The Liposome Company, Inc.

Lois E Bolcsak

Andrew S Janoff

Alan L Weiner

Paul A Tremblay

Mircea C Popescu

Michael V Bergamini

Christine E Swenson

Lawrence T Boni

Robert L Suddith

Jo Ann Jedrusiak

Pieter Rutter Cullis

Marcel B Bally

Lawrence D Mayer

Robert P Lenk

Sharma R Minchey

Steven J Weiss

Paul S Tremblay

Andrew Stuart Janoff

Alan Lee Weiner

Mircea Constantine Popescu

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

Aminoglycosides, analogs and derivatives thereof, in the form of phosphate salts are described as well as the process for making and utilizing same. Aminoglycoside phosphate liposomes and nonguanadino aminoglycoside phosphate liposomes, their preparation and use, are particularly described.

Liposomes comprising aminoglycoside phosphates and methods of production

A method for making a pharmaceutical composition is described. The composition is comprised of an organic acid derivative of alpha tocopherol, and may additionally comprise other lipids. The composition may be in the form of liposomes, and as such are associated with or entrap a bioactive agent. Particularly suited for such systems are drugs stable at acidic pH, for example drugs having imidazole groups, such as pilocarpine. The composition requires a stabilizer to maintain the bilayer phase of the organic acid derivative of alpha tocopherol in a low pH environment. Such a stabilizer is for example a detergent. Upon in vivo administration of the system and concomitant increase of pH, viscosity of the preparation increases.

Tocopherol-based pharmaceutical systems

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

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

Alpha tocopherol-based vesicles

Composition using salt form of organic acid derivative of

Methods and compositions are described for the preparation of 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. The method is rapid, efficient, and does not require the use of organic solvents. The sterol hemisuccinate 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.

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Lawrenceville, NJ, United States of America

Lois E Bolcsak