title: [Pharmacokinetics of SN-38 in rats and tissue distribution of 7-ethyl-10-hydroxycamptothecin in mice after intravenous injection of irinotecan hydrochloride nanoparticles].
abstract: The paper reported an investigation of the pharmacokinetics of SN-38 (7-ethyl-10-hydroxy-camptothecin) in rats and the tissue distribution in mice after injection of irinotecan hydrochloride nanoparticles (CPT-11) via tail veins. An LC-MS/MS method was established to determine the concentrations of SN-38 in whole blood of rats and in different tissues of mice. The pharmacokinetics and tissue distribution of SN-38 were compared after the intravenous injection of CPT-11 NPs and CPT-11 solution. Compared with irinotecan solution, the elimination half-life of SN-38 was prolonged from 2.17 h to 2.67 h after the intravenous injection of CPT-11 NPs, but its AUC had little change. After the injection of CPT-11 NPs in mice, over time, the concentrations of CPT-11-metabolized SN-38 in CPT-11 NPs were significantly higher in the whole blood, colon and lungs than those in CPT-11 solution, followed by in the spleen and liver, but those in the heart and brain had no change. However, the amount of SN-38 in the kidneys was reduced with time. CPT-11 NPs could prolong SN-38's (one of its metabolites) blood circulation time in rats and significantly increased the concentration of CPT-11-metabolized SN-38 in the whole blood, colon and lungs of mice. CPT-11 NPs made SN-38 efficiently target-bind to the colon and lungs of mice.
authors.forename: Fu-Ying
authors.initials: FY
authors.lastname: Yang
authors.forename: Wen-Ping
authors.initials: WP
authors.lastname: Zhang
authors.forename: Xin-Yu
authors.initials: XY
authors.lastname: Wang
authors.forename: Wen-Cheng
authors.initials: WC
authors.lastname: Yang
authors.forename: Hong-Wan
authors.initials: HW
authors.lastname: Dang
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000493:pharmacokinetics*; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D002853:Chromatography, Liquid; D003106:Colon / Q000378:metabolism; D006207:Half-Life; D007275:Injections, Intravenous; D000077146:Irinotecan; D008168:Lung / Q000378:metabolism; D051379:Mice; D053758:Nanoparticles / Q000008:administration & dosage; D051381:Rats; D053719:Tandem Mass Spectrometry; D014018:Tissue Distribution
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D000077146:Irinotecan; D002166:Camptothecin