INCORPORATION OF AMPHOTERICIN-B (FUNGIZONE(R)) IN RAT-BRAIN TOTAL LIPID LIPOSOMES MARKEDLY DECREASES ITS IV TOXICITY IN MICE

Toxicity of the clinically utilized formulation of amphotericin B (1; Fungizone(R)) incorporated in different lipid liposomes was compared i n mice. The relative toxicity of i.v. administration of 67 mg Fungizon e/kg (30 mg 1/kg), was in the order: Fungizone > Fungizone in phosphat idylcholine liposomes > Fungizone in phosphatidylcholine/cholesterol l iposomes > Fungizone in rat brain total lipid liposomes. The survival time of the mice after administration of Fungizone and of Fungizone in total lipid liposomes was less than 1 min and over 30 d, respectively . Using EPR spectroscopy of spin probes a relation between dynamics an d disorder of the Fungizone liposomes and their toxicity was observed.