Short chain ceramide-based lipids and uses thereof
Inventors
Lencer, Wayne I. • Chinnapen, Daniel J F
Assignees
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Publication Number
US-12383606-B2
Publication Date
2025-08-12
Expiration Date
Abstract
Provided herein, in some aspects, are delivery vehicles comprising a glycosphingolipid and an agent to be delivered attached to the glycosphingolipid. In some embodiments, the glycosphingolipid comprises an oligosaccharide and a short chain (e.g., C0-C3) ceramide. In some embodiments, the agent to be delivered is a therapeutic agent. The glycosphingolipid is able to deliver the agent to a cell or to a cellular compartment, as well as across the musical barrier. In some embodiments, agents delivered using the glycosphingolipid described herein exhibit longer half-life, compared to agents delivered alone. Methods of delivering a therapeutic agent to a subject for treating a disease using the glycosphingolipid delivery vehicle are also provided.
Core Innovation
The invention relates to synthetic delivery vehicles and glycosphingolipid-agent complexes in which a glycosphingolipid comprises an oligosaccharide that presents a ceramide domain. The ceramide domain includes either a short-chain fatty acid (C1–C3) or no fatty acid. An agent to be delivered is attached to the oligosaccharide of the glycosphingolipid to form a glycosphingolipid-agent complex or glycosphingolipid-therapeutic agent complex.
The described problem being solved is the need to enhance the half-life of an agent in a subject and to treat a disease or condition by delivering therapeutically effective amounts of an agent. Conventional delivery is limited such that intracellular sorting and transcytosis across mucosal or epithelial barriers are desired while avoiding toxicity, and delivery should also yield prolonged cellular or systemic exposure.
In the disclosed approach, the use of short-chain and lyso-ceramide-containing glycosphingolipids is associated with intracellular sorting and transcytosis across mucosal or epithelial barriers, including trans-epithelial transport and transcytosis dependence. The resulting complexes are described as enabling enhanced release from membranes to solution for short-chain species, thereby improving transport of attached cargo and supporting systemic absorption and persistence.
Claims Coverage
The provided independent claims cover two method categories: enhancing the half-life of an agent in a subject, and treating a disease or condition by administering an effective amount of a glycosphingolipid-based delivery vehicle. Each independent claim shares the same core structural requirements: a glycosphingolipid with an oligosaccharide and a ceramide domain with either a C1–C3 short-chain fatty acid or no fatty acid, with the agent attached to the oligosaccharide.
Ceramide short-chain or fatty-acid-free glycosphingolipid with oligosaccharide-attached agent to enhance half-life
A method comprising administering a delivery vehicle with a glycosphingolipid comprising an oligosaccharide, wherein the glycosphingolipid comprises a ceramide that comprises a short-chain fatty acid (C1–C3) or a ceramide that does not contain a fatty acid, and wherein the agent to be delivered is attached to the oligosaccharide of the glycosphingolipid, thereby enhancing the half-life of the agent in a subject.
Effective disease or condition treatment using ceramide short-chain or fatty-acid-free glycosphingolipid with oligosaccharide-attached agent
A method comprising administering to the subject an effective amount of a delivery vehicle comprising a glycosphingolipid comprising an oligosaccharide, wherein the glycosphingolipid comprises a ceramide that comprises a short-chain fatty acid (C1–C3) or a ceramide that does not contain a fatty acid, and wherein the agent to be delivered is attached to the oligosaccharide of the glycosphingolipid, wherein the effective amount is an amount sufficient to ameliorate or reduce the extent to which the disease or condition occurs.
Across both independent claims, the inventive coverage is centered on delivering an agent attached to a glycosphingolipid oligosaccharide while specifying the ceramide domain as either containing a C1–C3 short-chain fatty acid or lacking a fatty acid, applied to either half-life enhancement of the agent or amelioration or reduction of a disease or condition through administration of an effective amount.
Stated Advantages
Enhances the half-life of an agent in a subject.
Ameliorates or reduces the extent to which a disease or condition occurs in the subject.
Documented Applications
Treating a disease or condition in a subject by administering a glycosphingolipid delivery vehicle with an agent attached to an oligosaccharide and a ceramide domain containing either a C1–C3 short-chain fatty acid or lacking a fatty acid.
Enhancing the half-life of an agent in a subject in need thereof by administering the glycosphingolipid delivery vehicle with an agent attached to the oligosaccharide and the specified ceramide domain.
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