Study On Preparation Of Genistein Chitosan Nanoparticles, Their Absorption And Antioxidation In Vivo

Genistein is a weak plant estrogen, belongs to isoflavone compounds, whichmainly exists in the legume. Genistein has many physiological activities, such asanti-cancer, osteoporosis prevention, cardiovascular system protection,antioxidation, detoxification hepatoprotective and so on. However its biologicalactivity in vivo has been greatly affected because of its insoluble in water and lowbioavailability.In this paper, genistein chitosan nanoparticles were prepared by ioniccross-linking method. The encapsulating efficiency of genistein nanoparticles wasmeasured by centrifugal-UV spectrophotometer. Taken encapsulation efficiency asmain index, the preparation process of the genistein chitosan nanoparticles wereoptimized by orthogonal design. The optimal preparation crafts: the concentrationof chitosan was2.5mg/ml, the concentration of TPP was1.5mg/ml, the ratio ofacetic acid to ethanol2:1, the amount of genistein was2.5mg. Obtained genisteinnanoparticles is round or oval-shaped microspheres, evenly distributed, the averageparticle size was below40nm. Fourier transform infrared spectroscopy (FTIR) andX-ray diffraction (XRD) was used to characterize the structure of genisteinnanoparticles. The experiments of release in vitro showed that genisteinnanospheres had good release effect, genistein can be slowly released in pH6.8artificial intestinal fluid.The mice were fed with genistein chitosan nanoparticles, genistein, the contentof lycopene in liver and serum were determined by HPLC. The results showed thatthe content of lycopene in liver and serum in genistein nanoparticles group washigher than genistein group, the content of genistein in liver was significantlyincreased (p<0.01), but in serum was no significantly change (p>0.05). Theexperiments of absorption preliminary proved that genistein nanoparticles couldincrease the absorption of genistein in vivo, improve its bioavailability and livertargeting.The activities of superoxide dismutase (SOD), catalase (CAT), glutathionereductase (GSH), and the content of malondialdehyde (MDA) were determined inliver. The results showed that the activities of SOD, CAT in genistein chitosannanoparticles group were significantly higher than both in control group andgenistein group (p<0.01), the activity of GSH increased highly (p<0.05) and the concent of MDA decreased highly (p<0.01). The experiments of antioxidationfurther proved genistein nanoparticles had liver targeting, Chitosan nanoparticles asconveyor system could improve the bioavailability and biological effects ofgenistein.