Murahashi N, Ishihara H, Sakagami M, Sasaki A
Drug Delivery System Institute, Ltd., Science University of Tokyo, Chiba, Japan.
Biol Pharm Bull. 1997 Jun;20(6):704-7. doi: 10.1248/bpb.20.704.
We synthesized various glycolipid derivatives and examined the in vivo behaviors of liposomes modified with these novel glycolipid derivatives. Gal-t-psa (1,¿8-(2-hexadecyloctadecanoylamido)-3,6-dioxaoctyl¿-beta-D- galactoside), Lac-t-psa (3, 8-(2-hexadecyloctadecanoylamido)-3,6-dioxaoctyl beta-D-lactoside) and GalNAc-t-psa (4, 8-(2-hexadecyloctadecanoylamido)-3,6-dioxaoctyl 2-acetamido-beta-D-galactopyranoside) modified liposomes were recognized by the liver. Lac-t-psa (3) modified liposome was accumulated to the highest degree, followed by GalNAc-t-psa (4) modified liposome and then Gal-t-psa (1) modified liposome. The intrahepatic distributions of Gal-t-psa (1), GalNAc-t-psa (4), Glc-t-psa (2, 8-(2-hexadecyloctadecanoylamido)-3,6-dioxaoctyl beta-D-glucopyranoside) and Lac-t-psa (3) modified liposomes were investigated. GalNAc-t-psa (4) and Lac-t-psa (3) modified liposome were accumulated to greater extents than Gal-t-psa (1) modified liposome in hepatic parenchymal cells. The intrahepatic distribution of these liposomes showed that Lac-t-psa (3) and GalNAc-t-psa (4) were preferable to Gal-t-psa (1) for the selective delivery of liposomes to hepatic parenchymal cells.
我们合成了各种糖脂衍生物，并研究了用这些新型糖脂衍生物修饰的脂质体在体内的行为。半乳糖 - t - psa（1,8 -（2 - 十六烷基十八烷酰胺基）- 3,6 - 二氧杂辛基 - β - D - 半乳糖苷）、乳糖 - t - psa（3,8 -（2 - 十六烷基十八烷酰胺基）- 3,6 - 二氧杂辛基β - D - 乳糖苷）和N - 乙酰半乳糖胺 - t - psa（4,8 -（2 - 十六烷基十八烷酰胺基）- 3,6 - 二氧杂辛基2 - 乙酰氨基 - β - D - 吡喃半乳糖苷）修饰的脂质体可被肝脏识别。乳糖 - t - psa（3）修饰的脂质体积累程度最高，其次是N - 乙酰半乳糖胺 - t - psa（4）修饰的脂质体，然后是半乳糖 - t - psa（1）修饰的脂质体。研究了半乳糖 - t - psa（1）、N - 乙酰半乳糖胺 - t - psa（4）、葡萄糖 - t - psa（2,8 -（2 - 十六烷基十八烷酰胺基）- 3,6 - 二氧杂辛基β - D - 吡喃葡萄糖苷）和乳糖 - t - psa（3）修饰的脂质体在肝脏内的分布。N - 乙酰半乳糖胺 - t - psa（4）和乳糖 - t - psa（3）修饰的脂质体在肝实质细胞中的积累程度比半乳糖 - t - psa（1）修饰的脂质体更大。这些脂质体在肝脏内的分布表明，对于将脂质体选择性递送至肝实质细胞而言，乳糖 - t - psa（3）和N - 乙酰半乳糖胺 - t - psa（4）比半乳糖 - t - psa（1）更具优势。
