Preparation Technique Optimization of Norcantharidin Liposome and Its Pharmaceutical Properties / 中国药房

ABSTRACT

OBJECTIVE:To optimize the preparation technique of norcantharidin liposome(NL) and study its pharmaceutical properties. METHODS: With envelopment efficiency(EE), mean particle size and span of the liposome as indexes, the effects of thin-film dispersion method, injection method, reverse phase evaporation and reverse phase film-evaporation method on the EE and particle size of the NL were evaluated. And the uniform design was used to optimize the reverse phase film-evaporation preparation technique of NL with the amount of phospholipid (X1), the mass ratio of phospholipid/ cholesterol (X2), the sonde-type ultrasounding times (X3), the dilution times of buffer phosphate (X4), the volume ratio of oil/water phase (X5) and the mass ratio of lipoids/ drug (X6) as integrated indexes. A verification test was performed on the optimal technique. RESULTS: The formulation prepared by reverse phase film-evaporation technique exhibited the best EE. The preparation conditions of the optimized NL were as follows X1=200 mg; X2=7∶1; X3=20 times; X4=50 times; X5=1∶4; X6=30∶1. The verification test showed that the EE, the mean particle size and the span of the liposome were (42.5?1.3)%, (210.9?2.1) nm and (0.61?0.12), respectively. CONCLUSION: NL was prepared successfully.