Influence on the distribution of rehydrated particle sizes of freeze-dried docetaxel liposome / 中国药学杂志

ABSTRACT

OBJECTIVE: To investigate factors that affected the distribution of rehydrated particle size of freeze-dried docetaxel liposome and develop a technique of producing docetaxel liposome that can meet clinical requirements. METHODS: The single factor method was utilized in this study. Docetaxel liposome were prepared using different types of negatively charged phospholipids, or lecithins with varying phosphatidylcholine (PC) content, or various cryoprotectants at different gradient concentrations, followed by freeze-drying with different protocols. The particle sizes of corresponding rehydrated products were compared and the effects of different factors were analyzed. RESULTS: The optimal liposomal membrane was composed of dipalmitoyl phosphatidic acid (DPPA), 20% trehalose and lecithin containing 92% PC. The best freeze-drying protocol included following steps; flash freezing, 19 h of sublimation-drying and 9 h of desorption-drying. CONCLUSION: The parameters, including negatively charged phospholipids, cryoprotectants, PC content of lecithin and lyophilization protocols, had various effects on the particle sizes of reconstituted docetaxel liposome.