Liposome Technology, Inc.

Sequus Pharmaceuticals, Inc.

Alza Corporation

Martin C Woodle

Francis J Martin

Samuel Zalipsky

Yechezkel Barenholz

Herve Bercovier

Carl T Redemann

Annie Yau-Young

Danilo D Lasic

Ramachandran Radhakrishnan

Shi Kun Huang

Jacqueline K Morano

Irma Ajm Bakker-Woudenberg

A liposome composition comprising small, surface-bound effector molecules is disclosed. The liposomes have a surface layer of hydrophilic polymer chains, for enhanced circulation time in the bloodstream. The effector molecules are attached to the distal ends of the polymer chains. In one embodiment, the effector is polymyxin B, for treatment of septic shock.

Enhanced circulation effector composition and method

Enhanced ciruclation effector composition and method

A method of treating a site of systemic infection which includes administering a therapeutic compound entrapped in liposomes. Also included is a liposomal composition and a method of preparing a liposomal composition for use in concentrating a therapeutic compound to an infected region via the bloodstream. The liposomes, which contain the agent in entrapped form, are composed of vesicle-forming lipids, a vesicle-forming lipid derivatized with hydrophilic biocompatible polymer, and have sizes in a selected size range between 0.07 and 0.2 microns. After parenteral administration, the liposomes are selectively taken up by the infected region within 24-48 hours, for release of entrapped compound into the infected region.

Method of treatment of infected tissues

A lipid-polymer conjugate for use in forming long-circulating liposomes is disclosed. The conjugate includes a vesicle-forming lipid having covalently attached to its polar head group, one of the polymers: polyvinylpyrrolidone, polyvinylmethylether, polyhydroxypropyl methacrylate, polyhydroxypropylmethacrylamide, polyhydroxyethyl acrylate, polymethacrylamide, polydimethylacrylamide, polymethyloxazoline, polyethyloxazoline, polyhydroxyethyloxazoline, polyhydroxypropyloxazoline, or polyaspartamide. A method for preparing liposomes containing the lipid-polymer conjugate is also disclosed.

Lipid-polymer conjugates and liposomes

A method of and composition for concentrating a therapeutic agent in an inflamed dermal region are disclosed. The composition, which is also used in the method, is a liposomal composition. The liposomes contain the therapeutic agent in entrapped form and are composed of vesicle-forming lipids including a vesicle-forming lipid derivatized with hydrophilic biocompatible polymer. After intravenous administration, the liposomes are taken up by the inflamed region within 24-48 hours, for site-specific release of entrapped compound into the inflamed region.

Method of treatment of inflamed tissues

A liposome composition for extended release of a therapeutic compound into the bloodstream. The liposomes are composed of vesicle-forming lipids and between 1-20 mole percent of a vesicle-forming lipid derivatized with hydrophilic polymer, have sizes in a selected size range between 0.1 and 0.4 microns, and contain the therapeutic compound in liposome-entrapped form. The dosage form of the composition contains at least about three times the dose of the compound required for intravenous injection in free form. Also disclosed in a method for extending to at least 24 hours the period in which an intravenously administered therapeutic compound is therapeutically active in the bloodstream, and novel liposomes compositions for practicing the method.

Microreservoir liposome composition and method

A liposome composition for localizing an anti-tumor compound to a solid tumor via the bloodstream. The liposomes, which contain the agent in entrapped form, are composed of vesicle-forming lipids and between 1-20 mole percent of a vesicle-forming lipid derivatized with hydrophilic biocompatible polymer, and have sizes in a selected size range between 0.07 and 0.12 microns. After intravenous administration, the liposomes are taken up by the tumor within 24-48 hours, for site-specific release of entrapped compound into the tumor. In one composition for use in treating a solid tumor, the compound is an anthracycline antibiotic drug which is entrapped in the liposomes at a concentration of greater than about 50 .mu.g agent/.mu.mole liposome lipid. The method results in regression of solid colon and breast carcinomas which are refractory to anthracycline antibiotic drugs administered in free form or entrapped in conventional liposomes.

Solid tumor treatment method and composition

A liposome composition which contains between 1-20 mole percent of an amphipathic lipid derivatized with a polyalkylether, as exemplified by phosphatidylethanolamine derivatized with polyethyleneglycol. The derivatized lipid enchances the circulation time of the liposomes severalfold, and this enhancement is achieved with either fluid or membrane-rigidifying liposome components. Also disclosed are methods for delivering a drug for slow release from the bloodstream, and for targeting a selected tissue or cells with liposomes, via the bloodstream.

Liposomes with enhanced circulation time

A suspension of heterogeneous size liposomes is passed through a polymer filter having a web-like construction providing a network of interconnected, tortuous-path capillary pores, and a membrane thickness of at least about 100 microns. The processed liposomes have a selected average size less than about 0.4 microns, and a narrow size distribution.

Growing community of inventors

Menlo Park, CA, United States of America

Martin C Woodle