Selective transfer of cyclosporin to thoracic lymphatic systems by the application of lipid microspheres.
To overcome some of the disadvantages of present cyclosporin A (CsA) therapy, lipid microspheres incorporating CsA (lipo-CsA) were designed and their selective transfer to thoracic lymphatic systems was evaluated in vivo. It was found that concentrations of CsA in lymph-ducts were about 46 times higher after 2 h and 9-10 times higher after 3 h following oral administration of lipo-CsA, compared with those of conventional CsA. The concentrations in plasma produced by lipo-CsA were also higher than those produced by conventional CsA.
Yanagawa
A
A
First Department of Internal Medicine, School of Medicine, St. Marianna University, Kanagawa-Pref, Japan.
Iwayama
T
T
Saotome
T
T
Shoji
Y
Y
Takano
K
K
Oka
H
H
Nakagawa
T
T
Mizushima
Y
Y
D000818:Animals; D001692:Biological Transport; D003524:Cyclosporins / Q000008:administration & dosage* / Q000493:pharmacokinetics; D004337:Drug Carriers; D008055:Lipids / Q000008:administration & dosage*; D008208:Lymphatic System / Q000378:metabolism*; D008863:Microspheres; D051381:Rats; D011919:Rats, Inbred Strains
D003524:Cyclosporins; D004337:Drug Carriers; D008055:Lipids