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以半乳糖神经酰胺(galactosylceramide,GC) 为材料, 采用冷冻干燥脱水再水化法(DRV 法)制成包裹有蓖麻毒蛋白的半乳糖神经酰胺脂质体(ricinGCLs), 并对其性质及体外细胞毒性和动物毒性做了研究。实验结果表明,ricinGCLs 的最大包封率可达74 .1 % , 粒度分布主要在0.5 ~0.8 μm 之间, 符合静脉注射液的标准。脂质体冻干粉在4 ℃储存近半年, 粒度分布几乎没有变化。体外细胞毒性实验结果表明,ricinGCLs 和游离蓖麻毒蛋白对人肝癌细胞7721 均有杀伤作用。RicinGCLs 的杀伤力比游离蓖麻毒蛋白更强;它们的细胞存活半数抑制浓度(IC50) 之比为1∶3 .89 。小鼠毒性试验中, 游离蓖麻毒蛋白的半数致死量(LD50) 为(30 .6 ±8 .49) μg/kg, 而ricinGCLs 的LD50 为(41.8 ±9.33) μg/kg, 高于游离蓖麻毒蛋白36 .29 % 。蓖麻毒蛋白经GCLs 包裹后, 提高了对人肝癌细胞7721 的杀伤力, 同时降低了对小鼠的整体毒性
The galactosylceramide (GC) was used as the material to prepare ricinGCLs coated with ricin by freeze-drying dehydration and rehydration (DRV method) Nature and in vitro cytotoxicity and animal toxicity were studied. The experimental results show that the maximum entrapment efficiency of ricinGCLs can reach 74. 1%, the particle size distribution is mainly between 0.5 ~ 0.8 μm, in line with the standard intravenous fluids. Liposomal lyophilized powder stored at 4 ℃ for nearly six months, the particle size distribution almost no change. In vitro cytotoxicity test results show that, ricin GCLs and free ricin on human hepatocellular carcinoma cells 7721 have killing effect. Ricin-GCLs are more lethal than free ricin; their ratio of IC50 to cell survival is 1: 3. 89. In mouse toxicity test, the LD50 of free ricin was (30.6 ± 8.79) μg / kg, while the LD50 of ricinGCLs was (41.8 ± 9.33) μg / kg, higher than free ricin 36. 29%. The inclusion of ricin in GCLs increased the lethality of human hepatocellular carcinoma cell line 7721 while reducing the overall toxicity to mice