Methods for the preparation of liposomes
Inventors
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Assignees
Member
CuriRxCuriRx is a minority woman-owned Contract Research, Development, and Manufacturing Organization (CRDMO) based in Massachusetts. The company provides comprehensive solutions for drug development with expertise in bioprocessing, formulation development, analytical testing, and manufacturing support. CuriRx offers services across the therapeutic development spectrum, including customized solutions, collaboration, cutting-edge analytical methods, and process optimization to accelerate client projects from discovery to clinical and commercial stages.
CuriRx is a minority woman-owned Contract Research, Development, and Manufacturing Organization (CRDMO) based in Massachusetts. The company provides comprehensive solutions for drug development with expertise in bioprocessing, formulation development, analytical testing, and manufacturing support. CuriRx offers services across the therapeutic development spectrum, including customized solutions, collaboration, cutting-edge analytical methods, and process optimization to accelerate client projects from discovery to clinical and commercial stages.
Publication Number
US-9402812-B2
Publication Date
2016-08-02
Expiration Date
Abstract
Provided herein are methods for preparing liposomes and uses thereof. In certain embodiments, liposomes are prepared without using heat, organic solvents, proteins, and/or inorganic salts in the process. In certain embodiments, the liposomal preparation contains one or more active agents. In certain embodiments, the liposomal preparations are used in the treatment of diseases or disorders.
Core Innovation
The invention relates to a method of preparing a pharmaceutical composition comprising unilamellar liposomes, wherein the unilamellar liposomes comprise a hydrophobic pharmaceutical agent. The method forms multilamellar liposomes by dispersing one or more solid phospholipids in an aqueous medium that is free of organic solvents, surfactants, and protein excipients, and that is at ambient temperature. In one approach, the suspension is rendered isotonic by adding a disaccharide.
The invention further homogenizes the multilamellar liposome suspension to form an isotonic suspension of unilamellar liposomes. The method adds the hydrophobic pharmaceutical agent as a solid to the isotonic suspension and subjects the mixture to microfluidization to form the pharmaceutical composition. The unilamellar liposomes are less than about 100 nm in diameter and comprise the hydrophobic pharmaceutical agent.
In an alternative method, the invention forms liposomes by concurrently mixing one or more solid phospholipids, a disaccharide, and the hydrophobic pharmaceutical agent added as a separate component in solid form in an aqueous medium. The resulting multilamellar liposomes are homogenized to form unilamellar liposomes that are less than about 100 nm in diameter and comprise the hydrophobic pharmaceutical agent.
Claims Coverage
The partial claim set includes two independent claims with five inventive features. The claims center on forming multilamellar liposomes in an aqueous, ambient-temperature medium free of specified excipients or chemicals, converting to unilamellar liposomes by homogenizing, and producing sub-100-nm unilamellar liposomes comprising a hydrophobic pharmaceutical agent using microfluidization or concurrent solid mixing.
Ambient temperature multilamellar liposome formation in an aqueous medium free of organic solvents and protein excipients
forming a suspension of multilamellar liposomes by dispersing one or more solid phospholipids in an aqueous medium, wherein the aqueous medium is free of organic solvents and protein excipients, and the aqueous medium is at ambient temperature
Isotonic disaccharide rendering followed by homogenizing to unilamellar liposomes
adding a disaccharide to the multilamellar liposome suspension, rendering the suspension isotonic; homogenizing the multilamellar liposome suspension to form an isotonic suspension of unilamellar liposomes
Solid addition of a hydrophobic pharmaceutical agent and microfluidization to sub-100 nm unilamellar liposomes
adding the hydrophobic pharmaceutical agent as a solid to the isotonic suspension of unilamellar liposomes and subjecting the mixture to microfluidization to form the pharmaceutical composition comprising unilamellar liposomes, wherein the unilamellar liposomes are less than about 100 nm in diameter and comprise the hydrophobic pharmaceutical agent
Concurrent solid mixing of phospholipids, disaccharide, and hydrophobic pharmaceutical agent in an aqueous medium at ambient temperature
forming liposomes by concurrently mixing one or more solid phospholipids, a disaccharide, and the hydrophobic pharmaceutical agent added as a separate component in solid form in an aqueous medium to produce multilamellar liposomes comprising the hydrophobic pharmaceutical agent, wherein the aqueous medium is free of organic solvents, surfactants, and protein excipients, and the aqueous medium is at ambient temperature
Homogenizing to form sub-100 nm unilamellar liposomes comprising the hydrophobic pharmaceutical agent
homogenizing the composition to form the pharmaceutical composition comprising unilamellar liposomes, wherein the unilamellar liposomes are less than about 100 nm in diameter and comprise the hydrophobic pharmaceutical agent
Across both independent claims, the inventive coverage centers on creating multilamellar liposomes at ambient temperature in an aqueous medium free of specified components, converting to isotonic or directly formed unilamellar liposomes by homogenizing, and incorporating a hydrophobic pharmaceutical agent as a solid, with unilamellar liposomes limited to less than about 100 nm in diameter.
Stated Advantages
Documented Applications
Disease treatment use cases with parenteral administration across diverse disorders and infections [procedural detail omitted for safety].
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