title: Selective delivery of 5-fluorouracil (5-FU) to i.p. tissues using 5-FU microspheres in rats.
abstract: A new formulation has been developed for the delivery of 5-fluorouracil (5-FU) in treating peritoneal carcinomatosis. The new formulation (5-FU-MS) involves the incorporation of 5-FU into microspheres composed of a poly(glycolide-co-lactide) matrix. The incorporated 5-FU is released slowly over a 3 week period. We investigated the drug distribution and pharmacokinetics of 5-FU in rats receiving an i.p. injection of 5-FU-MS or aqueous 5-FU solution. The concentration of 5-FU was higher in the i.p. tissues (omentum and mesentery) and lower in the extraperitoneal tissues (blood plasma, lung and heart) in rats given 5-FU-MS than in rats given the aqueous 5-FU solution. Pharmacokinetic analysis showed that the area under the curve (AUC) was significantly greater in the omentum and the mesentery than in other tissues of rats given 5-FU-MS. There was no significant difference in the AUC in the tissues of rats given the aqueous 5-FU solution.
authors.affiliation: First Department of Surgery, Kyoto Prefectural University of Medicine, Kamigyo-ku, Japan.
authors.forename: A
authors.initials: A
authors.lastname: Hagiwara
authors.forename: C
authors.initials: C
authors.lastname: Sakakura
authors.forename: H
authors.initials: H
authors.lastname: Tsujimoto
authors.forename: T
authors.initials: T
authors.lastname: Imanishi
authors.forename: M
authors.initials: M
authors.lastname: Ohgaki
authors.forename: J
authors.initials: J
authors.lastname: Yamasaki
authors.forename: K
authors.initials: K
authors.lastname: Sawai
authors.forename: T
authors.initials: T
authors.lastname: Takahashi
authors.forename: T
authors.initials: T
authors.lastname: Fujita
authors.forename: A
authors.initials: A
authors.lastname: Yamamoto
authors.forename: S
authors.initials: S
authors.lastname: Muranishi
authors.forename: Y
authors.initials: Y
authors.lastname: Ikada
mesh_terms: D000818:Animals; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D007274:Injections, Intraperitoneal; D007668:Kidney / Q000737:chemistry / Q000187:drug effects; D008099:Liver / Q000737:chemistry / Q000187:drug effects; D008297:Male; D008863:Microspheres; D009852:Omentum; D051381:Rats; D017208:Rats, Wistar; D013154:Spleen / Q000737:chemistry / Q000187:drug effects; D014018:Tissue Distribution
chemical_list: D005472:Fluorouracil