Asai Yasuyuki
Formulation Research Laboratory Kawashima Eisai Co., Ltd. 1 Takahaya-machi, Kawashima-cho, Hashima-gun, Gifu 501-6195, Japan.
Pharm Dev Technol. 2006;11(2):229-33. doi: 10.1080/10837450600561430.
A sonicated dispersion of the novel lipid A analog, E5531, was feeze-dried in the presence of various additives such as saccharides and polyalcohols, and their cryoprotective effects were investigated. Fusion of the vesicles was examined by measuring fluorescence energy transfer and size distribution. Cryoprotective ability differed among the addtive species. The addition of polyalcohols led to considerable fusion. Although monosaccharides, similar to disaccharides, completely prevented the fusion of the vesicles during lyophilization, they showed far less ability to retain the entrapped calcein in the vesicles compared to disaccharides. Differential scanning calorimetry heating profiles of vesicles that had been lyophilized with various additives were obtained. Disaccharides and monosaccharides again resulted in markedly different thermal properties of the vesicles. This variety in cryoprotective ability of saccharide species can be attributed to differences in their interaction with the E5531 head group.
新型脂多糖类似物E5531的超声分散液在存在各种添加剂(如糖类和多元醇)的情况下进行冷冻干燥,并研究了它们的冷冻保护作用。通过测量荧光能量转移和尺寸分布来检测囊泡的融合情况。不同添加剂的冷冻保护能力各不相同。添加多元醇会导致显著的融合。虽然单糖与二糖类似,在冻干过程中完全阻止了囊泡的融合,但与二糖相比,它们在保留囊泡中包封的钙黄绿素方面的能力要低得多。获得了用各种添加剂冻干后的囊泡的差示扫描量热法加热曲线。二糖和单糖再次导致囊泡具有明显不同的热性质。糖类的这种冷冻保护能力的差异可归因于它们与E5531头部基团相互作用的差异。