Disulfide Crosslinked Protein Nanoparticles for IBD Delivery

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Solution Overview

Problem

Current therapies for inflammatory bowel disease (IBD) face challenges due to the harsh environment of the gastrointestinal tract, which limits the effectiveness of biologics and leads to systemic immunosuppression and toxicity, necessitating improved delivery methods for therapeutic agents.

Innovation Solution

Development of nanoparticles comprising recombinant proteins, such as AvrA, with disulfide bonds for crosslinking, which are designed to withstand the gastrointestinal environment and target specific sites for enhanced therapeutic delivery and bioactivity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If biologics are administered orally or by injection to treat IBD, then therapeutic effect is achieved, but the biologics cannot survive serum proteases, harsh gastrointestinal environment, or clearance processes leading to reduced effectiveness

Engineering Contradiction:
Improvesurvival of biologics in gastrointestinal environmentVSAvoidharsh gastrointestinal environment, serum proteases, clearance processes
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses nanoparticles as intermediary carriers to protect biologics from the harsh gastrointestinal environment. The nanoparticle carrier shields the biologic from serum proteases and clearance processes, enabling oral or injectable administration while maintaining therapeutic effectiveness in IBD treatment.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs disulfide crosslinking to modify the structural parameters of nanoparticles, creating a stable configuration that withstands gastrointestinal conditions. The disulfide bonds provide structural integrity while allowing controlled disassembly in the reducing environment of the gut, thereby protecting and delivering biologics effectively.

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If current IBD therapies use systemic corticosteroids and immunosuppressants, then inflammation is suppressed, but systemic immunosuppression and toxicities occur

Engineering Contradiction:
Improveinflammation suppressionVSAvoidsystemic immunosuppression, toxicities
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent enables localized delivery of therapeutic proteins to the intestinal tract through nanoparticle formulation. This local delivery approach concentrates the therapeutic effect at the site of inflammation while minimizing systemic exposure, thereby reducing systemic immunosuppression and toxicities associated with conventional IBD therapies.

Inventive Principle:
Principle #3Local quality

3Stability of the object's composition

If nanoparticles are designed to withstand gastrointestinal environment, then stability is improved, but the complexity of maintaining stability and bioactivity increases

Engineering Contradiction:
Improvenanoparticle stability in gastrointestinal conditionsVSAvoidcomplexity of maintaining stability and bioactivity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent creates composite nanoparticle structures combining proteins with disulfide crosslinkers. This composite approach provides inherent stability in gastrointestinal conditions through the crosslinked network while maintaining bioactivity, avoiding the need for complex protective coatings or additional stabilizing agents.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent utilizes the redox parameter change between the oxidizing gastrointestinal environment and the reducing intracellular environment to control nanoparticle stability and disassembly. Disulfide crosslinks remain intact in the gut but break in the reducing environment, providing automatic stability control without complex design interventions.

Inventive Principle:
Principle #35Parameter changes

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 nanoparticles effectively deliver therapeutic proteins to the intestinal tract, reducing inflammation and improving symptoms in IBD models by suppressing pro-inflammatory signaling, while maintaining stability and bioactivity in the harsh gastrointestinal conditions.

Implementation Method 1

particles comprising recombinant proteins, such as AvrA, with disulfide bonds for crosslinking

Methodology Applied
Scientific EffectDisulfide bonding: Chemical Bonding

Implementation Method 2

The nanoparticles effectively deliver therapeutic proteins to the intestinal tract

Methodology Applied
Scientific EffectNanoparticle transport:

Implementation Method 3

reducing inflammation and improving symptoms in IBD models by suppressing pro-inflammatory signaling

Methodology Applied
Scientific EffectAnti-inflammatory signaling:

Data Source

PatentEP2970399B1Protein particles comprising disulfide crosslinkers and uses related thereto
Publication Date: 2021.11.10 GEORGIA TECH RES CORP
  • EP2970399B1 patent drawingFigure 1~2C
  • EP2970399B1 patent drawingFigure 3A~3D
  • EP2970399B1 patent drawingFigure 4A~5

AI summary

This disclosure relates to particles comprising recombinant proteins, pharmaceutical composition comprising the particles, and therapeutic uses related thereto. In certain embodiments, the particles are made by the process of producing recombinant proteins and conjugating the recombinant proteins to form nanoparticles with a linking reagent comprising disulfide bonds. Typically the recombinant protein has a polypeptide of viral, fungal, or bacterial origin such as secreted effector proteins AvrA and YopJ. In certain embodiments, the disclosure relates to treating or preventing autoimmune diseases, cancer, or inflammatory diseases, or conditions such as inflammatory bowel disease (IBD).