Liposomes for in-vivo delivery
AssigneeTechnion Research & Development Foundation Limited
InventorsNahum Allon, Moshe Gavish
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Abstract
The present invention provides a liposome based composition wherein the liposome includes a peptide conjugated thereto via a peptide bond, wherein the peptide includes a spacer amino acid and a short Apolipoprotein E recognition sequence or a short Amyloid beta recognition sequence. This invention further provides a process for making the liposome and methods of utilizing the liposome based composition for therapeutic and diagnostic purposes.
Claims27
A composition comprising a liposome and a liposome-anchored blood-brain-barrier (BBB) recognition peptide covalently conjugated to said liposome, said covalently conjugated is conjugated via a peptide bond between a carboxyl end of a succinate group within said liposome lipid bilayer and an amino group of said peptide, wherein said BBB recognition peptide comprises the amino acid sequence AHRERMS (SEQ ID NO:
- 6) or ARERMS (SEQ ID NO:
- 4).
A process for the preparation of a liposome conjugated to a peptide comprising at least one spacer amino acid followed by an amino acid sequence selected from the group consisting of SEQ ID NOs:
- 3, 4, or 6, comprising the steps:
- (a) dissolving in ethanol or chloroform:
- (1) Cholesterol (Ch), 1,2-dioleoyl-5nglycero-3-phosphocholine (DOPC), and 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE);
- or (2) Cholesterol (Ch), 1,2-dioleoyl-5n-glycero-3-[phosphor-L-serine] (DOPS), and 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE);
- (b) adding to the mixture of step (a) a peptide comprising at least one spacer amino acid followed by an amino acid sequence selected from the group consisting of SEQ ID NOs:
- 3, 4, or 6 conjugated to either 1,2-dioleoyl-5n-glycero-3-succinate or 1,2-dioleoyl-5n-glycero-3-succinate at a concentration of 0.1-1 mol %;
- (c) removing said chloroform and obtaining a dried lipid film;
- and
- (d) hydrating said dried lipid film in an isotonic buffer;
- thereby obtaining a liposome conjugated to a peptide comprising at least one spacer amino acid followed by an amino acid sequence selected from the group consisting of SEQ ID NOs:
- 3, 4, or 6.
Dependencies are inferred from the claim text.