Yamauchi H, Kikuchi H, Sawada M, Tomikawa M, Hirota S
Tokyo R&D Center, Daiichi Pharmaceutical Co. Ltd., Japan.
J Microencapsul. 1994 Mar-Apr;11(2):179-88. doi: 10.3109/02652049409040449.
In this study we characterized liposomes containing the synthetic glycolipids, lactose mono-fatty acid esters (LFEs), whose structures were the most simple ones compared to the other synthetic glycolipids. Gel filtration chromatography was used to confirm that 78 per cent of lactose monostearic acid ester (LSE) or 85 per cent of lactose monoarachidic acid ester (LAE) existed in the liposomal fraction. The size distribution of liposomes containing LFEs was similar to that of the control liposomes which did not contain LFEs. Liposomes containing LFEs were aggregated by Ricinus communis agglutinin from caster bean (RCA120) while the control liposomes were not, with the agglutinability of the liposomes containing LAE being greater than that of those containing LSE. These findings therefore suggested that the LFEs were incorporated into the liposomal membrane with the galactose residues exposed to the outer aqueous phase. Next, the tissue distribution of liposomes containing LAE at 30 min after intravenous administration was compared to that of the control liposomes in rats. Hepatic uptake was 2-fold higher than that of the control liposomes. These results thus demonstrate that liposomes containing LFEs represent potential drug carriers to the liver.
在本研究中，我们对含有合成糖脂乳糖单脂肪酸酯（LFE）的脂质体进行了表征，与其他合成糖脂相比，其结构最为简单。采用凝胶过滤色谱法确认，78%的乳糖单硬脂酸酯（LSE）或85%的乳糖单花生酸酯（LAE）存在于脂质体部分。含有LFE的脂质体的大小分布与不含LFE的对照脂质体相似。含有LFE的脂质体被来自蓖麻的蓖麻凝集素（RCA120）凝集，而对照脂质体则不会，含有LAE的脂质体的凝集性大于含有LSE的脂质体。因此，这些发现表明LFE被整合到脂质体膜中，半乳糖残基暴露于外部水相。接下来，将静脉注射30分钟后含有LAE的脂质体与对照脂质体在大鼠体内的组织分布进行了比较。肝脏摄取量比对照脂质体高2倍。因此，这些结果表明含有LFE的脂质体是肝脏潜在的药物载体。
