Lipid-encapsulated polyanionic nucleic acid
First Claim
1. A nucleic acid-lipid particle, comprising a lipid layer surrounding and encapsulating a central region containing a polyanionic nucleic acid, wherein said lipid layer comprises (i) an amino lipid comprising an amino group having a pKa of from 4 to 11, and (ii) a polyethyleneglycol-diacylglycerol (PEG-DAG) conjugate.
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Abstract
Methods for the preparation of a lipid-nucleic acid composition are provided. According to the methods, a mixture of lipids containing a protonatable or deprotonatable lipid, for example an amino lipid and a lipid such as a PEG- or Polyamide oligomer-modified lipid is combined with a buffered aqueous solution of a charged therapeutic agent, for example polyanionic nucleic acids, to produce particles in which the therapeutic agent is encapsulated in a lipid vesicle. Surface charges on the lipid particles are at least partially neutralized to provide surface-neutralized lipid-encapsulated compositions of the therapeutic agents. The method permits the preparation of compositions with high ratios of therapeutic agent to lipid and with encapsulation efficiencies in excess of 50%.
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26 Claims
- 1. A nucleic acid-lipid particle, comprising a lipid layer surrounding and encapsulating a central region containing a polyanionic nucleic acid, wherein said lipid layer comprises (i) an amino lipid comprising an amino group having a pKa of from 4 to 11, and (ii) a polyethyleneglycol-diacylglycerol (PEG-DAG) conjugate.
Specification