Increased therapeutic efficiency of a lipid-soluble alkylating agent incorporated in liposomes.
A highly hydrophobic alkylating agent, 1-N,N-bis(beta-bromoethyl) amino-3-methylnaphthalene, given as the free drug in oil, cured a substantial proportion of mice bearing the PC6 myeloma in the dose range 2-7 mg/kg. However, these doses were toxic, and the LD50 was 6-7 mg/kg. When incorporated in liposomes, similar curative effects were obtained at doses of 10-41 mg/kg without material toxicity, even at the highest dose. Liposome entrapment therefore greatly increases the therapeutic efficiency of this agent.
D015057:1-Naphthylamine / Q000031:analogs & derivatives / Q000627:therapeutic use* / Q000633:toxicity; D000477:Alkylating Agents / Q000627:therapeutic use* / Q000633:toxicity; D000818:Animals; D004305:Dose-Response Relationship, Drug; D008081:Liposomes / Q000008:administration & dosage*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D009101:Multiple Myeloma / Q000188:drug therapy*; D009281:Naphthalenes / Q000627:therapeutic use*; D009374:Neoplasms, Experimental / Q000188:drug therapy; D009821:Oils / Q000008:administration & dosage
D000477:Alkylating Agents; D008081:Liposomes; D009281:Naphthalenes; D009821:Oils; C035403:1-N,N-bis(beta-bromoethyl)amino-3-methylnaphthalene; D015057:1-Naphthylamine