Syntheses of Novel Galoctosyl Ligands for Liposomes and the Influence of the Spacer on Accumulation in the Rat Liver.
作者:Atsushi SASAKI、Naokazu MURAHASHI、Harutami YAMADA、Anri MORIKAWA
DOI:10.1248/bpb.18.740
日期:——
We modified the surface of liposomes with galactosyl ligands. At first we determined whether or not the galactosyl moiety was exposed on the liposomes. We then investigated the effect of the ligands on the hepatic accumulation of liposomes in rats. We introduced an oligoethylene glycol moiety as a spacer. Among the various ligands tested, those with a tri-or tetraethylene glycol moiety as a spacer caused the greatest accumulation of liposomes in the liver. Liposomes bearing ligands with a tri-or tetraethylene glycol moiety as a spacer, were aggregated by Ricinus communis agglutinin. On the other hand, those modified with ligands with a mono- or diethylene glycol spacer did not clearly agglutinate. These results show the importance of a spacer between the homing device and the ligand anchor.
我们将半乳糖基配体修饰到脂质体表面。首先,我们确定半乳糖基团是否暴露在脂质体表面。然后,我们研究了这些配体对大鼠肝脏中脂质体积累的影响。我们引入了一个聚乙二醇基团作为间隔基。在测试的各种配体中,具有三或四聚乙二醇间隔基的配体导致脂质体在肝脏中积累最多。带有三或四聚乙二醇间隔基配体的脂质体被蓖麻凝集素聚集。另一方面,修饰有单或二聚乙二醇间隔基配体的脂质体没有明显聚集。这些结果显示了归巢装置与配体锚定基之间间隔基的重要性。