The Liposome Company, Inc.

Air Products and Chemicals, Inc.

Igen, Inc.

Paul A Tremblay

Andrew S Janoff

Alan L Weiner

Mircea C Popescu

Lois E Bolcsak

John J Kearns

Robert L Suddith

Christine E Swenson

Michael V Bergamini

Marc J Ostro

Carl R Alving

Robert P Lenk

Michael W Fountain

Swaminathan Sunder

Rajiv Mathur

Lawrence T Boni

Joel B Portnoff

Raymond J Robey

Elaine Chan

Lois E Bolscak

Frank G Pilkiewicz

Andrew Stuart Janoff

Alan Lee Weiner

Mircea Constantine Popescu

Mathew Cherian

Frank Pilkiewicz

Methods and compositions are described for the preparation of bioactive agents entrapped in lipid vesicles the bilayers of which comprise a salt form of an organic acid derivative of a sterol, such as the tris-salt form of a sterol hemisuccinate, and to bompositions comprising a mixtue of tris(hydroxymethyl)aminomethane salt of cholesteryl hemisuccinate with either an antifungal compound or a peptide. These compositions have various applications in vivo.

Steroidal liposomes

A composition having equal to or greater than about 97 percent by weight phosphatidylcholine and about equal to or less than about 3 percent by weight to about 0.5% sphingomylin and equal to or less than about 0.5% lysophosphatidylcholine (undetectable by UV at 205 nm) has been found to result in liposomes having improved stability. Methods for preparing the composition are disclosed whereby the phospholipids are extracted and then purified using silica chromatography.

Phospholipid composition

A reduced fat chocolate preparation comprising lipid vesicles is disclosed. Also disclosed is a method of manufacturing the reduced fat chocolate preparation. The chocolate has less fat than regular chocolate and a higher percentage of water.

Reduced fat chocolate and method of manufacture

Phospholipid composition and liposomes made therefrom

Methods and compositions are described for the preparation of alpha-tocopherol vesicles, the bilayers of which comprise a salt form of an organic acid derivative of alpha-tocopherol such as the Tris salt form of alpha-tocopherol hemisuccinate. The method is rapid and efficient and does not require the use of organic solvents. The alpha-tocopherol vesicles may be used to entrap compounds which are insoluble in aqueous solutions. Such preparations are especially useful for entrapping bioactive agents of limited solubility, thus enabling administration in vivo.

Entrapment of water-insoluble compound in alpha tocopherol-based vesicles

Methods and compositions are described for the preparation of bioactive agents entrapped in lipid vesicles the bilayers of which comprise a salt form of an organic acid derivative of a sterol, such as the tris-salt form of a sterol hemisuccinate, and to compositions comprising a mixture of tris(hydroxymethyl)aminomethane salt of cholesteryl hemisuccinate with either an antifungal compound or a peptide. These compositions have various applications in vivo.

Sterodial liposomes

Method for preparing alpha-tocopherol vesicles

Methods and compositions are described for the preparation of bioactive agents entrapped in lipid vesicles the bilayers of which comprise a salt form of an organic acid derivative of a sterol, such as the tris-salt form of a sterol hemisuccinate, and to bompositions comprising a mixture of tris(hydroxymethyl)aminomethane salt of cholesteryl hemisuccinate with either an antifungal compound or a peptide. These compositions have various applications in vivo.

Compositions containing tris salt of cholesterol hemisuccinate and

A pharmacological agent-lipid solution preparation comprising a lipophilic pharmacological agent, a desalted charged lipid and an aqueous-miscible lipid solvent such that upon introduction into an aqueous medium a suspension of lipid aggregates associated with the pharmacological agent are formed, and methods of manufacture and use.

Pharmacological agent-lipid solution preparation

The present invention relates to novel liposomes and liposome-like structures (vesicles) comprising an amount of a derivatized sterol either alone or in combination with additional liposome-forming lipids. Sterols such as cholesterol or other lipids, to which numerous charged or neutral groups are attached, may be used to prepare liposomes and liposome-like structures such as micelles, reverse micelles and hexagonal phases, suspensions of multilamellar vesicles or small unilamellar vesicles. The novel liposomes of the present invention may be prepared with or without the use of organic solvents. These vesicles may entrap compounds varying in polarity and solubility in water and other solvents. The vesicles of the present invention may function as vaccines after entrapment or association of an immunogen, as adjuvants, either alone or in combination with additional adjuvants, including, for example, Freund's adjuvant (and other oil emulsions), Bortedella Pertussis, aluminum salts and other metal salts and Mycobacterial products (including muramyldipeptides), among others. The present invention relates to novel liposomes and liposome-like structures (vesicles) comprising an amount of a derivatized sterol either alone or in combination with additional liposome-forming lipids.

Steroidal liposomes exhibiting enhanced stability

A process for the separation and purification of individual phospholipids, especially phosphatidylcholine or lecithin and phosphatidylethanolaine, from mixtures containing members of the sub-class of phosphatides, incorporating methods of solvent extraction appropriate to the scale of the sample and utilizing an acetonitrile, acetonitrile-hydrocarbon, or acetonitrile-fluorocarbon solvent, which exhibit differential solubility properties towards the individual phospholipids.

Process for purification of phospholipids

Preparations of drugs in admixture with certain ligands are described which, when administered to animals or humans, are less toxic than conventional drug preparations. Although the toxicity of the drug-ligand preparations described is greatly reduced, the drug retains pharmacological activity.

Drug preparations of reduced toxicity

Alpha tocopherol-based vesicles

Steroidal liposomes comprising a bioactive agent and method for their administration are disclosed, the bilayers of said steroidal liposomes comprising a salt form of a carboxylic acid derivative of a sterol, a salt form of a polycarboxylic acid derivative of a sterol, a salt form of a hydroxy carboxylic acid derivative of a sterol, a salt form of an amino acid derivative of a sterol or a salt form of a poly (amino acid) derivative of a sterol; or a salt form of an organic acid derivative of cholesterol, a vitamin D, a phytosterol, or a steroidal hormone.

Growing community of inventors

Hamilton, NJ, United States of America

Paul A Tremblay