Entrapment of water-insoluble compound in alpha tocopherol-based vesicles
AssigneeThe Liposome Company, Inc.
InventorsAndrew S. Janoff, Lois E. Bolcsak, Alan L. Weiner, Paul A. Tremblay, Michael V. W. Bergamini, Robert L. Suddith
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Abstract
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.
Claims22
A method for the treatment of a water-insoluble compound in alpha-tocopherol vesicles, comprising
- (a) dissolving the water-insoluble compound in an organic solvent;
- (b) removing the organic solvent, leaving a dried preparation comprising the water-insoluble compound;
- and
- (c) adding to the dried preparation an aqueous suspension of alpha-tocopherol vesicles prepared by adding to an aqueous phase a salt form of an organic acid derivative of alpha-tocopherol capable of forming closed bilayers in an amount sufficient to form completely closed vesicles, and agitating the mixture until a suspension of vesicles is formed.
A method for the entrapment of a water-insoluble compound in alpha-tocopherol vesicles, comprising
- (a) co-solubilizing an organic solvent the water-insoluble compound and a salt form of an organic acid derivative of alpha tocopherol capable of forming bilayers in an aqueous phase;
- (b) evaporating the organic solvent, leaving a dried preparation comprising the compound and the salt form of an organic acid derivative of alpha tocopherol;
- and
- (c) adding an aqueous phase to the dried preparation and agitating to form a suspension of completely closed vesicles.
Dependencies are inferred from the claim text.