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多烯紫杉醇脂质体的制备及其性质考察
Preparation and characterization of docetaxel liposomes
【摘要】 目的:制备多烯紫杉醇冻干脂质体并对其性质进行考察。方法:本实验采用改善的薄膜分散法制备了多烯紫杉醇脂质体并将其冻干制成多烯紫杉醇冻干粉,通过粒径测定、ζ电位的测定、包封率的测定、稳定性的考察等研究了多烯紫杉醇冻干脂质体的性质。结果:通过在脂质材料中加入聚山梨酯80可以较好地提高药物在其中的溶解能力,提高脂质体的载药量。采用蔗糖和甘露醇混合使用作为冻干保护剂可以使脂质体冻干粉具有较好的成形性和复溶能力。测得珠干前后多烯紫杉醇脂质体的包封率分别为98.6%和95.3%,粒径分别为136和152 nm,ζ电位分别为-21.3和-20.8 mV。脂质体在葡萄糖输液中6 h内含量和粒径均无明显变化,而包封率有下降的趋势。结论:本实验所制得的多烯紫杉醇脂质体粒径分布范围窄,包封率较高,是很有应用前景的一种脂质体制剂。
【Abstract】 Objective:To prepare and characterize docetaxel liposomes.Methods:The docetaxel liposomes were prepared using a film dispersion method followed by a lyophilization technique.The ly- ophilized docetaxel liposomes were characterized with regards to the particle size,ζpotential,entrapment efficiency and the stability.Results:Tween-80 in the liposome formulation enhanced the compatibility and loading amount of docetaxel in the liposomes.A mixture of saccharose and mannitol as protective a- gents caused optimal appearance and redissolubility of the lyophilized liposomes.The docetaxel liposomes pre-and post-lyophilization featured an entrapment rate of 98.6% and 95.3%,particle size of 136 nm and 152 nm andζpotential of -21.3 mV and -20.8 mV,respectively.The concentration and particle size of the liposomes were stable and the entrapment concentration showed a decline in glucose transfusion within 6 h.Conclusion:Docetaxel liposomes with a narrow range of size distribution and high entrapment efficiency were attainable.
【Key words】 docetaxel; liposome; lyophilization; entrapment efficiency; stability;
- 【文献出处】 中国新药杂志 ,Chinese Journal of New Drugs , 编辑部邮箱 ,2007年10期
- 【分类号】R943
- 【被引频次】21
- 【下载频次】1202