title: Modification of liposomes by addition of HCO60. I. Targeting of liposomes to liver by addition of HCO60 to liposomes.
abstract: The influence of HCO60 on the blood clearance and tissue distribution of soybean phosphatidylcholine (PC) liposomes, encapsulating alpha-tocopherol as a marker, was studied in rats. The liposomes were prepared by the hydration method from a lipid film containing different amounts of HCO60, and by extrusion through a 0.1 micron polycarbonate membrane filter. The blood clearance and liver uptake of alpha-tocopherol after i.v. administration increased with increasing the amount of HCO60 the liposome contained. With 80 wt% HCO60 liposomes, the accumulation of alpha-tocopherol in the liver was approximately three-fold that of the 100% PC liposomes. The uptake by lungs, spleen and kidneys did not change with the addition of HCO60. The findings obtained in a gel-filtration study suggested that alpha-tocopherol is not removed from the liposomes, with or without HCO60, by rat plasma proteins and the HCO60 micelle may form a complex with rat plasma proteins. Our findings suggest that liposomes containing large amounts of HCO60 (more than 60 wt%) will be useful for delivering drug to the liver.
authors.affiliation: Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Shizuoka, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Kato
authors.forename: K
authors.initials: K
authors.lastname: Watanabe
authors.forename: T
authors.initials: T
authors.lastname: Hosokawa
authors.forename: E
authors.initials: E
authors.lastname: Hayakawa
authors.forename: K
authors.initials: K
authors.lastname: Ito
mesh_terms: D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D002368:Castor Oil / Q000031:analogs & derivatives*; D002850:Chromatography, Gel; D004337:Drug Carriers; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry; D008099:Liver / Q000378:metabolism*; D008297:Male; D008823:Micelles; D010713:Phosphatidylcholines / Q000008:administration & dosage; D051381:Rats; D017208:Rats, Wistar; D013501:Surface-Active Agents; D014018:Tissue Distribution; D014810:Vitamin E / Q000008:administration & dosage / Q000378:metabolism
chemical_list: D001798:Blood Proteins; D004337:Drug Carriers; D008081:Liposomes; D008823:Micelles; D010713:Phosphatidylcholines; D013501:Surface-Active Agents; D014810:Vitamin E; C023040:polyethoxylated castor oil; D002368:Castor Oil