Preparation And Pharmacokinetic Studies Of Baicalein Solid Lipid Nanoparticles

ObjectiveBaicalein(Baicalein,Ba)is flavonoids,antibacterial and anti-inflammatory,antimicrobial,antiviral and multiple pharmacological effects,has a wide prospect of clinical application.In view of the shortcomings of poor water solubility and low bioavailability of baicalein,based on solid lipid nanoparticles as carrier,the morphology of solid lipid nanoparticles was constructed,in vivo studies have investigated Baicalein solid lipid nanoparticles how to improve the oral absorption,and other related properties.MethodsThe Baicalein solid lipid nanoparticles were prepared by emulsion evaporation solidified at low temperature method.In the encapsulation was investigated by single factor and orthogonal test to determine the best technology and prescription.Though the electron microscope and laser particle size instrument measure its morphology and particle size distribution,drug release properties were investigated by using dialysis method in vitro.The freeze-drying agent was added to the optimal formulation,though the DSC?PXRD and FT-IR were examined to the crystal type of the drug in the nanoparticles.In vivo pharmacokinetics of baicalein solid lipid nanoparticles were investigated by SD rats as the research properties.ResultsThe optimal formulation was determined : Baicalein 10 mg,Glycerol monostearate 100 mg,Lecithin 200 mg,F68 150 mg,Tween 80 100 mg.The solid lipid nanoparticles were prepared by emulsion evaporation solidification at low temperature,the appearance of a light yellow opalescent.The physical form of the nanoparticles under electron microscopy was spherical and dispersed uniformly,the measured particle size of average particle size was 87.63±1.83 nm,PDI was 0.254 ±0.010,Zeta potential was-33.0±1.7 m V,the encapsulation efficiency was 81.3±1.2 %.The encapsulation efficiency was no significant change at 4 ? in 15 days.In vitro release,compared with the raw material drug,it was obvious sustained release effect.Add 5 % to suspension of mannitol cryoprotectants,the appearance of cyophilized powder was yellow,no color,compact and full appearance.By DSC,PXRD,FT-IR of the lyophilized powder was analyzed and found that the nanoparticles Ba to amorphous state dispersed nanoparticles.In 4 ? environment for 30 days,the encapsulation rate has no obvious change.In the experiment of drug action,the oral bioavailability of the solid lipid nanoparticles in SD rats increased nearly 2 times.ConclusionsThe baicalein prepared by emulsion evaporation solidification at low temperature in solid lipid nanoparticles,the encapsulation efficiency,particle size,PDI and Zeta potential were all consistent with the stability requirements.In vitro experiments showed that the drug has a sustained release effect.After drug preparation into freeze-dried powder,through DSC?PXRD proved the drug to amorphous state dispersion in the nanoparticles.Animal experiments showed that the oral bioavailability of the solid lipid nanoparticles in SD rats was improved.