Algal Oil Peptide Composition for Oral Delivery

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Solution Overview

Problem

Current oral delivery systems for biomolecules, such as insulin, face challenges including low bioavailability, rapid inactivation by the liver, and adverse effects due to portal circulation, as well as instability and side effects associated with fish oil and other omega-3 fatty acid sources, limiting their effectiveness in treating metabolic disorders like diabetes.

Innovation Solution

An oral, algal oil-based gastrointestinal tract permeable composition comprising peptides, a protease inhibitor, and a chelating agent, specifically ethylenediaminetetraacetic acid, enhances the stability and bioavailability of biomolecules by protecting them from intestinal enzymes and improving absorption, using algal oil enriched with docosahexaenoic acid as a carrier.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral delivery systems for biomolecules are used, then patient compliance is improved and adverse effects from parenteral administration are reduced, but bioavailability is poor and rapid inactivation by intestinal enzymes occurs

Engineering Contradiction:
Improvepatient complianceVSAvoidbioavailability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent employs protease inhibitors as intermediary substances that mediate between the biomolecule and intestinal enzymes. These inhibitors bind to proteases (trypsin, chymotrypsin, pepsin) and prevent them from degrading the biomolecule, thereby protecting the biomolecule during oral transit while maintaining patient compliance benefits

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent applies preliminary action by pre-treating the biomolecule with protease inhibitors before oral administration. The inhibitors are incorporated into the formulation in advance, so that when the biomolecule enters the gastrointestinal tract, the protective action is already in place to prevent enzymatic degradation

Inventive Principle:
Principle #10Preliminary action

2Reliability

If parenteral administration is used, then bioavailability is improved, but adverse effects such as lipoatrophy, lipohypertrophy, and peripheral hyperinsulinemia occur

Engineering Contradiction:
ImprovebioavailabilityVSAvoidadverse effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent substitutes the mechanical/physical parenteral administration system (injections, needles) with an oral chemical formulation system. By replacing the parenteral route with oral delivery protected by protease inhibitors, the patent eliminates the mechanical trauma and associated adverse effects like lipoatrophy and lipohypertrophy while maintaining biomolecule bioavailability

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

3Quantity of substance

If fish oil is used as carrier, then omega-3 fatty acid supplementation is provided, but instability and side effects such as fishy odor and gastrointestinal discomfort occur

Engineering Contradiction:
Improveomega-3 fatty acid contentVSAvoidoxidative stability
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent replaces fish oil with algal oil as the carrier medium. Algal oil serves as a stable, oxidatively resistant alternative that provides the necessary lipid environment for biomolecule delivery without the instability and adverse effects associated with fish oil, while still delivering omega-3 fatty acids

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

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 composition effectively treats glucose metabolism disorders and metabolic syndrome by enhancing the bioavailability and stability of peptides, reducing the risk of adverse effects, and providing a cost-effective, eco-friendly alternative to traditional parenteral administration methods.

Implementation Method 1

a protease inhibitor, and a chelating agent in the presence of water in an algal oil

Methodology Applied
Scientific EffectProtease inhibition: Enzyme

Implementation Method 2

a chelating agent in the presence of water in an algal oil

Methodology Applied
Scientific EffectChelation:

Implementation Method 3

oral, algal oil-based gastrointestinal tract permeable composition

Methodology Applied
Scientific EffectPermeation: Permeation

Data Source

PatentUS20240366731A1Oral algal oil based gastro-intestinal tract permeable peptide composition
Publication Date: 2024.11.07 CELAGENEX RES INDIA PVT LTD
  • US20240366731A1 patent drawing
  • US20240366731A1 patent drawing

AI summary

The invention disclosed herein related to an oral, algal oil-based, gastro-intestinal tract permeable peptide composition. Particularly, the invention relates to the oral, water in algal oil-based, peptide compositions for the treatment of glucose metabolic disorders comprising peptides that generally degraded in GIT, a protease inhibitor and algal oil enriched with stabilized DHA along with pharmaceutically acceptable excipients, wherein protease inhibitor forms stoichiometric complex with the protease active site with activity of 5000 to 10,000 BAEE units per mg protein.