Formulation Optimization of Transferrin Modified Tetrandrine and Vincristine Liposomes by Central Com-posite Design-response Surface Method / 中国药房

ABSTRACT

OBJECTIVE:To prepare transferrin(TF)modified tetrandrine(TET)and vincristine(VCR)active targeting lipo-somes,and to optimize its formulation. METHODS:TF modified TET and VCR liposomes were prepared by ammonium sulfate gradient method. Using comprehensive score of encapsulation efficiency of TET and VCR as index,central composite design-re-sponse surface method was used to optimize and validate mole ratio of EPC/Chol,mole ratio of EPC/PEG2000-DSPE and TF mass fraction. RESULTS:The optimal formulation was that the mole ratios of EPC/Chol and EPC/PEG2000-DSPE were 1.51 and 201, TF mass fraction was 0.10%. The encapsulation efficiency of TET and VCR were 97.80% and 93.00%,respectively. The compre-hensive score was 94.44(n=3)which was close to the predicted value of 93.81. CONCLUSIONS:The optimal formulation is sta-ble and can be used for the preparation of TF modified TET and VCR liposomes.