Polyene microlide pre-liposomal powders

Abstract

Abstract The present invention involves a process for producing fine powder suitable for the preparation of antifungal polyene microlide-containing liposomes upon suspension in an aqueous solution. This process comprises the following steps. Quantities of polyene macrolide and phospholipids are dissolved respectively in a first solvent and a second solvent to form a first solution and a second solution. The first solution and the second solution are mixed in a desired ratio to form a mixture. The first solvent and the second solvent are then removed from the mixture, for example by evaporation, to form a residue. The residue is then dissolved in a third solvent comprising tertiary butanol and methylene chloride to form a third solution. The third solvent is then removed from the third solution to form a remnant. The remnant is then dissolved in a solvent consisting essentially of tertiary butanol to form a fourth solution. The fourth solution is then filtered through a filter having orifices of between about 0.05 and 0.5 micrometers in diameter to produce a filtrate. The filtrate is lyophilized to remove the tertiary butanol and a fine powder remains. This fine powder may be used to form polyene macrolide-containing liposomes by simple incubation or suspension in an aqueous solution.

Inventors

• 👤 Reeta Mehta
• 👤 Gabriel Lopez-Berestein

Bibliographic Details