Antitumor activity of a water-insoluble compound entrapped in liposomes on L1210 leukemia in mice.
The use of sonicated phospholipid vesicles (liposomes) as carriers of 2-[3'-(methoxycarbonylamino)-phenyl]-3-phenyl-6-methoxycarbonylamino-4-(3H)- quinazolone (NSC-251635), a water-insoluble antimitotic compound, was investigated in mice. NSC-251635 was incorporated in egg yolk lecithin, cholesterol, and stearylamine (4:3:1) liposomes. In vitro, NSC-251635 in suspension or entrapped in liposomes was not toxic for L1210 cells. In vivo, after ip or iv injections to CDF1 mice bearing intraperitoneal or intravenous L1210 leukemia, NSC-251635 was active only when it was incorporated in the liposomes and not when it was given as a suspension in Klucel or in saline. The NSC-251635 liposome preparation induced significantly prolonged survival of the treated animals.
D000818:Animals; D002850:Chromatography, Gel; D004305:Dose-Response Relationship, Drug; D005260:Female; D066298:In Vitro Techniques; D007274:Injections, Intraperitoneal; D007275:Injections, Intravenous; D007939:Leukemia L1210 / Q000188:drug therapy* / Q000473:pathology; D008081:Liposomes / Q000008:administration & dosage* / Q000302:isolation & purification; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009368:Neoplasm Transplantation; D011799:Quinazolines / Q000008:administration & dosage*
D008081:Liposomes; D011799:Quinazolines; C038202:NSC 251635