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Lipid formulations for nucleic acid delivery,Lipid encapsulated interfering RNA,Cationic lipids and methods of use,Modified siRNA molecules and uses thereof,Nucleic Acid-Lipopolymer Compositions

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Lipid formulations for nucleic acid delivery

ActiveUS8058069B2Organic active ingredientsSpecial deliveryLipid formationLipid particle

The present invention provides novel, stable lipid particles comprising one or more active agents or therapeutic agents, methods of making the lipid particles, and methods of delivering and / or administering the lipid particles. More particularly, the present invention provides stable nucleic acid-lipid particles (SNALP) comprising a nucleic acid (such as one or more interfering RNA), methods of making the SNALP, and methods of delivering and / or administering the SNALP.

Lipid formulations for nucleic acid delivery

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Lipid encapsulated interfering RNA

InactiveUS20060008910A1Inhibit aggregationReduce overexpressionBiocideOrganic active ingredientsLipid formationLipid particle

The present invention provides lipid-based formulations for delivering, e.g., introducing, nucleic acid-lipid particles comprising an interference RNA molecule to a cell, and assays for optimizing the delivery efficiency of such lipid-based formulations.

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Cationic lipids and methods of use

ActiveUS20060083780A1Increase flexibilityImprove propertiesUltrasonic/sonic/infrasonic diagnosticsNervous disorderLipid formationLipid particle

The present invention provides compositions comprising cationic lipids, liposomes and nucleic acid-lipid particles comprising the cationic lipids, and methods of using such compositions, liposomes, and nucleic acid-lipid particles.

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Modified siRNA molecules and uses thereof

ActiveUS20070135372A1Decrease immunostimulatory propertyImmunostimulatory activity of siRNA can be abolishedOrganic active ingredientsSugar derivativesLipid formationLipid particle

The present invention provides chemically modified siRNA molecules and methods of using such siRNA molecules to silence target gene expression. Advantageously, the modified siRNA of the present invention is less immunostimulatory than its corresponding unmodified siRNA sequence and retains RNAi activity against the target sequence. The present invention also provides nucleic acid-lipid particles comprising a modified siRNA, a cationic lipid, and a non-cationic lipid, which can further comprise a conjugated lipid that inhibits aggregation of particles. The present invention further provides methods of silencing gene expression by administering a modified siRNA to a mammalian subject. Methods for identifying and / or modifying an siRNA having immunostimulatory properties are also provided.

Modified siRNA molecules and uses thereof

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Nucleic Acid-Lipopolymer Compositions

InactiveUS20090042829A1Increase efficiency and dosing flexibilityEfficiently be lyophilizedSpecial deliveryPeptide/protein ingredientsCholesterolFiller Excipient

Compositions, methods, and applications that increase the efficiency of nucleic acid transfection are provided. In one aspect, a pharmaceutical composition may include at least about 0.5 mg / ml concentration of a nucleic acid condensed with a cationic lipopolymer suspended in an isotonic solution, where the cationic lipopolymer includes a cationic polymer backbone having cholesterol and polyethylene glycol covalently attached thereto, and wherein the molar ratio of cholesterol to cationic polymer backbone is within a range of from about 0.1 to about 10, and the molar ratio of polyethylene glycol to cationic polymer backbone is within a range of from about 0.1 to about 10. The composition further may include a filler excipient.

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Owner:CLSN LAB

Lipid encapsulated interfering RNA

ActiveUS20060240093A1Inhibit aggregationMetabolism disorderMicroencapsulation basedLipid formationLipid particle

The present invention provides compositions and methods for silencing gene expression by delivering nucleic acid-lipid particles comprising a siRNA molecule to a cell.

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Lipid encapsulated interfering RNA

InactiveUS20050064595A1Inhibit aggregationMetabolism disorderMicroencapsulation basedLipid formationLipid particle

The present invention provides compositions and methods for silencing gene expression by delivering nucleic acid-lipid particles comprising a siRNA molecule to a cell.

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Owner:PROTIVA BIOTHERAPEUTICS

Cationic lipids and methods for the delivery of therapeutic agents

InactiveUS8569256B2Organic active ingredientsSpecial deliveryLipid particleProtein target

The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

Cationic lipids and methods for the delivery of therapeutic agents

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Owner:PROTIVA BIOTHERAPEUTICS

Systems and methods for manufacturing liposomes

ActiveUS20070042031A1Fast preparationOrganic active ingredientsMicroencapsulation basedLipid formationBuffer solution

The present invention provides apparatus and processes for producing liposomes. By providing a buffer solution in a first reservoir, and a lipid solution in a second reservoir, continuously diluting the lipid solution with the buffer solution in a mixing chamber produces a liposome. A therapeutic agent, such as nucleic acid, is included in one of the buffer solution or the lipid solution. Upon mixing a liposome encapsulating the therapeutic product is substantially instantaneously formed. Thereafter the liposome solution formed is immediately diluted with buffer solution to enhance homogeneity and maintain small particle size.

Systems and methods for manufacturing liposomes

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Lipid formulations for nucleic acid delivery

ActiveUS8283333B2Improve effectivenessHigh activityOrganic active ingredientsSugar derivativesLipid particleActive agent

The present invention provides novel, serum-stable lipid particles comprising one or more active agents or therapeutic agents, methods of making the lipid particles, and methods of delivering and / or administering the lipid particles. More particularly, the present invention provides serum-stable nucleic acid-lipid particles (SNALP) comprising a nucleic acid (e.g., one or more interfering RNA molecules), methods of making the SNALP, and methods of delivering and / or administering the SNALP (e.g., for the treatment of cancer). In particular embodiments, the present invention provides tumor-directed lipid particles that preferentially target solid tumors. The tumor-directed formulations of the present invention are capable of preferentially delivering a payload such as a nucleic acid to cells of solid tumors compared to non-cancerous cells.

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Lipid encapsulated interfering RNA

InactiveUS7799565B2Ultrasonic/sonic/infrasonic diagnosticsBiocideLipid formationAssay

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Cationic lipids and methods of use

ActiveUS7745651B2Increase flexibilityGood fluidityUltrasonic/sonic/infrasonic diagnosticsBiocideLipid particleLiposome

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Polyethyleneglycol-modified lipid compounds and uses thereof

ActiveUS7803397B2Improve stabilityImprove propertiesNervous disorderOrganic chemistryPolyethylene glycolLiposome

The present invention provides compositions comprising polytheylyene-dialkyloxypropyl conjugates (PEG-DAA), liposomes, SNALP, and SPLP comprising such compositions, and methods of using such compositions, liposomes, SNALP, and SPLP.

Polyethyleneglycol-modified lipid compounds and uses thereof

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Biodegradable poly(β-amino esters) and uses thereof

InactiveUS6998115B2Antibacterial agentsPowder deliveryAmino estersNucleotide

Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer / polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

Biodegradable poly(β-amino esters) and uses thereof

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Owner:MASSACHUSETTS INST OF TECH

Cationic lipids and methods for the delivery of therapeutic agents

InactiveUS20120202871A1Cyclic stabilitySize requirementBiocideOrganic active ingredientsLipid formationLipid particle

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Owner:PROTIVA BIOTHERAPEUTICS

Modified nucleoside, nucleotide, and nucleic acid compositions

InactiveUS20130156849A1Therapeutically effectiveRaise hemoglobinOrganic active ingredientsPowder deliveryProtein precursorNucleotide

The present disclosure provides, inter alia, formulation compositions comprising modified nucleic acid molecules which may encode a protein, a protein precursor, or a partially or fully processed form of the protein or a protein precursor. The formulation composition may further include a modified nucleic acid molecule and a delivery agent. The present invention further provides nucleic acids useful for encoding polypeptides capable of modulating a cell's function and / or activity.

Modified nucleoside, nucleotide, and nucleic acid compositions

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Owner:MODERNA THERAPEUTICS INC

Lipid-nucleic acid particles prepared via a hydrophobic lipid-nucleic acid complex intermediate and use for gene transfer

InactiveUS7422902B1BiocideMicroencapsulation basedParticulatesLipid formation

Novel lipid-nucleic acid particulate complexes which are useful for in vitro or in vivo gene transfer are described. The particles can be formed using either detergent dialysis methods or methods which utilize organic solvents. Upon removal of a solubilizing component (i.e., detergent or an organic solvent) the lipid-nucleic acid complexes form particles wherein the nucleic acid is serum-stable and is protected from degradation. The particles thus formed have access to extravascular sites and target cell populations and are suitable for the therapeutic delivery of nucleic acids.

Lipid-nucleic acid particles prepared via a hydrophobic lipid-nucleic acid complex intermediate and use for gene transfer

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Owner:TEKMIRA PHARMA CORP +1

Polymeric micelles for drug delivery

ActiveUS20060240092A1BiocideNervous disorderPharmaceutical SubstancesPolymer chemistry

The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same.

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Owner:INTEZYNE TECH INC

Method of preventing aggregation of a lipid:nucleic acid complex

InactiveUS6858224B2Microencapsulation basedGenetic material ingredientsLipid formationPolyethylene glycol

Particle aggregation of lipid:nucleic acid complex particles is prevented by incorporating a non-cationic lipid into lipid:nucleic acid complex particles containing a cationic lipid and a nucleic acid polymer. The non-cationic lipid is a polyethylene glycol-based polymer.

Method of preventing aggregation of a lipid:nucleic acid complex

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Owner:TEKMIRA PHARMA CORP +1

Novel low molecular weight cationic lipids for oligonucleotide delivery

ActiveUS20130178541A1Good curative effectReduce liver toxicityBiocideMicroencapsulation basedTolerabilityNanoparticle

The instant invention provides for novel catiomc lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Novel low molecular weight cationic lipids for oligonucleotide delivery

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Owner:SIRNA THERAPEUTICS INC

Histidine copolymer and methods for using same

InactiveUS7163695B2Prolong half-life in vivoEnhanced transfectionPowder deliveryPeptide/protein ingredientsHistidine residueCopolymer

The invention provides a pharmaceutical agent delivery composition comprising: (i) a transport polymer comprising a linear or branched peptide having from about 10 to about 300 amino acid residues, having from about 5 to 100% histidine residues, and optionally having from 0 to about 95% non-histidine amino acid residues; (ii) at least one pharmaceutical agent; and optionally (iii) one or more intracellular delivery components in association with the transport polymer. The invention also provides methods for using such composition to deliver the pharmaceutical agent to the interior of cells.

Histidine copolymer and methods for using same

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Owner:MIXSON A JAMES

Nucleic acid-containing lipid particles and related methods

ActiveUS20120276209A1Avoid mixingPowder deliveryOrganic active ingredientsLipid formationLipid particle

Lipid particles containing a nucleic acid, devices and methods for making the lipid particles, and methods for using the lipid particles.

Nucleic acid-containing lipid particles and related methods

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Owner:THE UNIV OF BRITISH COLUMBIA

Novel lipid formulations for nucleic acid delivery

ActiveUS20100130588A1Organic active ingredientsSpecial deliveryLipid formationLipid particle

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Owner:ARBUTUS BIOPHARMA CORPORAT ION

Emulsions and methods of making nanocarriers

InactiveUS20110262491A1Powder deliveryOrganic active ingredientsEmulsionNanocarriers

This invention relates, in part, to methods of using emulsions for making synthetic nanocarriers and the synthetic nanocarriers formed by such methods.

Emulsions and methods of making nanocarriers

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Owner:SELECTA BIOSCI

Branched histidine copolymers and methods for using same

InactiveUS7070807B2Prolong half-life in vivoEnhanced transfectionPowder deliveryPeptide/protein ingredientsIn vivoLocal injection

The invention provides a branched transport polymer characterized as having at least 10 amino acids and a ratio of histidine to non-histidine amino acids greater than 1.5, said branched transport polymer comprising one or more backbones, one or more terminal branches, and optionally, one or more non-terminal branches. The branched transport polymer may be associated with a pharmaceutical agent to form a pharmaceutical agent delivery composition useful for in vivo therapies based on local injection.

Branched histidine copolymers and methods for using same

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Owner:MIXSON A JAMES

Self-assembling nanoparticle drug delivery system

InactiveUS20090226525A1High binding affinityHigh affinityPowder deliveryMicroencapsulation basedLipid formationMedicine

A self-assembling nanoparticle drug delivery system for the delivery of various bioactive agents including peptides, proteins, nucleic acids or synthetic chemical drugs is provided. The self-assembling nanoparticle drug delivery system described herein includes viral capsid proteins, such as Hepatitis B Virus core protein, encapsulating the bioactive agent, a lipid layer or lipid / cholesterol layer coat and targeting or facilitating molecules anchored in the lipid layer. A method for construction of the self-assembling nanoparticle drug delivery system is also provided.