Nexstar Pharmaceuticals, Inc.

Gilead Sciences, Inc.

Vestar, Inc.

Vestar Research, Inc.

Jill P Adler-Moore

Richard T Proffitt

Su-Ming Chiang

William A Ernst

Ronald C Gamble

Larry J Moore

Richard Thomas Proffitt

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.

Amphotericin B liposome preparation

Formulations consisting of phospholipid small unilamellar particles encapsulating polyene antifungal antibiotics and methods for using such compositions to treat systemic fungal infections are described. In a preferred embodiment, the particles are in the form of vesicles which comprise a polyene antifungal antibiotic, preferably amphotericin B and/or nystatin, egg phosphatidylcholine and cholesterol, preferably in the molar ratio of about 0.2 (AMB):2(PL):1(CHOL). These vesicles may also have an amine modified surface. The vesicles are suspended in a low isonic strength saccharide/tris solution at a pH of from about 6.0 to about 8.0 and may be administered to deliver the antifungal antibiotic to treat systemic fungal infections.

Treatment of systemic fungal infections with phospholipid particles

A process for preparing a liposomal cyclosporin therapeutic formulation, which comprises dissolving a combination of a neutral and negatively charged phospholipid and a cyclosporin in an organic solvent; drying the solution to form a solid phase, and hydrating the solid phase in an aqueous solution having a pH ranging from 7.5 to 9.5.

Pharmaceutical formulation and process

An improved liposomal cyclosporin therapeutic formulation, comprising phosphatidylcholine, phosphatidylglycerol and a cyclosporin in a mole ratio of from 25:3:1 to 17:3:1 is described. The formulation includes unilamellar vesicles having reduced toxicity. The formulation is used as an immunosuppressive agent and is an enhancer of the efficacy of antineoplasties for drug resistant cancer cells. A method is also provided for inhibiting the growth of cancer cells.

Liposomal cyclosporin pharmaceutical formulation

An improved liposomal cyclosporin therapeutic formulation, comprising phosphatidylcholine, cholesterol, dimyristoylphosphatidylglycerol and a cyclosporin in a mole ratios of about 21:0.5:3:1 to 21:1.5:3:1 and 24:0.5:3:1 to about 24:1.5:3:1. The formulations are useful as immunosuppressive agents and enhancers of antineoplastic agents in drug resistant cancer cells.

Liposomal cyclosporin formulations as agents for immunosuppression and

Adhesions in synovial capsules are prevented through the administration of liposome intercalated nonsteroidal anti-inflammatory agents.

Prevention of synovial adhesions

Formulations consisting of phospholipid small unilamellar particles encapsulating polyene antifungal antibiotics and methods for using such compositions to treat systemic fungal infections are described. In a preferred embodiment, the particles are in the form of vesicles which comprise a polyene antifungal antibiotic, preferably amphotericin B and/or nystatin, egg phosphatidylcholine and cholesterol, preferably in the molar ratio of about 0.2 (AMB):2(PL):1(CHOL). These vesicles may also have an amine modified surface. The vesicles are suspended in a low ionic strength saccharide/tris solution at a pH of from about 6.0 to about 8.0 and may be administered to deliver the anti-fungal antibiotic to treat systemic fungal infections.

Growing community of inventors

Altadena, CA, United States of America

Jill P Adler-Moore