Modified Alginate Hydrogel for Oral Bioactive Delivery

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Solution Overview

Problem

Current oral delivery methods for bioactive substances face challenges such as degradation by stomach acids and enzymatic action, leading to reduced bioavailability and efficacy, as well as adverse side effects like stomach upset and nausea, and difficulties in administering medications to animals.

Innovation Solution

A modified alginate hydrogel is developed by combining an aromatic compound with alginate, which encapsulates bioactive substances, protecting them from acidic environments and releasing them in the small intestine, thereby increasing bioavailability and reducing side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral delivery methods are used for bioactive substances, then the substances can be administered conveniently, but they are degraded by stomach acids and enzymatic action, reducing bioavailability and efficacy

Engineering Contradiction:

Improveconvenience of oral administrationVSAvoidbioavailability and therapeutic efficacy

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent uses alginate as an intermediary carrier substance that protects bioactive substances from stomach acids. The alginate forms a protective matrix that allows the substance to pass through the stomach intact and release it in the intestine, mediating between the harmful stomach environment and the fragile bioactive substance.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the chemical structure of alginate by introducing aromatic amino acid residues (such as tyrosine, phenylalanine, or tryptophan) to change its properties. This modification makes the alginate more resistant to stomach acid degradation while maintaining its ability to release the bioactive substance in the intestine, thus improving reliability.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If probiotic cultures are taken orally, then they can recolonize the gut with good bacteria, but they are destroyed in the stomach by stomach acids and enzymatic action, leaving few live cultures to reach the intestine

Engineering Contradiction:

Improvecolony recolonization effectivenessVSAvoidstomach acid and enzymatic destruction

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The modified alginate acts as a protective intermediary that shields probiotic cultures from stomach acids and enzymes. The alginate matrix allows the probiotics to survive passage through the stomach and reach the intestine alive, where they can then recolonize the gut effectively.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies alginate by incorporating aromatic amino acid residues that enhance its stability in acidic environments. This parameter change allows the alginate to maintain structural integrity in stomach acid while still permitting probiotic survival and subsequent release in the intestine.

Inventive Principle:

Principle #35Parameter changes

3Ease of operation

If medications are administered orally, then they can be delivered conveniently, but they cause severe stomach upset, nausea, and vomiting as adverse side effects

Engineering Contradiction:

Improveconvenience of oral deliveryVSAvoidstomach upset, nausea, and vomiting

Core Design Contradiction:

Ease of operationVSObject-generated harmful factors

Solution Approach 1:

The alginate serves as a protective intermediary barrier that prevents direct contact between the medication and the stomach lining. This mediation allows the medication to be administered orally for convenience while avoiding the harmful side effects of stomach upset and nausea by delaying release until intestinal passage.

Inventive Principle:

Principle #24Intermediary (Mediator)

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 modified alginate hydrogel effectively protects bioactive substances from stomach degradation, enhances their bioavailability, and reduces adverse side effects, allowing for more effective oral delivery of medications and supplements in humans and animals.

Implementation Method 1

A modified alginate hydrogel is developed by combining an aromatic compound with alginate

Methodology Applied

Scientific EffectChemical modification: Chemical Bonding

Implementation Method 2

which encapsulates bioactive substances, protecting them from acidic environments

Methodology Applied

Scientific EffectEncapsulation: Physical Containment

Implementation Method 3

releasing them in the small intestine, thereby increasing bioavailability

Methodology Applied

Scientific EffectpH-dependent degradation: Hydrolysis

Data Source

PatentEP3478725B1Modified carbohydrates, compositions comprising the same, and methods of making and using the same

Publication Date: 2022.08.10 WAKE FOREST UNIVERSITY HEALTH SCIENCES INC

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AI summary

Modified alginates are described herein along with hydrogels comprising the same. A modified alginate may be prepared by reacting alginate and an aromatic compound (e.g., an aromatic amine) and/or pH sensitive compound. The modified alginates, hydrogels, and/or methods described herein may be used to coat and/or encapsulate at least a portion of a bioactive substance, optionally for oral delivery in humans and other animals.