Ionic Liquid GLP-1 and Amylin Salt Compositions for Oral Delivery

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Solution Overview

Problem

Existing formulations for therapeutic agents like GLP-1 analogs and amylin analogs face challenges in effectively delivering these proteins orally due to their stability and solubility issues, particularly when crossing mucosal membranes.

Innovation Solution

The development of compositions that non-covalently or covalently attach proteins or peptides to ions present in ionic liquids, which are then formulated for oral administration, utilizing ionic liquids to enhance solubility and delivery across mucosal membranes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If therapeutic agents like GLP-1 analogs and amylin analogs are administered orally, then patient compliance and ease of administration are improved, but stability and solubility issues prevent effective delivery across mucosal membranes

Engineering Contradiction:

Improveease of administrationVSAvoiddelivery effectiveness

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent uses ionic liquids as intermediary carriers to transport therapeutic peptides across mucosal membranes. The ionic liquid composition acts as a mediator that facilitates the passage of GLP-1 analogs and amylin analogs through the mucosal barrier, enabling oral delivery while maintaining drug stability and effectiveness.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physical and chemical parameters of the therapeutic agents by forming complexes with ionic liquids. This changes the solubility, stability, and membrane permeability characteristics of the peptides, allowing them to survive gastric conditions and cross mucosal barriers effectively for oral administration.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If ionic liquids are used to enhance solubility and delivery of therapeutic agents, then oral bioavailability is improved, but formulation complexity increases

Engineering Contradiction:

Improveoral bioavailabilityVSAvoidformulation complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent creates composite formulations by combining ionic liquids with therapeutic peptides in specific ratios. This composite approach integrates the solubility-enhancing properties of ionic liquids with the therapeutic activity of the peptides, achieving improved oral bioavailability while managing formulation complexity through defined compositional parameters.

Inventive Principle:

Principle #40Composite materials

3Stability of the object's composition

If proteins are attached to ions in ionic liquids, then solubility and membrane crossing ability are enhanced, but manufacturing precision requirements increase

Engineering Contradiction:

ImprovesolubilityVSAvoidattachment precision

Core Design Contradiction:

Stability of the object's compositionVSManufacturing precision

Solution Approach 1:

The patent segments the attachment process into controlled stages, forming ionic liquid-peptide complexes with defined stoichiometries. This segmentation allows for precise control of the attachment process, ensuring consistent solubility enhancement while managing manufacturing precision requirements through standardized preparation protocols.

Inventive Principle:

Principle #1Segmentation

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

This approach improves the oral delivery of therapeutic agents by enhancing their solubilization and systemic circulation, making them suitable for treating metabolic disorders and gastro-intestinal inflammation.

Implementation Method 1

compositions of matter and methods of use for the treatment of diseases or disorders... a protein or a peptide is non-covalently attached to one or more ions wherein such ions are also present in the said ionic liquid

Methodology Applied

Scientific EffectIonic attachment: Ion Repulsion/Attraction

Implementation Method 2

utilizing ionic liquids to enhance solubility and delivery across mucosal membranes... improves the oral delivery of therapeutic agents by enhancing their solubilization and systemic circulation

Methodology Applied

Scientific EffectSolubilization: Solvation

Data Source

PatentUS12350320B2Compositions comprising pharmaceutically acceptable salts of glucagon-like peptide-1 analogs and pharmaceutically acceptable salts of amylin analogs, and uses thereof

Publication Date: 2025.07.08 I2O THERAPEUTICS INC

AI summary

Provided herein are compositions comprising a first compound having the structure of first Formula Ia, wherein the first compound comprises a first therapeutic agent having the configuration of [diacid]-[linker]-[an amylin analog], in which the amylin analog has the amino acid sequence of SEQ ID NO: 20, with a proviso that the amino acid sequence comprises one or more of the following amino acid substitutions: N14E, V17R, Y37P, F15E, L16E, V17E, or any combination thereof, and the first compound has an anion: cation molar ratio of from about 1:1 to about 1:3, and a second compound having the structure of second Formula Ia, wherein the second compound comprises a second therapeutic agent having the sequence of SEQ ID NO: 35, and the second compound has an anion: cation molar ratio of from about 1:1 to about 1:7, and methods of using thereof for the treatment of metabolic diseases or disorders, including type 1 diabetes, type 2 diabetes, obesity, overweight, and nonalcoholic steatohepatitis, and for reducing weight in a subject in need thereof.