Incorporation of amphotericin B(Fungizone) in rat brain total lipid liposomes markedly decreases its i.v. toxicity in mice.
Toxicity of the clinically utilized formulation of amphotericin B (1; Fungizone) incorporated in different lipid liposomes was compared in mice. The relative toxicity of i.v. administration of 67 mg Fungizone/kg (30 mg 1/kg), was in the order: Fungizone > Fungizone in phosphatidylcholine liposomes > Fungizone in phosphatidylcholine/cholesterol liposomes > 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 and disorder of the Fungizone liposomes and their toxicity was observed.
Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava.
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D000666:Amphotericin B / Q000008:administration & dosage* / Q000633:toxicity; D000818:Animals; D001923:Brain Chemistry; D004578:Electron Spin Resonance Spectroscopy; D007275:Injections, Intravenous; D007928:Lethal Dose 50; D008081:Liposomes; D051379:Mice; D010743:Phospholipids; D051381:Rats
D008081:Liposomes; D010743:Phospholipids; D000666:Amphotericin B