Apigenin Solid Lipid Nanoparticles

Apigenin is one kind of the flavonoids,which exists widely in many sorts of fruits and vegetables.The research shows that Apigenin possess some pharmacological effects,such as anticancer,anti-inflammatory,antivirus,and antioxidation,and it is a.perspective traditional Chinese medicine active component.Apigenin is insoluble in water,and its gastrointestinal absorption and bioavailability is low.To efficiently elevate its bioavailability,improve its effect of gastrointestinal absorption,this thesis adopted solid lipid nanoparticles(SLN)the drug delivery system as carrier,prepared apigenin nanoparticle suspension to achieve above-mentioned objectives.The method of high performance liquid chromatography(HPLC)was developed to inspect the physicochemical characteristics of apigenin and the assaying of SLN in pre-formulation study.The elementary physicochemical characteristics of the model drug were preliminary investigated.On the base of pre-formulation study,hot-melt ultrasonic method was chosen to prepare apigenin solid lipid nanoparticles(AP-SLN).Set particle diameter,entrapment efficiency and stability as indexes,optimized the formulation by the single factor exploration and orthogonal design.Studied the pharmacy character of the prepared AP-SLN.The appearance of AP-SLN were examined by transmission electron microscopy as sphere-like with the mean size of 135 nm,the potential of-18.90 mV,respectively.The in vitro release profiles could be expressed by first-order release equation.To aim directly at the stability of SLN,used cryodesiccate method to freeze SLN,evaluated the physicochemical characteristics of those freeze dried products products.An HPLC method was developed for the determination of apigenin in the plasma of rats.Made self-made apigenin suspension as control group,inspected pharmacokinetics processes of taking AP-SLN of the rats by oral.The results of oral administration pharmacokinetics indicated that SLN significantly enhanced the oral bioavailability.The average AUC_0-tof SLN group was 17.337μg h/mL,while5.3μg h/mL of control group.Cmax of SLN group was 3.07μg/mL,obviously higher than 1.544μg/mL of control group.The elimination rate constant,Ke,of SLN group was 0.232/h, lower than the control group.The relative bioavailability of the AP-SLN was 327%.