Preparation of Scutellariae Radix total flavonoids-loaded liposomes and their in vitro anti-tumor activity / 中成药

ABSTRACT

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.