鬼臼毒素衍生物脂质体处方和制备工艺优选

目的:优选鬼臼毒素衍生物5-氟尿嘧啶乙酸鬼臼酯(5-FPE)脂质体处方和制备工艺。方法:采用薄膜超声分散法制备5-FPE脂质体,以包封率为指标通过正交试验法优选制备处方和工艺,并考察制备的脂质体的包封率、载药量、形态、粒径分布、Zeta电位及在25、4℃条件下存放10d后的体外稳定性。结果:确定了最优处方和工艺,以此制备的3批脂质体的平均包封率为66.45%,平均载药量为7.97%,粒径均值为284.7nm,平均Zeta电位为—22.15mV;脂质体存放10d后包封率下降,但在4℃条件下存放的脂质体的包封率变化比25℃的更小。结论:以优选处方和工艺制备5-FPE脂质体具有可行性,可为进一步的制剂研究提供基础。

Optimization of the Formulation and Preparation Technology of Podophyllotoxin Derivative Liposomes

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.