Design of liposomes to improve delivery of amphotericin-B in the treatment of aspergillosis.

The efficacy and toxicity of free and liposome intercalated amphotericin-B (Amp-B) in controlling Aspergillosis, caused by Aspergillus fumigatus in BALB/c mice were studied. Liposomal Amp-B had higher LD50 (8.1 mg/kg) as compared to that of the free drug (1.2 mg/kg). An improvement in the therapeutic index of the drug was observed with liposomal formulation of the drug. We also focussed on the effect of lipid composition and surface sugar in modulating the therapeutic potency of Amp-B. The most effective liposomal preparation was composed of egg phosphatidylcholine (EPC): L-alpha-phosphatidylethanolamine, dipalmitoyl (DPPE): cholesterol (Chol) in the molar ratio of 6:1:3. Amp-B intercalated into mannose grafted liposomes (LD50 = 9.3 mg/kg) was more effective as compared to the other formulation tested.