Enhanced delivery of sphingolipids

• US 20070031480A1
• Filed: 03/08/2004
• Published: 02/08/2007
• Est. Priority Date: 03/07/2003
• Status: Abandoned Application

• Current Assignee: Celator Pharmaceuticals Inc.
• Original Assignee: Celator Pharmaceuticals Inc.
• Inventors: Mayer, Lawrence, Bally, Marcel, Shabbits, Jennifer
• Application Number:
  US10/548,371
• Publication Number:
  US 20070031480A1
• Time in Patent Office: Days
• US Class Current: 424/450
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/685 one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
• CPC Class Codes: A61K 31/739 Lipopolysaccharides
• CPC Class Codes: A61K 9/1272 with substantial amounts of non-phosphatidyl, i.e. non-acylglycerophosphate, surfactants as bilayer-forming substances, e.g. cationic lipids with cholesterol as the only non-phosphatidyl surfactant A61K9/127; lipids as modifying agent A61K47/543
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

Compositions which comprise delivery vehicles having stably associated therewith at least one organic acid derivative of a sterol are useful in achieving enhanced cellular delivery of physiologically relevant sphingolipids when the compositions are administered.

Claims

1. A composition which comprises delivery vehicles, said delivery vehicles having stably associated therewith at least one acid-derivatized sterol and at least one sphingolipid.

2. The composition of claim 1 wherein said acid-derivatized sterol is an organic acid derivative of a sterol.

3. The composition of claim 2 wherein said sterol is cholesterol.

4. The composition of claim 3 wherein said acid-derivatized sterol is cholesteryl hemisuccinate.

5. The composition of claim 1 wherein said sphingolipid is hydrophobic.

6. The composition of claim 1 wherein said sphingolipid contains at least 6 carbon atoms in at least one acyl chain.

7. The composition of claim 1 wherein said sphingolipid is a sphingosine or a derivative thereof.

8. The composition of claim 7 wherein said sphingolipid is a sphingosine derivative that inhibits ceramide metabolism.

9. The composition of claim 7 wherein said sphingolipid is a ceramide or a derivative thereof.

10. The composition of claim 9 wherein said sphingolipid is a ceramide derivative that inhibits ceramide metabolism.

11. A method to deliver an effective amount of at least one sphingolipid into cells which method comprises contacting said cells with the composition of claim 1.

13. The composition of claim 1 which further comprises at least one anti-cancer agent.

14. A method to treat cancer in a subject, which method comprises administering to a subject in need of such treatment an effective amount of the composition of claim 1.

15. A method to treat cancer in a subject, which method comprises administering to a subject in need of such treatment an effective amount of the composition of claim 13.

12. A method to prepare a composition which comprises at least one hydrophobic sphingolipid, which method comprises incorporating said sphingolipid into delivery vehicles wherein said delivery vehicles have stably associated therewith at least one acid-derivatized sterol.