Sasaki A, Murahashi N, Yamada H, Morikawa A
Drug Delivery System Institute, Ltd., Science University of Tokyo, Chiba, Japan.
Biol Pharm Bull. 1994 May;17(5):680-5. doi: 10.1248/bpb.17.680.
The effects of liposomes, bearing galactosyl ligands on their surface, on their clearance from circulation and on tissue distribution were studied in rats. The ligands were obtained through coupling 2,3,4,6-tetraacetyl-(2-[2-(2-aminoethoxy)ethoxy]ethyl)-beta- D-galactoside p-toluenesulfonate with hydrophobic anchors, followed by deprotection. We introduced mid-chain or long, branched or non-branched alipathic chains, and cholesterol as anchors. Among various anchors tested, that with a dihexadecyl branch caused the greatest accumulation of liposomes in the liver. On the other hand, liposome bearing these ligands were aggregated by Ricinus communis agglutin. This showed that these ligands were similarly incorporated to liposomes. These results show the importance of the balance between lipophilicity and the structure of ligands.
研究了表面带有半乳糖基配体的脂质体对其在大鼠体内循环清除率及组织分布的影响。这些配体是通过将2,3,4,6-四乙酰基-(2-[2-(2-氨基乙氧基)乙氧基]乙基)-β-D-半乳糖苷对甲苯磺酸盐与疏水锚定基团偶联，然后进行脱保护而获得的。我们引入了中链或长链、支链或非支链脂肪族链以及胆固醇作为锚定基团。在测试的各种锚定基团中，带有二十六烷基二分支的锚定基团使脂质体在肝脏中的积累最多。另一方面，带有这些配体的脂质体被蓖麻凝集素凝集。这表明这些配体以相似的方式掺入脂质体中。这些结果表明了亲脂性与配体结构之间平衡的重要性。
