Amphotericin B liposome preparation
AssigneeGilead Sciences, Inc.
InventorsRichard T. Proffitt, Jill Adler-Moore, Su-Ming Chiang
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Abstract
A novel composition and method for solubilizing amphiphilic drugs in a small amount of organic solvent for use in improved liposomes is disclosed. A phosphatidylglycerol is acidified in a small amount of organic solvent. The amphiphilic drug, such as Amphotericin B, suspended in organic solvent is then added to the acidified phosphatidylycerol and a soluble complex is formed between the phosphatidylglycerol and the amphiphilic drug. When the liposome composition incorporating the soluble complex is hydrated, the final pH of the hydrating aqueous buffer is carefully controlled. The Amphotericin B liposomes formed have markedly reduced toxicity.
Claims22
A process for solubilizing amphiphilic drugs for use in the preparation of liposomes, comprising:
- a) acidifying a phospholipid in a small quantity of organic solvent;
- b) adding said amphiphilic drug to said organic solvent;
- and
- c) forming a soluble complex between said acidified phospholipid and said amphiphilic drug.
A therapeutic formulation for treating disseminated fungal infections comprising a polyene antibiotic encapsulated within a liposome, said liposome comprising phosphatidylcholine, a sterol, and a soluble complex of said polyene and phosphatidylglycerol and in an aqueous solution having a pH between about 2.0 and 5.5.
Dependencies are inferred from the claim text.