Preparation of Conjugated Linoleic Acid Microemulsions and their Biodistribution.
Conjugated linoleic acid (CLA) has several beneficial biological properties. Specifically, trans10, cis12-CLA, one of the CLA isomers, has strong physiologic activity against cancer and obesity. However, compared with cis9, trans11-CLA, a naturally occurring CLA isomer, trans10, cis12-CLA tends to be easily metabolized. Therefore, to make efficient use of its biological properties, it is necessary to overcome the rapid clearance of trans10, cis12-CLA from the blood. Here, we employed premix membrane emulsification to prepare two oil-in-water CLA microemulsions (CLA-ME), 100 nm CLA-ME and 200 nm CLA-ME, and investigated their pharmacokinetics in a mouse model. We report that 100 nm CLA-ME contributed to the concentration of blood CLA for longer than 200 nm CLA-ME, indicating that small CLA microparticles were more suitable for maintaining blood trans10, cis12-CLA levels in vivo. However, both CLA-ME could be hardly detected in blood and other tissues 24 h after administration, suggesting that additional strategies for prolonging CLA-ME half-life are required.
Interdisciplinary Graduate School of Agriculture and Engineering, University of Miyazaki.
Kazuaki
K
Kishita
Kayo
K
Ibaraki
Shoko
S
Itakura
Yumi
Y
Yamasaki
Naoko
N
Nishikata
Kenji
K
Yamamoto
Masataka
M
Shimizu
Kazuo
K
Nishiyama
Masao
M
Yamasaki
D000818:Animals; D004655:Emulsions / Q000032:analysis / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D044243:Linoleic Acids, Conjugated / Q000097:blood* / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D014018:Tissue Distribution
D004655:Emulsions; D044243:Linoleic Acids, Conjugated