Solid fat nanoemulsions
AssigneePharmos Corporation
InventorsShimon Amselem, Doron Friedman
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Abstract
The present invention provides pharmaceutical compositions comprising nanoemulsions of particles comprising a lipid core which is in a solid or liquid crystalline phase at 25.degree. C., stabilized by at least one phospholipid envelope, for the parenteral, oral, intranasal, rectal, or topical delivery of both fat-soluble and water-soluble drugs. Particles have a mean diameter in the range of 10 to 250 nm. A wide variety of drugs and oxygen transporting perfluorocarbons may be encapsulated in the particles. In addition to drug delivery vehicles, the invention provides oxygen transporting blood substitutes, and nanoemulsions for extracorporeal maintenance of tissues prior to transplantation.
Claims39
A nanoemulsion comprising a plurality of noncellular lipid particles having a mean diameter of about 10 to 250 nm in a pharmaceutically acceptable carrier solution, wherein each lipid particle has a core of a lipid which is in a solid phase at a temperature of at least about 25.degree. C., said lipid core being surrounded by at least one phospholipid bilayer which has two phospholipid layers separated by an aqueous compartment.
A composition comprising dehydrated lipid particles each having a lipid core which is in a solid phase at a temperature of about 25.degree. C. and which is surrounded by at least one phospholipid bilayer, wherein, upon rehydration, a nanoemulsion is formed with said lipid particles having a mean diameter of about 10 to 250 nm and said bilayer comprising two phospholipid layers separated by an aqueous compartment.
A method for making a nanoemulsion for administration of a drug, comprising the steps of:
- preparing a mixture comprising phospholipid and triglyceride in the weight ratio range of about 0.5:1 to 1.5:1 wherein said triglyceride has a solid to liquid phase transition temperature of greater than 25.degree. C.;
- suspending said mixture in a aqueous solution at a temperature below the sold to liquid transition temperature of the triglyceride;
- and
- reducing the size of the suspension to yield a nanoemulsion of lipid particles having a mean particle diameter of between about 10 nm and 250 nm.
A method for delivery of a drug to an animal comprising administration to said animal of a nanoemulsion comprising a plurality of noncellular lipid particles having a mean diameter of about 50 to 250 nm, wherein each said lipid particle comprises a lipid core composed of lipid which is in a solid phase at at least about 25.degree. C., and is surrounded by at least one phospholipid bilayer containing at least two phospholipid layers separated by a aqueous compartment, and wherein said lipid particle contains a drug.
Dependencies are inferred from the claim text.