Non-vesicular cationic lipid formulations

1 - 22 . (canceled)

23 . A non-vesicular preparation comprising at least one cationic amphiphile in a concentration of about 10 mM to about 600 mM with a mean chain length from C12 to C24, optionally at least one further amphiphile of up to about 60 mol % based on the total amphiphile concentration and optionally at least one stabilizing agent in a concentration of about 10 mM to about 600 mM in an aqueous phase, wherein said preparation is characterized by being transparent, isotropic and substantially homogeneous.

24 . The preparation of claim 23 , comprising at least one cationic amphiphile in a concentration of about 25 mM to about 500 mM, preferably in a concentration of about about 100 mM to about 400 mM and most preferably in a concentration of about 200 mM to about 300 mM.

25 . The preparation of claim 23 , comprising a stabilizing agent in a concentration of about 100 mM to about 500 mM, preferably in a concentration of about about 200 mM to about 400 mM.

26 . The preparation of claim 23 , wherein said cationic amphiphile is selected from lipids, lysolipids, pegylated lipids having a positive net charge.

27 . The preparation of claim 26 , wherein said cationic amphiphile is selected from cationic lipids with at least one tertiary amino or quaternary ammonium group such as N-[1-(2,3-diacyloxy)propyl]-N,N-dimethylamine or N-[1-(2,3-diacyloxy)propyl]-N,N,N-trimethyl ammonium.

28 . The preparation of claim 23 , wherein said further amphiphile has a negative or a neutral net charge.

29 . The preparation of claim 23 , wherein said further amphiphile is selected from sterols or lipids such as cholesterol, phospholipids, lysolipids, lysophospholipids, sphingolipids or pegylated lipids with a negative or neutral net change.

30 . The preparation of claim 27 , wherein the neutral amphiphile is diacylphosphatidylcholine.

31 . The preparation of claim 23 , wherein said stabilizing agent is selected from a sugar or an alcohol or a combination thereof such as trehalose, maltose, sucrose, glucose, lactose, dextran, mannitol or sorbitol.

32 . The preparation of claim 31 , wherein said stabilizing agent is trehalose or glucose.

33 . The preparation of claim 23 , further comprising an active compound, wherein said active compound may be hydrophilic, hydrophobic or amphipathic.

34 . The preparation of claim 33 , wherein said compound is a therapeutic agent, preferably camptothecin or a derivative thereof, a taxane or an other microtubuli interacting agent such as an epothilone, discodermolide, laulimalide, isolaulimalide, eleutherobin, colchicine and/or a derivative thereof, a vinca alkaloid such as vinorelbine, a platinum complex such as oxaliplatin, an anthracycline such as doxorubicin or a statin (e.g., lovastatin) and more preferably camptothecin or a derivative thereof in its carboxylate form.

35 . The preparation of claim 34 , wherein said therapeutic agent is in the range of about 0.1 mol % to about 20 mol %, preferably in the range of about 1 mol % to about 15 mol % and more preferably in the range of about 3 mol % to about 10 mol % based on the total amphiphile concentration.

36 . The preparation of claim 33 , wherein said compound is a diagnostic agent, preferably an imaging agent.

37 . The preparation of claim 36 , wherein said diagnostic agent is in the range of about 0.1 mol % to about 50 mol %, preferably in the range of about 10 mol % to about 50 mol % and more preferably in the range of about 30 mol % to about 50 mol % based on the total amphiphile concentration.

38 . A method of producing a liposome suspension comprising using a preparation of claim 23 to form a liposome suspension.

39 . A method of producing a liposome suspension from the preparation of claim 23 by diluting said preparation with an aqueous solution.

40 . A Pharmaceutical composition comprising the preparation of claim 23 , optionally together with a pharmaceutically acceptable carrier, diluent and/or adjuvant

41 . A method of preparing a medicament or a diagnostic formulation comprising using a preparation of claim 23 to produce a medicament or diagnostic formulation.

42 . A method of treating angiogenesis associated condition such as cancer, chronic or acute inflammatory diseases, rheumatoid arthritis, dermatitis, psoriasis or wound healing comprising administering a pharmaceutical composition of claim 40 .

43 . A method of producing the non-vesicular preparation of claim 23 , comprising:

(a) providing

i) said cationic amphiphile, optionally said further amphiphile, optionally said stabilizing agent, optionally said active compound, and

ii) an aqueous phase; and

(b) dispersing the components of i) in said aqueous phase of ii).

44 . The method of claim 43 , comprising:

(a) providing

i) said cationic amphiphile, optionally said further amphiphile, optionally said stabilizing agent, and

ii) an aqueous solution;

(b) dispersing the components of i) in said aqueous phase of ii); and

(c) adding an active agent to the dispersion of step (b).

45 . The method of claim 43 , wherein step (b) comprises a single phase evaporation or high pressure homogenisation method.

46 . A method of producing the non-vesicular preparation of claim 23 , comprising:

a) providing said cationic amphiphile, optionally said further amphiphile, optionally said stabilizing agent, optionally said active compound and an aqueous phase; and

b) subjecting the components of step a) to conditions so that an isotropic, transparent and substantially homogenous preparation is formed,

wherein step b) comprises a single phase evaporation or high pressure homogenisation method.