Emulsion and micellar formulations for the delivery of biologically active substances to cells
AssigneeUniversity of Pittsburgh
InventorsDexi Liu, Feng Liu, Jing-Ping Yang, Leaf Huang
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Abstract
New emulsion and micelle formulations are described as are complexes of these formulations with biologically active substances. The novel formulations are different from cationic lipid vectors such as cationic liposomes in that the complexes formed between biologically active substances and the emulsion and micellar formulations of this invention are physically stable and their transfection activity is resistant to the presence of serum. These novel formulations are disclosed to be useful in areas such as gene therapy or vaccine delivery.
Claims24
A micellar formulation consisting essentially of lipid components, a nucleic acid and an aqueous carrier, wherein the lipid components comprise a cationic amphiphile component, and a nonionic surfactant component,
- wherein the nonionic surfactant component is a synthetic detergent selected from the group consisting of a sorbitan fatty acid ester, a sorbitan polyoxyethylene fatty acid ester, a Pluronic surfactant and an octoxynol surfactant, and
- wherein the cationic amphiphile component is present in an amount from about 30 to about 90 weight % of the total lipid components and the nonionic surfactant component is present in an amount from about 70 to about 10 weight % of the total lipid components, and
- wherein the micellar formulation is suitable for administration to a human.
A micellar formulation, wherein the formulation is made by a process comprising the steps of:
- (a) combining an organic solvent with a cationic amphiphile component and a nonionic surfactant component, wherein the nonionic surfactant component is a synthetic detergent selected from the group consisting of a sorbitan fatty acid ester, a sorbitan polyoxyethylene fatty acid ester, a Pluronic surfactant and an octoxynol surfactant;
- (b) removing the organic solvent to leave a lipid film;
- (c) suspending the lipid film in an aqueous carrier to form a first micellar formulation;
- and
- (d) combining said first micellar formulation with a nucleic acid, thereby forming a second micellar formulation consisting essentially of lipid components, a nucleic acid and an aqueous carrier, wherein the lipid components comprise a cationic amphiphile component, and a nonionic surfactant component, wherein the cationic amphiphile component is present in an amount from about 30 to about 90 weight % of the total lipid components and the nonionic surfactant component is present in an amount from about 70 to about 10 weight % of the total lipid components, and wherein the second micellar formulation is suitable for administration to a human.
A micellar formulation comprising lipid components, a nucleic acid and an aqueous carrier, wherein the lipid components comprise a cationic amphiphile component, and a nonionic surfactant component,
- wherein the nonionic surfactant component is a synthetic octoxynol surfactant, and
- wherein the micellar formulation is suitable for administration to a human.
Dependencies are inferred from the claim text.