RESUMO
OBJECTIVE:To prepare silybin liposomes(SLBL)coated by N-trimethyl chitosan(TMC)(TMC60-SLBL),and to optimize the formula. METHODS:The effects of 3 kinds of preparation methods on encapsulation efficiency of SLBL were com-pared,including film dispersion method,multiple emulsion method and reverse evaporation method. The formula of TMC60-SLBL was optimized by orthogonal test using encapsulation efficiency as index with the concentration of phospholipid,ratio of phospholip-id to cholesterol,ratio of silybin to lipids,hydration temperature as factors. The stability of TMC60-SLBL by optimal formula at 4 and 25℃within 30 d,the particle size and Zeta potential of TMC60-SLBL and SLBL were all compared. RESULTS:The encapsu-lation efficiency of TMC60-SLBL prepared by the film dispersion method was the highest,without statistical significance in encap-sulation efficiency before and after cutting (P>0.05). The optimal formula was with the concentration of phospholipid 6 mg/ml;the ratio of phospholipid to cholesterol 40∶1;the ratio of silybin to lipids 1∶30;the temperature of hydration medium 45 ℃;the encapsulation efficiency were(82.08±2.6)%,RSD=3.17%(n=3). The preparation was stable at 4℃;the mean diameter of SL-BL and TMC60-SLBL were(131.9±1.9)nm and(161.2±2.0)nm,and Zeta potential respectively were(-23.18±1.14)mV and (36.73 ± 2.84) mV. CONCLUSIONS:TMC60-SLBL is prepared successfully,and its formula is simple and practicable with high encapsulation efficiency.
