Uptake characteristics of liposomes by rat alveolar macrophages: influence of particle size and surface mannose modification.
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.
Chono
Sumio
S
Department of Pharmaceutics, Hokkaido Pharmaceutical University, 7-1 Katsuraoka-cho, Otaru-city 047-0264, Japan. s-chono@hokuyakudai.ac.jp
Tanino
Tomoharu
T
Seki
Toshinobu
T
Morimoto
Kazuhiro
K
D000281:Administration, Intranasal; D000814:Aniline Compounds / Q000737:chemistry*; D000818:Animals; D001992:Bronchoalveolar Lavage Fluid / Q000166:cytology; D002460:Cell Line; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D008168:Lung / Q000378:metabolism; D016676:Macrophages, Alveolar / Q000378:metabolism*; D008297:Male; D008362:Mannosides / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D013499:Surface Properties
D000814:Aniline Compounds; D008081:Liposomes; D008362:Mannosides; C034056:4-aminophenylmannoside