78 results about "Neutral lipid" patented technology

Provided herein are PEGylated liposomes, and methods of making and using thereof. The PEGylated liposomes comprise at least a cholesterol, a non-PEGylated neutral lipid, and a PEGylated lipid, wherein the average molecular weight of the PEG component in the PEGylated lipid is about 5000 Daltons or less. The PEGylated liposomes are stable and capable of delivery of an agent for the generation of an immune response, for example an agent for vaccine, therapeutic, or diagnostic uses. Compositions and methods related to making the PEGylated liposomes and using the PEGylated liposomes for stimulating an immune response are also provided.

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.

The invention relates to lidocaine multivesicular liposome as well as a preparation method and application thereof, belongs to the field of medicines, and solves at least one of the problems of higher toxicity, insufficient safety, short action time, limited clinical application range, higher cost and the like of the existing postoperative analgesic medicine. The lidocaine multi-vesicular liposome is prepared from lidocaine and a lipid, wherein the lidocaine and the lipid are added into the lidocaine multi-vesicular liposome; the lipid comprises amphiphilic lipid, negatively charged phospholipid, neutral lipid and cholesterol. The lidocaine multi-vesicular liposome prepared by the preparation method is high in safety, solves the problems of systemic toxicity, neurotoxicity, cardiotoxicity and the like of the existing postoperative analgesic drugs, has the characteristics of long-acting slow release, remarkable analgesic effect and wide clinical application range, and is suitable for clinical application. And a new solution is provided for effectively relieving postoperative pain.

Provided herein are lipid nanoparticles encapsulating nucleic acids having a neutral lipid in a molar ratio of at least 30%, a sterol or a derivative thereof, and a targeting moiety anchored in its lipid layer by a lipophilic moiety. Methods of using the lipid nanoparticles for targeted delivery in vivo are also provided. Such lipid nanoparticles may have significantly improved delivery and targeting to extrahepatic tissues and / or organs.

Provided herein are PEGylated liposomes, and methods of making and using thereof. The PEGylated liposomes comprise at least a cholesterol, a non-PEGylated neutral lipid, and a PEGylated lipid, wherein the average molecular weight of the PEG component in the PEGylated lipid is about 5000 Daltons or less. The PEGylated liposomes are stable and capable of delivery of an agent for the generation of an immune response, for example an agent for vaccine, therapeutic, or diagnostic uses. Compositions and methods related to making the PEGylated liposomes and using the PEGylated liposomes for stimulating an immune response are also provided.

The present invention provides an amino lipid, and lipid nanoparticles (LNPs) and a use thereof, the amino lipid having a structure represented by general formula (I), or an isomer, pharmaceutically acceptable salt, prodrug or solvate of the amino lipid. The present invention further provides LNPs containing the amino lipid. According to the present invention, the amino lipid having a structure represented by general formula (I) is used as an ionizable lipid compound, and the LNPs are obtained by means of self-assembly of the ionizable lipid compound, a steroid, a neutral lipid, and a polymer-bonded lipid. The LNPs can further improve the translation expression level of a nucleic acid load in cells, improve the effect of a nucleic acid-LNP preparation, and enable the nucleic acid-LNP preparation to provide a theoretical basis for personalized treatment.

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

Provided is a preparation method for a liposome, 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 liposome. Compared with the prior art, the present invention uses an ultrasonic emulsification method to prepare the liposome, so that the quality of the liposome prepared in different batches is controllable, and the preparation of the liposome 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 liposomes, so that the method can be used to not only prepare a liposome with unsaturated fatty acid chain phospholipids and neutral lipids as raw materials, but also synthesize a liposome 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 liposome production can be expanded.

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 invention relates to application of biochanin A in preparation of medicines for preventing or treating liver diseases or liver injury. The biochanin A has the characteristics of remarkable curative effect, safety, reliability, small toxic and side effects and the like when being used for treating the non-alcoholic fatty liver disease; the biochanin A reduces the accumulation of lipid peroxidation products and reduces the neutral lipid level by inhibiting the iron accumulation of liver tissues, so that the fatty degeneration of the liver and the liver injury are relieved. Starting from a monomeric compound, the compound intervenes in the non-alcoholic fatty liver disease, the levels of ALT, AST and TC in serum of a model mouse and TG in liver tissue are remarkably reduced, liver adiposis and inflammatory injury are relieved, and the compound has a good clinical application prospect.

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.

Disclosed herein are pH-sensitive nanoemulsions as well as methods of using thereof. These pH-sensitive nanoemulsions can comprise a lipid particle encapsulating an active agent. The lipid particle can comprise one or more ionizable lipids; one or more neutral lipids; one or more PEGylated lipids; and optionally one or more fusogenic oils. In some embodiments, these compositions can be buffered at an acidic pH (e.g., a pH of less than 6.5, such as a pH of from 4 to 6.5, or a pH of from 5.0 to 6.5). By buffering at an acidic pH, the delivery efficiency of the compositions can be enhanced as compared to otherwise identical compositions buffered at a pH of 7 or more.

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.

The invention provides lipid bodies isolated from yeast, compositions comprising the lipid bodies, products made from the lipid bodies, methods of making the lipid bodies, and methods of using the lipid bodies. The lipid bodies of the invention have an exceptionally large size and high internal neutral lipid content, providing a number of advantages for a variety of practical applications.

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.