Optimization of the Formulation and Preparation Technology of Podophyllotoxin Derivative Liposomes / 中国药房

ABSTRACT

OBJECTIVE:To optimize the formulation and preparation technology of podophyllotoxin derivative(5-FPE) liposomes.METHODS:A thin film-ultrasonic dispersion method was used to prepare the 5-FPE liposomes.Orthogonal experiment was performed to optimize its best formulation and preparation technology with entrapment efficiency as the evaluation index;meanwhile,the entrapment efficiency,drug-loading amount,morphology,particle size distribution,Zeta electric potential and stabilities of the liposomes within 10 days' storing at 25 ℃ or 4 ℃ were investigated.RESULTS:The optimal formulation and prepariton technology of the liposomes has been established in our study.3 batches of liposomes prepared in the optimal conditions had a mean entrapment efficiency of 66.45%,a mean drug-loading amount of 7.97%,mean particle size of 284.7 nm and mean Zeta electric potential of-22.15 mV.The entrapment efficiency of the liposomes decreased more after storing for 10 days at 25 ℃ than at 4 ℃.CONCLUSION:The optimal formulation and preparation technology of 5-FPE liposomes are feasible and which serve as a basis for the further study of 5-FPE preparations.