脂质体冻干保护剂的种类及其作用机制研究进展

Progress on liposomal lyoprotectants and the mechanism of action

目的对脂质体冻干保护剂作用机制及保护剂的种类进行综述,为脂质体冻干保护剂的选择提供参考。方法参阅近年来国内外文献46篇,综述脂质体冻干保护剂的作用机制,并对不同保护剂的作用效果及其可能的保护原理进行归纳、总结和分析。结果脂质体冻干保护剂通过以下3个方面发挥保护作用:a.以氢键形式与磷脂膜结合,在干燥状态下替代脂膜表面的水分子,维持脂质体膜稳定;b.冻干保护剂的渗透和体积效应,抑制干燥脂膜相变温度升高;c.在脂质体周围形成玻璃态的间隔基质,抑制膜融合及膜相变温度升高。以糖类为代表的脂质体冻干保护剂因糖的类型及磷脂种类的差异呈现出不同的保护效果。结论为脂质体冻干保护剂的选择及脂质体冻干产品的开发提供了参考。

Objective To summarize the lyoprotective mechanisms and types of liposomal lyoprotectants, in order to give guidance for the selection of liposomal lyoprotectants. Methods The lyoprotective mechanisms and types of lyoprotectants were summarized and analyzed on the basis of 46 published literatures. Results The lyoprotectants may play a role in protecting liposomes from damage through the following three aspects ： （ 1 ） Dry lipids have physical properties similar to those of hydrated lipids due to the interaction between the lyoprotectants and phosphate headgroup by means of hydrogen bonding. （2） The dehydration-induced liquid crystalline to gel phase transitions was restrained as a result of the osmotic and volumetric properties of lyo- protectants. （3）The glass matrix between the membranes prevented liposome fusion and restrained the in- creasing of the phase transitions temperature. The protective effects of lyoprotectents represented by saccha- rides varied according to the types of lyoprotectants and phospholipids. Conclusions This article will provide references for the selection of liposomal lyoprotectants and the development of lyophilized products.