The Liposome Company, Inc.

Ortho Pharmaceutical Corporation

Johnson Matthey Inc.

Robert L Suddith

Paul A Tremblay

Michelle L Tomsho

Andrew S Janoff

Robert P Lenk

Robert J Klimchak

Alan L Weiner

Lois E Bolcsak

John J Kearns

Michael V Bergamini

Marc J Ostro

Sharma R Minchey

Scott K Larsen

Michael Bornstein

Howard F Solomon

Diane C Corbo

N Adeyinka Williams

Mary Jean Link

A lyophilized imaging agent formulation and methods for making same are disclosed, such formulations comprise a targeting molecule such as antibody or chemotactic peptide, a linker such as diethylenetriaminepentaacetic acid (DTPA) or succinimidyl 6-hydrazinium nicotinate hydrochloride (SHNH), drying protectant such as mannitol, maltose or tricine, and excipient such as polysorbate 80, in citrate buffer. The formulations of the invention are lyophilized and may be stored stably for extended periods of time. Following reconstitution with diluent, the formulations are administered to a subject for scintigraphic imaging or therapeutic use. Also contemplated is a kit comprising a two-vial system wherein a first vial comprises a lyophilized formulation of imaging agent in the form of a lyophilized cake, and a second vial comprises a pharmaceutically acceptable carrier or diluent.

Lyophilized imaging agent formulation comprising a chemotactic peptide

This invention provides a multilamellar liposome containing an arachidonic acid metabolite, two or more lipid-containing bilayers and two or more aqueous compartments containing a release-inhibiting buffer. Preferred arachidonic acid metabolites are the prostaglandins, particularly PGE.sub.1. The liposomal formulations can be used to treat animals, particularly humans, for diseases, disorders or conditions which can be ameliorated by prostaglandins, e.g., disorders characterized by cellular activation and adhesion, inflammation and/or toxemia.

Therapeutic use of multilamellar liposomal prostaglandin formulations

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 method of extruding liposomes from liposomal material comprising extruding the liposomal material through a frit, and apparatus for extrusion.

Liposome continuous size reduction method and apparatus

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

A liposome composition and methods for making same are disclosed, such compositions comprise an arachidonic acid metabolite such as a prostaglandin, preferably prostaglandin E.sub.1, a lipid, and a drying protectant such as a saccharide. The liposomes may be loaded with prostaglandin passively, or using a transmembrane concentration gradient, preferably using a transmembrane pH gradient. Using this transmembrane loading technique, trapping efficiencies of 50% to 100% are achieved, and the release rate of the prostaglandin from the liposomes is reduced. The liposome size is maintained after lyophilization and reconstitution.

Prostaglandin-lipid formulations

Composition using salt form of organic acid derivative of

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Robbinsville, NJ, United States of America

Robert L Suddith