title: Sustained-release methotrexate for intracavitary chemotherapy.
abstract: Methotrexate was encapsulated into a lipid-based drug-delivery system to create a slow-release formulation (Depo/methotrexate) for intracavitary administration. Depo/methotrexate was stable in storage at 4 degrees C for > 4 months. In human plasma at 37 degrees C, the half-life of drug release was 40 days. After intraperitoneal injection of Depo/methotrexate in mice, the intraperitoneal apparent half-life of free methotrexate was 39.6 h, in contrast to a half-life of 0.5 h for the unencapsulated standard methotrexate (std/methotrexate). In L1210 murine leukemia model, the potency of a single dose of Depo/methotrexate was 334-fold higher, the increased life-span (ILS) was 2-fold greater, and the therapeutic index was 2-fold higher than a single dose of std/methotrexate.
authors.affiliation: University of California San Diego, Cancer Center, La Jolla 92093-0812.
authors.forename: E
authors.initials: E
authors.lastname: Chatelut
authors.forename: P
authors.initials: P
authors.lastname: Suh
authors.forename: S
authors.initials: S
authors.lastname: Kim
mesh_terms: D000818:Animals; D017690:Cell Transplantation; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D007274:Injections, Intraperitoneal; D007939:Leukemia L1210 / Q000188:drug therapy; D008297:Male; D008727:Methotrexate / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D051379:Mice; D008815:Mice, Inbred Strains; D009368:Neoplasm Transplantation
chemical_list: D003692:Delayed-Action Preparations; D008727:Methotrexate