Short Chain Fatty Acid PEG Conjugates for Sustained Release

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Solution Overview

Problem

Current short chain fatty acid (SCFA) therapeutic compounds have limited efficacy due to rapid absorption in the small intestine and short half-life, necessitating the development of safe and effective compositions for treating or preventing diseases and disorders.

Innovation Solution

A composition comprising at least one SCFA, an SCFA precursor, or an SCFA biosynthesis precursor, linked to a moiety such as polyethylene glycol (PEG), which hydrolyzes under low pH conditions to release the SCFA, combined with additional moieties like butyrate, propionate, and other therapeutic agents, formulated as enteric-coated extended-release capsules or eyedrops for targeted delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional methods (probiotics, prebiotics, antibiotics) are used to modulate gut microbiota, then some therapeutic effect may be achieved, but they fail to effectively increase the population of beneficial bacteria and restore healthy microbiota composition

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidability to restore healthy microbiota
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent uses short-chain fatty acids (SCFAs) as an intermediary substance that mediates between dietary intake and gut microbiota modulation. SCFAs serve as a direct metabolic product that can be supplemented to achieve therapeutic effects without relying on live probiotics or complex prebiotic formulations, thereby overcoming the limitations of conventional methods.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the therapeutic parameter from administering live organisms (probiotics) or complex substrates (prebiotics) to administering specific metabolic products (SCFAs). This parameter change simplifies the treatment approach while directly targeting the metabolic needs of beneficial bacteria and the physiological effects required for therapy.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If probiotics and prebiotics are administered, then some modulation of gut flora occurs, but the methods are complex and require specific storage and administration conditions

Engineering Contradiction:
Improvemodulation of gut floraVSAvoidcomplexity of administration
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent employs short-chain fatty acids as stable, non-living molecular compounds that do not require the complex storage and handling conditions necessary for live probiotics. SCFAs are chemically stable, have long shelf lives, and can be administered without special equipment or conditions, dramatically simplifying the therapeutic approach.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Object-affected harmful factors

If antibiotics are used to treat infections, then pathogenic bacteria are reduced, but beneficial bacteria are also damaged and microbiota balance is disrupted

Engineering Contradiction:
Improveinfection treatmentVSAvoiddamage to beneficial bacteria
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent converts the harmful effect of broad-spectrum antibiotic use into a beneficial opportunity by addressing the resulting microbiota imbalance through SCFA supplementation. Rather than trying to prevent collateral damage, the treatment embraces the disrupted state and uses SCFAs to selectively restore and promote beneficial bacteria that produce SCFAs, thereby converting the harm of antibiotic-induced dysbiosis into a chance for targeted microbiota rehabilitation.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Data Source

PatentEP3573612A1Use of short chain fatty acids for the treatment and prevention of diseases and disorders
Publication Date: 2019.12.04 TEMPLE UNIV

AI summary

The invention relates to compositions and methods that include short chain fatty acids (SCFAs), related therapeutic compounds, and other compounds, including combinations thereof, for the treatment or prevention of diseases or disorders.