Amphotericin B liposome preparation
First Claim
1. A process for solubilizing a polyene antibiotic, comprising forming a soluble complex between the polyene antibiotic and a phosphatidylglycerol in an acidified organic solvent and maintaining said soluble complex at a pH of 4.5 or less.
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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.
60 Citations
16 Claims
- 1. A process for solubilizing a polyene antibiotic, comprising forming a soluble complex between the polyene antibiotic and a phosphatidylglycerol in an acidified organic solvent and maintaining said soluble complex at a pH of 4.5 or less.
- 7. A process for the formation of liposomes containing a polyene antibiotic, comprising forming a soluble complex between a polyene antibiotic and a phosphatidylglycerol in an acidified organic solvent and maintaining said soluble complex at a pH of 4.5 or less, removing the organic solvent to form a dried complex, and hydrating the dried complex with an aqueous buffer solution to form liposomes having a diameter of less than 2.0 μ
- 12. The soluble complex of a polyene antibiotic and a phosphatidylglycerol, maintained in an acidified organic solvent having a pH of 4.5 or less.
Specification