脂质体由于其特殊的结构和性能,是一种很有发展潜力的药物载体,在医药和化妆品等行业具有广阔的应用前景。超临界逆向蒸发法是用超临界流体代替有机溶剂制备脂质体的方法,具有对水溶性药物脂质体制备过程简单、包覆率高等特点。以葡萄糖为模型药物,利用该方法制备出了葡萄糖脂质体,并详细考察了不同工艺条件对脂质体粒径和包覆率的影响。结果表明:用超临界逆向蒸发法可成功地制备出最小粒径为290nm、包覆率最高可达41.3%的葡萄糖脂质体。压力、温度和平衡时间对粒径和包覆率都有较大的影响。压力在10~30MPa时,随压力的增加,脂质体粒径显著减小至某一值后,基本趋于稳定,而包覆率逐渐增加,达到25.7%~27.5%,随后包覆率逐渐减小;温度在35~65℃时,随温度的增加粒径显著减小至最小值,然后逐渐增大,而包覆率一直增大,最高可达41.3%;平衡时间在15~45min时,随平衡时间的增加,粒径相对稳定,而包覆率显著增加,超过45min之后,粒径显著增加,包覆率显著下降。
Liposomes have proven to be promising carriers for their special structure and characteriza tion, and can be widely used in pharmacy and cosmetics. Supercritical reverse phase evaporation (SRPE) is a new technique for preparing liposomes with supercritical fluid instead of organic solvent. The process has characteristic of simple and high coating ratio for water-soluble substances. The tech- nique was used to prepare liposomes with water soluble glucose,and the effects of the process parame- ters on the particle size and the coating ratio of liposomes were investigated in detail. The liposomes with an average volume diameter of 290-330 nm were successfully prepared by this technique and the coating ratio for water-soluble glucose was as high as 41.3%. It is confirmed that the temperature, pressure and equilibrium time have great effects on the particle size and the coating ratio. As the pres- sure increased from 10 to 30 MPa,the particle size first decreased remarkably and then kept approxi- mately constant,while the coating ratio gradually increased to 25.7%- 27.5% and then gradually de- creased;as the temperature increased from 35 to 65 ℃, the particle size decreased obviously to its min- imum value and then gradually increased, while the coating ratio increased all along, even to 41.3%. With the equilibrium time increasing from 15 to 45 min,the particle size kept relatively stable,while the coating ratio increased remarkably;when the equilibrium time exceeded 45 min,the particle size in creased remarkably, while the coating ratio decreased remarkably.