Preparation of liposomes with peg-bound phospholipid on surface
First Claim
1. A process for the preparation of a liposome comprising PEG-bound phospholipid on the surface thereof, wherein said PEG-bound phospholipid extends outwardly, and does not substantially extend inwardly from the surface of said liposome, said process comprising preparing a liposome and adding PEG-bound phospholipid to said liposome thereby fixing the PEG-bound phospholipid on the surface of said liposome.
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Abstract
Agents for inhibiting adsorption of proteins on the liposome surface and liposomes which are agglutination-free by binding said inhibiting agent on the surface are disclosed. The above-mentioned inhibiting agents comprise a hydrophobic moiety and a hydrophilic macromolecular chain moiety. Adsorption of plasma proteins on the liposomes is inhibited due to the hydrophilic moiety exposed on the liposome surface with a result that agglutination of the liposomes in plasma is prevented. Therefore, there is no danger of embolism in blood vessels inhibiting blood flow when the liposomes are introduced into the living body. Accordingly, the liposomes are especially highly useful as artificial erythrocytes for which a large dose of liposomes is needed for administration.
Moreover, when liposomes are introduced into the living body, antibody protein (immunoglobulin) to the liposome which is an antigen will be adsorbed on the liposome to produce foreign body recognition in the phagocytes (macro-phage) with a result that the liposome will be included in the macrophage and disappear within a short period of time. Thus, inhibition of the protein adsorption on liposome can delay disappearance of the liposome in plasma.
In addition, a method for preparing the above-described liposomes is disclosed.
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Citations
18 Claims
- 1. A process for the preparation of a liposome comprising PEG-bound phospholipid on the surface thereof, wherein said PEG-bound phospholipid extends outwardly, and does not substantially extend inwardly from the surface of said liposome, said process comprising preparing a liposome and adding PEG-bound phospholipid to said liposome thereby fixing the PEG-bound phospholipid on the surface of said liposome.
- 10. A process for the preparation of a liposome comprising PEG-bound phospholipid on the surface thereof, wherein said PEG-bound phospholipid extends outwardly and does not substantially extend inwardly from the surface of said liposome, said process comprising preparing a liposome containing a phospholipid with a reaction-active functional group and adding PEG which is activated at one end to said liposome thereby allowing the PEG to couple with the phospholipid of said liposome.
Specification