Self forming, thermodynamically stable liposomes and their applications
A lipid composition forms liposomes spontaneously upon mixing with an aqueous solution. The lipid composition includes diacylglycerol-PEG compounds. Such lipid compositions are useful for forming liposomes, which in turn are useful for a variety of purposes, including the delivery of therapeutic agents.
1. A composition for use in preparing a liposomal formulation of a therapeutic agent, the composition comprising:
one or more lipids where the total lipids have a P a between about 0.84 and 0.88 and a P v between about 0.88 and 0.93,
where P a is the packing parameter with respect to surface and P v is the packing parameter with respect to volume,
where one or more of the lipids is a diacylglycerol-PEG having a melting point below about 40 degrees C. and also having acyl chains greater than 14 carbons in length, and the therapeutic agent.
2. The composition of claim 1 , where the PEG chain of the diacylglycerol-PEG has a molecular weight between about 300 Daltons and 5000 Daltons.
3. The composition of claim 1 , where the diacylglycerol-PEG comprises dioleolylglycerol-PEG-12.
4. The composition of claim 1 , where the therapeutic compound is selected from the group consisting of proteins, peptides, nucleic acids, agents for treating neoplasms, agents for treating inflammation, agents for treating infections, agents for treating gasterointestinal diseases, agents for treating immunological diseases, agents for treating skin diseases eye diseases, agents uses in diagnosing disease, nutrients, agents for treating blood diseases, agents for treating metabolic diseases, agents for treating cardiovascular diseases, agents for treating renal diseases, agents for treating genitourinary diseases, agents for treating respiratory diseases, and agents for treating central nervous system diseases.
5. The composition of claim 1 , where the composition is provided in a sealed container containing an inert gas.