磷脂酰聚乙二醇单甲醚的合成及其自组装纳米胶束的研究

Synthesis and Self-Assembling Nano-Micelles of Phosphatidyl Polyethyleneglycol Monomethyl Ether

以甘油为起始原料,通过苄基保护、加氢还原以及酯化等环节得到一系列含有不同长度PEG、不同脂肪酸的磷脂酰聚乙二醇单甲醚。通过溶剂挥发法制备了mPEG-磷脂胶束,并通过荧光探针法、扫描电子显微镜、透射电子显微镜和粒度及电位分析仪等对其进行了表征。结果表明,制备的磷脂酰聚乙二醇单甲醚胶束,具有明显的核-壳球状结构,粒径分布在100～200 nm;文中报道的磷脂酰聚乙二醇单甲醚的临界胶束浓度都在10-6mol/L,与小分子的表面活性剂相比,CMC值较低,在水中的稳定性增强,其中该磷脂胶束受到环境盐浓度/糖浓度的影响时粒径有不同程度的增大。所合成的磷脂酰聚乙二醇单甲醚自组装纳米胶束结构稳定,对于药物而言是一种较好的纳米载体。

A series of phosphatidyl polyethyleneglycol monomethyl ether nano-micelles were synthesized by benzyl protecting,hydrogenation reduction and esterification using glycerol as raw material.The micelles were prepared by solvent evaporation method,and characterized and analized by fluorescent probe,scanning electron microscopy,transmission electron microscopy,Zeta PALS-submicron size and potential analyzer.Experimental results showed that the mPEG-lipids formed spherical micelles with core-shell structure and an average diameter of 100-200 nm,and the CMC of nano-micelles were 10^-6 mol/L.Compared to conventional small molecules surfactant,mPEG-lipids micelles have better stability in water due to the lower CMC.Ambient effect such as salt,glucose exerts a strong influence on the stability of the micelles.And these influence is tightly correlated to their concentration.Due to their stable structure,phosphatidyl polyethyleneglycol monomethyl ether nano-micelles have promise of being applied as nano carriers for drugs.