Nexstar Pharmaceuticals, Inc.

Gilead Sciences, Inc.

Osi Pharmaceuticals, Inc.

Amplimed, Inc.

Su-Ming Chiang

Richard T Proffitt

Jill P Adler-Moore

Kevin R Bracken

Eskild A Petersen

Evan M Hersch

David Lloyd Emerson

Ning Hu

Karen Lewis Moynihan

Claudine S Ashvar

Gerard M Jensen

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

Liposomal encapsulated camptothecin formulations are provided. The liposomes have improved pharmacokinetics, enhanced efficacy as anti-tumor agents and provide an increased therapeutic index as compared to the free drug and topotecan. The formulations include liposomes comprising at least one phospholipid and a camptothecin or analog thereof.

Liposomal camptothecin formulations

Liposomal encapsulated benzoquinazoline thymidylate synthase inhibitor formulations are provided. The liposomes have improved pharmacokinetics and enhanced efficacy as anti-tumor agents compared to the free drug. The formulations include liposomes comprising at least one phosphatidylcholine, a cholesterol, and a benzoquinazoline thymidylate synthase inhibitor.

Liposomal benzoquinazoline thymidylate synthase inhibitor formulations

A liposomal aminoglycoside formulation comprising a neutral lipid, a negatively charged lipids and a sterol. The formulation contains unilamellar vesicles having an average size below 100 nm. A process of making liposomes containing an aminoglycoside is also provided. A method is also provided for the treatment of drug susceptible and drug resistant bacteria.

Antibiotic formulation and use for bacterial infections

A liposomal aminoglycoside formulation comprising a neutral lipid, a negatively charged lipid and a sterol. The formulation contains unilamellar vesicles having an average size below 100 nm. A process of making liposomes containing an aminoglycoside is provided. A method is also provide for the treatment of drug susceptible and drug resistant bacteria.

Antibiotic formulation and use for drug resistant infections

A liposomal aminoglycoside formulation comprising a neutral lipid, a negatively charged lipids and a sterol. The formulation contains unilamellar vesicles having an average size below 100 nm. A process of making liposomes containing an aminoglycoside is provided where the hydration temperature is significantly below the transition temperature of the formulation. A method for the treatment of drug susceptible and drug resistant bacteria.

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.

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Canoga Park, CA, United States of America

Su-Ming Chiang