , CL3.176L/h/kg; liposome groups: AUC (0 - ∞) 20.962mg / L * h, t1/2p 0.279h, Cmax 15.30mg / l, Tmax 0.083h, CL 2.385L/h/kg ; solid lipid nanoparticles group: AUC (0 - ∞) 17.61mg / L * h t1/2β0.116h Cmax of 18.60mg / l, Tmax 0.083h, CL 2.839L/h/kg. Experimental results show that Taxifolin liposomes and nanoparticles in mice AUC compared with the solution agent group larger eliminate speed reduction visible Taxifolin liposomes and nanoparticles can effectively extend the Douglas fir factors in vivo retention time, slow down the metabolism and excretion of drugs. The Taxifolin solution agent group, liposome, nanoparticle group Cmax were: 31.02mg / L, 15.30 mg / L, 18.60 mg / l, visible, solution to be fast in vivo distribution of the other two formulations .
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