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AIM To prepare Scutellariae Radix total flavonoids-loaded liposomes and to evaluate their in vitro anti-tumor activity.METHODS Liposomes were prepared by reverse evaporating method.Taking phospholipid concentration,ratio of phospholipid to cholesterol,ratio of organic phase to aqueous phase and total flavonoids concentration as influencing factors,together with encapsulation efficiency as an evaluation index,Box-Behnken design was applied to optimizing the preparation,after which MTT was employed to detect the obtained liposomes' inhibitory effect on human hepatocellular carcinoma cells HepG2.RESULTS The optimal conditions were determined to be 30 mg/mL for phospholipid concentration,3 ∶ 1 for ratio of phospholipid to cholesterol,2 ∶ 1 for ratio of organic phase to aqueous phase,and 5 mg/mL for total flavonoids concentration.The obtained round and uniform liposomes demonstrated an average particle size of (160.7 ± 12.0) nm,Zeta potential of (-41.4 ±2.3) mV,encapsulation efficiency of (86.19 ±0.44)％,drug loading of (5.32 ± 0.04)％,and accumulative release rate of (80.77 ± 2.53) ％ at 24 h.Compared with total flavonoids,liposomes exhibited stronger inhibitory effect on HepG2 cells with the IC50 of 48.853 μg/mL at 48 h in a time-and dose-dependent manner.CONCLUSION Scutellariae Radix total flavonoids-loaded liposomes stored at low temperature (4 ℃) display sustained-release effect and in vitro anti-tumor activity.
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To study the pharmacokinetic effect of different combined administration with monarch drug Ziziphi Spinosae Semen on its main components in rats. Sprague-Dawley (SD) rats were randomly divided into Ziziphi Spinosae Semen group, Ziziphi Spinosae Semen-Fructus Schisandrae Chinensis group, Ziziphi spinosae Semen-Salviae Miltiorrhize Radix et Rhizoma group and Zaoren Ansheng prescription group. After oral administration, HPLC was eluted with the mobile phase of acetonitrle-0.03% phosphate acid water in a gradient mode. The detection wavelength was 280 nm. The pharmacokinetic parameters of spinosin and ferulic acid were calculated by DAS 2. 0 software. Compared with Ziziphi Spinosae Semen group, Ziziphi Spinosae Semen-Fructus Schisandrae Chinensis group, Ziziphi Spinosae Semen-Salviae miltiorrhizae Radix et Rhizoma group showed a lower maximum plasma concentration (C(max)) and area under curve (AUC(0-t)) for spinosin and ferulic acid but higher clearance speed (CL/F); whereas the Zaoren Ansheng prescription group showed higher maximum plasma concentration (C(max)) and area under curve (AUC(0-t)) for spinosin and ferulic acid but lower clearance speed (CL/F). Compared with Ziziphi Spinosae Semen group, prescription group showed slower metabolism of spinosin and ferulic