48 results about "Neutral lipid" patented technology

Provided herein are methods for treating a pulmonary infection in a patient in need thereof, for example, a nontuberculous mycobacterial pulmonary infection for at least one treatment cycle. The method comprises administering to the lungs of the patient a pharmaceutical composition comprising a liposomal complexed aminoglycoside comprising a lipid component comprising electrically neutral lipids and an aminoglycoside. Administration comprises aerosolizing the pharmaceutical composition to provide an aerosolized pharmaceutical composition comprising a mixture of free aminoglycoside and liposomal complexed aminoglycoside, and administering the aerosolized pharmaceutical composition via a nebulizer to the lungs of the patient. The methods provided herein result in a change from baseline on the semi-quantitative scale for mycobacterial culture for a treated patient, and / or NTM culture conversion to negative during or after the administration period.

Provided is a preparation method for an adiposome, comprising the following steps: S1) subjecting polar lipids and neutral lipids to intermittent ultrasonic emulsification in a buffer solution to obtain a crude emulsion; and S2) purifying the crude emulsion to obtain the adiposome. Compared with the prior art, the present invention uses an ultrasonic emulsification method to prepare the adiposome, so that the quality of the adiposome prepared in different batches is controllable, and the preparation of the adiposome can be efficiently completed. Moreover, high-energy mechanical vibration and ultrasonic cavitation effects of ultrasonic waves are utilized in the ultrasonic emulsification method to widen the selection of raw materials for adiposomes, so that the method can be used to not only prepare an adiposome with unsaturated fatty acid chain phospholipids and neutral lipids as raw materials, but also synthesize an adiposome with saturated fatty acid chain phospholipids, neutral lipids, or high-melting-point lipids as raw materials. In addition, the utilization of raw materials can be improved, and the scale of adiposome production can be expanded.

The invention discloses a lipid compound for delivering a therapeutic agent as well as a preparation method and application thereof. The invention relates to a lipid compound, which is a compound with a structural formula I or a pharmaceutically acceptable form thereof. The lipid compounds may be used in combination with other lipid components, such as neutral lipids, cholesterol, and polymer-bound lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes (e.g., vaccination), enriching the species of ionizable lipid compounds.

The present invention relates to lipid nanoparticle compositions. Provided herein are lipids that can be used in combination with other lipid components, such as neutral lipids, cholesterol, and polymer-conjugated lipids, to form lipid nanoparticles for the delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination.

The problem to be solved by the present invention is to provide cationic lipids for oligonucleotide delivery which can provide a high drug: lipid ratio, which protect the nucleic acid from degradation and clearance in serum, which are suitable for systemic delivery, which can result in intracellular delivery of the nucleic acid, and which are well tolerated, provide an adequate therapeutic index, and treatment of patients with an effective dose of the nucleic acid is not associated with significant toxicity and / or risk to the patient.SOLUTION: The present invention relates to cationic lipids having one or more biodegradable groups located in the lipid portion (e.g., hydrophobic chain) of the cationic lipid. These cationic lipids can be incorporated into lipid particles for the delivery of active agents such as nucleic acids. The present invention also relates to a lipid particle comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the invention and optionally a sterol. The lipid particles may further comprise a therapeutic agent, such as a nucleic acid.SELECTED DRAWING: None

The invention discloses a structure annotation method for analyzing positions sn-and C = C of lipid based on liquid chromatography-organic matter ion electron collision excitation mass spectrometry. According to the method, a proper amount of 0.1 mM sodium acetate is added during lipid redissolution, so that polar lipid and neutral lipid are analyzed at the same time through one-time sample introduction. Meanwhile, a method for automatically annotating the complex organic matter ion electron collision excitation mass spectrum is developed, and the method comprises the steps of (1) extracting mass spectrum information in original data, (2) identifying lipid subclasses, (3) matching lipid total composition, (4) pairing sn-position, (5) positioning C = C position, and (6) determining annotation level. For 34 lipid standard substances in serum, the annotation accuracy rates of the annotation method on sn-and C = C isomer levels are 100% and 82.3% respectively. A total of 1312 sn-isomers and 1033 C = C isomers are annotated from mixed plasma samples of healthy people and patients with mild cognitive impairment of Alzheimer's disease. In a word, the lipid fine structure analysis method developed by the invention has the characteristics of simple pretreatment, high coverage and efficient annotation of the lipid fine structure.

The invention relates to HIF-1alpha siRNA lipid nanoparticles and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The preparation method comprises the following steps: S1, dissolving ionizable lipid, neutral lipid, cholesterol and pegylated lipid in an organic solvent to obtain an oil phase; the method comprises the following steps: dissolving HIF-1alpha siRNA in a first buffer solution to obtain a water phase; s2, mixing the oil phase and the water phase by adopting a micro-fluidic technology, diluting with a second buffer solution, removing the organic solvent, and concentrating to obtain the HIF-1alpha siRNA lipid nanoparticles, the targeted delivery of the HIF-1alpha siRNA is realized, so that the HIF-1alpha siRNA is effectively delivered to the rheumatoid arthritis diseased region through the delivery system to play a therapeutic role.

The present disclosure provides a lipid compound, which can be used in combination with other lipid components, such as neutral lipids, cholesterol, and polymer-lipid conjugates, to form lipid nanoparticles for delivery of therapeutic agents (e.g. nucleic acid molecules) for therapeutic or prophylactic purposes, comprising vaccination. Also provided herein is a lipid nanoparticle composition comprising the lipid compound.

The present invention relates to a novel lipid compound and a lipid nanoparticle composition containing the same. More specifically, the lipid nanoparticle composition contains an ionizable lipid, a helper lipid, a PEG-lipid, and an additive, and contains a biocompatible vitamin-based novel lipid compound and a helper lipid containing a neutral lipid, which can mitigate changes in the delivery mechanism and side effects, and can improve protein expression efficiency.

Provided herein is a lipid nanoparticle comprising an encapsulated oligonucleotide molecule, wherein the oligonucleotide molecule is single-stranded or double-stranded and has a length of between 5 and 500 nucleotides; and 20 to 70 mol % of a neutral lipid content relative to total lipid present in the lipid nanoparticle, an ionizable lipid; a sterol; and optionally a hydrophilic polymer-lipid conjugate.

A neogambogic acid adiposome formulation, a preparation method therefor, and use thereof. The neogambogic acid adiposome formulation comprises a monomolecular phospholipid membrane, and neogambogic acid and neutral lipid which are wrapped in the monomolecular phospholipid membrane. The adiposome formulation has good bioavailability and safety, thereby improving the anti-tumor effect.

A lipid nanoparticle composition targeting to antigen-presenting cells (APCs), comprising: at least a therapeutic agent, at least a cationic or ionizable cationic lipid, at least a neutral lipid, at least a steroid or steroid analogue, at least a PEGylated lipid, and atleast a phosphatidylglycerol.

Provided are a docetaxel adiposome formulation, a preparation method therefor, and use thereof. The docetaxel adiposome formulation comprises a monomolecular phospholipid membrane and docetaxel and a neutral lipid that are wrapped in the monomolecular phospholipid membrane. Targeted modification is further carried out on the surface of the docetaxel adiposome. The adiposome formulation has good bioavailability and safety, and the anti-cancer effect of the formulation is significantly superior to that of a clinically used docetaxel injection.

Provided herein are lipid compounds, which can be used in combination with other lipid components, such as neutral lipids, cholesterol, and polymer-conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination. Also provided herein are lipid nanoparticle compositions comprising the lipid compounds.

A nucleic acid-loaded calcium-containing cationic lipid nanoparticle, comprising a cationic lipid, a neutral lipid, a PEGylated lipid, and cholesterol and / or a cholesterol ester. The cationic lipid nanoparticle can be used for preparing a gene-based drug for local injection into the body or a nucleic acid vaccine for local or systemic injection into the body.

The present disclosure provides a lipid nanoparticle, the lipid nanoparticle comprises a cationic lipid, a neutral lipid, a PEG lipid and an active pharmaceutical ingredient, the cationic lipid comprises DOTAP, and the active pharmaceutical ingredient comprises one or more of nucleoside, a nucleoside analogue or a compound with a phosphate group. The lipid nanoparticles are high in stability and bioavailability, and the effect of the lipid nanoparticles is better than that of a drug monomer.

The present invention provides lipid nanoparticles that encapsulate nucleic acid and have at least 30mol% of neutral lipid, sterol or its derivative, and targeting moiety fixed to lipid layer via lipophilic moiety.Furthermore, the method of using lipid nanoparticles for in vivo targeted delivery is also provided.Such lipid nanoparticles can show significantly improved delivery and targeting to extrahepatic tissues and / or organs.

Provided is a lipid nanoparticle comprising capped mRNA bearing one or more ribose modifications, and 20 to 70 mol % of a neutral lipid, an ionizable lipid; and a sterol and optionally a hydrophilic polymer-lipid conjugate, the lipid nanoparticles exhibiting at least a 10% increase in extrahepatic protein expression of the mRNA in vivo, as measured in one or more extrahepatic organs or tissues. In some examples, the mRNA comprises a 5' cap having an N7-methylated guanosine at a position 0, and a nucleoside at a position 1 linked to the N7-methylated guanosine by a 5' to 5' bridge, wherein the N7-methylated guanosine has a modification at a 3' carbon of its ribose and / or the nucleoside at the position 1 has a modification at a 2' carbon of its ribose.

This disclosure provides unshielded lipid nanoparticles and a method for producing such unshielded lipid nanoparticles, thereby overcoming the challenge of preparing particles without causing their aggregation. The lipid nanoparticles comprise nucleic acid cargo molecules; sterols or derivatives thereof present in an amount of at least 12% molar ratio; neutral lipids, such as phospholipids having a choline head group, in an amount of 22% to 65% molar ratio; and ionizable cationic amino lipids in an amount of 15% to 45% molar ratio; wherein the lipid nanoparticles are not sterically stabilized by a hydrophilic polymer-lipid conjugate or are unshielded, and wherein each % molar ratio is relative to the total lipids present in the lipid nanoparticles.

Compositions comprising Serenoa serrulata (saw palmetto) fruit extract, Laminaria saccharina (brown algae) extract, and Glycyrrhiza inflata root extract are effective inhibit the activity of 5-alpha Reductase; lower neutral lipid content; and reduce expression of SREBP1, FASN and ACACA, in human sebocytes. By regulating excess sebum production, compositions of the invention are useful to improve the health and appearance of skin.

The present disclosure provides a lipid nanoparticle comprising: nucleic acid cargo; ionizable lipid; non-polar, neutral lipid, such as a phospholipid; non-polar lipid, such as a glyceride; and sterol, the lipid nanoparticle being unshielded and wherein each mol% content is relative to total lipid present in the lipid nanoparticle.

Provided herein are lipid compounds that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination. Also provided herein are lipid nanoparticle compositions comprising said lipid compounds.

To provide a lipid composition targeting an antigen-presenting cell, and use of the composition.SOLUTION: A lipid composition consists of (1) permanent anionic lipid, (2) permanent cationic lipid, and (3) neutral lipid, and the ratio of permanent anionic lipid, permanent cationic lipid and neutral lipid in the lipid composition by a molar ratio is 14 to 33:40 to 57:22 to 40. Because a composition provided by the present invention has satisfactory organ and cell targeting effect, a protein expression level of an antigen in the spleen can be significantly improved, and percentage of cells expressing antigen in antigen-presenting cells (e.g., B cell, pDC cell, cDC cell, macrophage) in the spleen is significantly increased, the composition can be used for immunotherapy of a disease.SELECTED DRAWING: None

The invention discloses a composition containing cationic polyester and application thereof. The composition containing cationic polyester comprises cationic polyester, ionizable cationic lipid, steroidal lipid, neutral lipid and lipid polyethylene glycol. According to the composition containing the cationic polyester, spleen targeting and efficient delivery of active pharmaceutical ingredients such as mRNA (messenger Ribonucleic Acid) can be realized, especially during intravenous administration. According to the composition containing the cationic polyester, the delivery efficiency of lung injection, nasal administration and intramuscular injection can be remarkably improved.

The invention relates to a process for the preparation of a composition comprising an oligosaccharide or a polysaccharide encapsulated in lipid nanoparticles, the process comprising the following steps: preparing a first solution of a lipid portion comprising a phospholipid, a neutral lipid, and a lipid sterol; preparing a second solution comprising a poly- or oligosaccharide; preparing a third solution containing a buffer; mixing the first and second solutions using a microfluidic system to obtain lipid nanoparticles encapsulating the oligosaccharide or the polysaccharide; combining the third solution with the first and second solutions. The invention also relates to a composition comprising lipid nanoparticles obtainable by the above-defined process, said composition comprising a lipid portion comprising a phospholipid, a neutral lipid compound in which a lipid chain is bound to a glycol group, and a lipid sterol; a buffer; and an oligosaccharide or polysaccharide.

Provided herein are methods for treating a pulmonary infection in a patient in need thereof, for example, a nontuberculous mycobacterial pulmonary infection for at least one treatment cycle. The method comprises administering to the lungs of the patient a pharmaceutical composition comprising a liposomal complexed aminoglycoside comprising a lipid component comprising electrically neutral lipids and an aminoglycoside. Administration comprises aerosolizing the pharmaceutical composition to provide an aerosolized pharmaceutical composition comprising a mixture of free aminoglycoside and liposomal complexed aminoglycoside, and administering the aerosolized pharmaceutical composition via a nebulizer to the lungs of the patient. The methods provided herein result in a change from baseline on the semi-quantitative scale for mycobacterial culture for a treated patient, and / or NTM culture conversion to negative during or after the administration period.

Compositions comprising Serenoa serrulata (saw palmetto) fruit extract, Laminaria saccharina (brown algae) extract, and Glycyrrhiza inflata root extract are effective inhibit the activity of 5-alpha Reductase; lower neutral lipid content; and reduce expression of SREBP1, FASN and ACACA, in human sebocytes. By regulating excess sebum production, compositions of the invention are useful to improve the health and appearance of skin.

Provided herein are polyglycerol conjugated lipid compounds that can be used in combination with other lipid components, such as cationic lipids, neutral lipids, and cholesterol, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes. Also provided herein are lipid nanoparticle compositions comprising said polymer conjugated lipid compounds.

The lipid nanoparticles provided herein comprise encapsulated oligonucleotide molecules, which may be single-stranded or double-stranded and have a length of 5 to 500 nucleotides, a neutral lipid content of 20 to 70 mol% relative to the total lipid present in the lipid nanoparticle, an ionizable lipid; a sterol; and, optionally, a hydrophilic polymer-lipid conjugate.