Preparation of Fisetin Nanomicelles Based on Rubusoside and Its Anti-colitis Activity
To prepare the fisetin nanomicelles on amphiphilic rubusoside(Fis/Rub),to en-hance the pharmacokinetics and therapeutic effect of Fis.Fis/Rub nanomicelles were pre-pared by film dispersion method and to determine their physicochemical properties;The an-tioxidant activity of Fis/Rub nanomicelles was determined by ferrous reducing capacity ex-periment;The in vitro release capacity of Fis/Rub micelles was determined by dialysis meth-od and HPLC;To investigate the pharmacokinetic properties and in vivo anti-colitis activity of Fis/Rub micelles.The particle size of Fis/Rub micelles was(7.6±1.2)nm,and the po-tential was(-3.86±0.43)mV.The water solubility of Fis in Fis/Rub was(19.12±0.84)mg·mL-1.in vitro release characterization of Fis in Fis/Rub was greatly improved.The antioxidant activity of Fis was also provoked improved.The pharmacokinetic results in rats showed that Fis/Rub micelles increased the oral bioavailability of laccaxanthin by 5.5 times compared with laccaxanthin suspension.The pharmacokinetic results in rats showed that Fis/Rub micelles increased the oral bioavailability of Fis up to 5.5 times compared with Fis suspension agent.Pharmacodynamic studies have shown that oral administration of Fis/Rub micelles can effectively improve the therapeutic effect of ulcerative colitis in mice model in-duced by dextran sodium sulfate(DSS).Fis/Rub has improved the poor water solubility of Fis,which has potential further development and clinical significance.
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