Chono Sumio, Tanino Tomoharu, Seki Toshinobu, Morimoto Kazuhiro
Department of Pharmaceutics, Hokkaido Pharmaceutical University, 7-1 Katsuraoka-cho, Otaru-city 047-0264, Japan.
J Pharm Pharmacol. 2007 Jan;59(1):75-80. doi: 10.1211/jpp.59.1.0010.
The influence of particle size and surface mannose modification on the uptake of liposomes by alveolar macrophages (AMs) was investigated in-vitro and in-vivo. Non-modified liposomes of five different particle sizes (100, 200, 400, 1000 and 2000 nm) and mannosylated liposomes with 4-aminophenyl-alpha-D-mannopyranoside (particle size 1000 nm) were prepared, and the uptake characteristics by rat AMs in-vitro and in-vivo were examined. The uptake of non-modified liposomes by rat AMs in-vitro increased with an increase in particle size over the range of 100-1000 nm, and became constant at over 1000 nm. The uptake of non-modified liposomes by AMs after pulmonary administration to rats in-vivo increased with an increase in particle size in the range 100-2000 nm. The uptake of mannosylated liposomes (particle size 1000 nm) by rat AMs both in-vitro and in-vivo was significantly greater than that of non-modified liposomes (particle size 1000 nm). The results indicate that the uptake of liposomes by rat AMs is dependent on particle size and is increased by surface mannose modification.
在体外和体内研究了粒径和表面甘露糖修饰对肺泡巨噬细胞（AMs）摄取脂质体的影响。制备了五种不同粒径（100、200、400、1000和2000 nm）的未修饰脂质体以及带有4-氨基苯基-α-D-甘露吡喃糖苷的甘露糖基化脂质体（粒径1000 nm），并检测了大鼠AMs在体外和体内的摄取特性。大鼠AMs在体外对未修饰脂质体的摄取在100 - 1000 nm范围内随粒径增加而增加，在1000 nm以上保持恒定。在体内将未修饰脂质体经肺部给药大鼠后，AMs对其摄取在100 - 2000 nm范围内随粒径增加而增加。大鼠AMs在体外和体内对甘露糖基化脂质体（粒径1000 nm）的摄取均显著大于未修饰脂质体（粒径1000 nm）。结果表明，大鼠AMs对脂质体的摄取取决于粒径，并且表面甘露糖修饰可增加其摄取。
Zotero 插件