Lipids, lipid complexes and use thereof
The present invention is related to uses of a composition comprising a pharmaceutically active component and a compound according to formula (I), wherein R 1 and R 2 are each and independently selected from the group comprising alkyl; n is any integer between 1 and 4; R 3 is an acyl selected from the group comprising lysyl, ornithyl, 2,4-diaminobutyryl, histidyl and an acyl moiety according to formula (II), wherein m is any integer from 1 to 3 and Y − is a pharmaceutically acceptable anion.
1. A composition comprising a carrier and a liposome comprising at least one helper lipid component selected from the group consisting of phospholipids and steroids and a compound according to formula (I),
wherein R 1 and R 2 are each and independently selected from the group comprising alkyl;
n is any integer between 1 and 4;
R 3 is an acyl selected from the group comprising lysyl, ornithyl, 2,4-diaminobutyryl, histidyl and an acyl moiety according to formula (II)
wherein m is any integer from 1 to 3 and
Y − is a pharmaceutically acceptable anion.
2. The composition according to claim 1 , wherein R 1 and R 2 are each and independently selected from the group comprising lauryl, myristyl, palmityl and oleyl.
3. The composition according to claim 1 , wherein R 1 is lauryl and R 2 is myristyl or R 1 is palmityl and R 2 is oleyl.
4. The composition according to claim 1 , wherein m is 1 or 2.
5. The composition according to claim 1 , wherein Y − is selected from the group consisting of halogenids, acetate and trifluoroacetate.
6. The composition according to claim 1 , wherein the compound is selected from the group consisting of:
7. The composition according to claim 1 , wherein the carrier is a pharmaceutically acceptable carrier.
8. The composition according to claim 1 , wherein the liposome is associated with a nucleic acid.
9. The composition according to claim 8 , wherein the nucleic acid is an oligonucleotide, polynucleotide or siRNA.
10. The composition according to claim 1 , wherein the helper lipid component is selected from the group comprising 1,2-diphytanoyl-sn-glycero-3-phosphoethanolamine and 1,2-dioleyl-sn-glycero-3-phosphoethanolamine.
11. The composition according to claim 10 , wherein the content of the helper lipid component is from about 20 mol % to about 80 mol % of the overall lipid content of the liposome.
12. The composition according to claim 1 , wherein said at least one helper lipid comprises a moiety which is selected from the group comprising a PEG moiety, a HEG moiety, a polyhydroxyethyl starch (polyHES) moiety and a polypropylene moiety.
13. The composition according to claim 12 , wherein the helper lipid comprising the PEG moiety is selected from the group comprising 1,2-distearoyl-sn-glycero-3-phosphoethanolamine, 1,2-dialkyl-sn-glycero-3-phosphoethanolamine; and Ceramide-PEG.
14. The composition according to claim 1 , said liposome comprising:
a) 50 mol % of β-arginyl-2,3-diamino propionic acid-N-palmityl-N-oleyl-amide trihydrochloride,
48 mol % of 1,2-diphytanoyl-sn-glycero-3-phosphoethanolamine; and
2 mol % 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-PEG2000; or
b) 50 mol % of β-L-arginyl-2,3-L-diamino propionic acid-N-palmityl-N-oleyl-amide trihydrocloride,
49 mol % 1,2-diphytanoyl-sn-glycero-3-phosphoethanolamine; and
1 mol % N(Carbonyl-methoxypolyethylenglycol-2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine.