Higgins J, Hodges N A, Olliff C J, Phillips A J
Department of Pharmacy, Brighton Polytechnic, UK.
J Pharm Pharmacol. 1987 Aug;39(8):577-82. doi: 10.1111/j.2042-7158.1987.tb03432.x.
The release of streptomycin from lecithin liposomes following a freeze-thaw cycle was used to measure the cryoprotective activities of glycinebetaine and dimethylsulphoxide (DMSO). At concentrations between 4 and 8% w/v in the external solution, glycinebetaine was superior to DMSO at freezing rates faster than 50 degrees C min-1. At lower rates their activities were similar, and drug loss ranged between 10 and 20% depending upon freezing rate and cryoprotectant concentration. The pattern of streptomycin loss when the concentrations of cryoprotectants inside and outside the liposome were varied indicated that glycinebetaine, in contrast to DMSO, does not diffuse across the liposome membrane. The activity of glycinebetaine was not impaired by the presence in the membrane of cholesterol or charged lipids.
利用冻融循环后链霉素从卵磷脂脂质体中的释放来测定甘氨酸甜菜碱和二甲基亚砜(DMSO)的冷冻保护活性。在外部溶液浓度为4%至8%(w/v)时,在冷冻速率快于50℃/分钟的情况下,甘氨酸甜菜碱比DMSO更具优势。在较低冷冻速率下,它们的活性相似,药物损失根据冷冻速率和冷冻保护剂浓度在10%至20%之间。当脂质体内外冷冻保护剂浓度变化时,链霉素损失模式表明,与DMSO不同,甘氨酸甜菜碱不会扩散穿过脂质体膜。膜中胆固醇或带电脂质的存在不会损害甘氨酸甜菜碱的活性。