Cyclodextrin Complexes for Stabilizing Specialized Pro-Resolving Mediators

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Solution Overview

Problem

Specialized pro-resolving mediators (SPMs) are chemically unstable due to their conjugated double-bond system, leading to isomerization and reduced biological activity, especially under elevated temperature and humidity conditions, posing challenges during manufacturing, formulation, packaging, storage, and distribution.

Innovation Solution

Formation of complexes between SPMs and cyclodextrins stabilizes the vulnerable triene structure of SPMs, enhancing chemical stability under conditions of elevated temperature and humidity, reducing degradation and maintaining potency.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If SPMs are stored under elevated temperature and humidity conditions, then manufacturing and distribution become more feasible, but chemical stability deteriorates due to isomerization

Engineering Contradiction:

Improvemanufacturing feasibilityVSAvoidchemical stability

Core Design Contradiction:

Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent introduces cyclodextrins as intermediary molecules that form inclusion complexes with SPMs. The cyclodextrin cage structure acts as a protective mediator, shielding the vulnerable triene system of SPMs from environmental factors like oxygen and humidity, thereby preventing isomerization while allowing feasible manufacturing and storage conditions.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite system by combining SPMs with cyclodextrins to form stable inclusion complexes. This composite structure integrates the therapeutic properties of SPMs with the protective characteristics of cyclodextrins, resulting in a formulation that maintains chemical stability under elevated temperature and humidity conditions.

Inventive Principle:

Principle #40Composite materials

2Productivity

If SPMs are exposed to air at elevated temperature, then distribution and storage are simplified, but biological activity is reduced due to degradation

Engineering Contradiction:

Improvedistribution efficiencyVSAvoidbiological activity

Core Design Contradiction:

ProductivityVSReliability

Solution Approach 1:

Cyclodextrins serve as protective intermediaries that encapsulate SPMs, shielding them from oxidative degradation and other environmental factors that would reduce biological activity. This allows for simplified distribution and storage under elevated temperature conditions while maintaining reliable biological efficacy.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The cyclodextrin complex formation provides beforehand protection against degradation pathways. By pre-encapsulating the SPM in the cyclodextrin cage structure, the vulnerable triene system is protected from contact with oxygen and humidity before degradation can occur, ensuring biological activity is maintained throughout distribution and storage.

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

3Device complexity

If SPMs are formulated without stabilization, then formulation simplicity is maintained, but chemical purity decreases due to isomerization

Engineering Contradiction:

Improveformulation complexityVSAvoidchemical purity

Core Design Contradiction:

Device complexityVSManufacturing precision

Solution Approach 1:

The patent forms a composite inclusion complex where cyclodextrins stabilize SPMs against isomerization. This composite approach maintains relatively simple formulation processes while significantly improving chemical purity by preventing degradation of the triene system during manufacturing and storage.

Inventive Principle:

Principle #40Composite materials

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

The SPM-cyclodextrin complexes maintain chemical purity and biological activity, ensuring effective pharmaceutical use by minimizing degradation and impurity formation during manufacturing, formulation, and storage.

Implementation Method 1

Formation of complexes between SPMs and cyclodextrins stabilizes the vulnerable triene structure of SPMs, enhancing chemical stability under conditions of elevated temperature and humidity

Methodology Applied

Scientific EffectInclusion complex formation:

Data Source

PatentUS12564644B2Cyclodextrin complexes of specialized proresolving mediators

Publication Date: 2026.03.03 THETIS PHARMACEUTICALS LLC

AI summary

The present invention provides complexes of a specialized pro-resolving mediator (SPM), or a salt, ester, or amide thereof, and a cyclodextrin (CD), wherein the SPM is a hydroxylated, polyunsaturated fatty acid derived from arachidonic acid, eicosapentaenoic acid, docosahexaenoic acid, or docosapentaenoic acid, 20 or 22 carbon atoms in length, with 4, 5 or 6 conjugated double bonds arranged in diene, triene, or tetraene systems or combinations thereof; and related compositions and methods.