Urolithin A Nanoparticles for Kidney Injury Treatment

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Urolithin A (UA) has poor absorption in the gastrointestinal tract and low oral bioavailability, requiring frequent and high doses for therapeutic benefits, especially for conditions like acute kidney injury, lupus, and inflammatory disorders, where there is a lack of effective treatments.

Innovation Solution

Nanoparticle compositions comprising UA, specifically polymeric nanoparticles conjugated with gambogic acid, are formulated for improved oral delivery, enhancing bioavailability and therapeutic efficacy by facilitating transport across biological barriers.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If UA is administered orally to patients, then therapeutic benefits can be achieved, but poor absorption in the GI tract results in low bioavailability requiring frequent high dosing

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoiddose frequency and amount

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent uses nanoparticle carriers as intermediaries to deliver UA through the GI tract. These nanoparticles protect UA from degradation, enhance intestinal absorption, and facilitate transport across biological barriers, thereby improving bioavailability and reducing the required dose frequency and amount while maintaining therapeutic efficacy

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physical and chemical parameters of UA by formulating it into nanoparticle systems with controlled size, surface charge, and composition. These parameter changes enhance solubility, stability, and permeability of UA in the GI tract, leading to improved absorption and reduced dosing requirements

Inventive Principle:

Principle #35Parameter changes

2Reliability

If high doses of UA are given to patients, then therapeutic benefits can be achieved, but poor oral bioavailability requires even higher and more frequent dosing

Engineering Contradiction:

Improvetherapeutic benefitVSAvoiddosing frequency

Core Design Contradiction:

ReliabilityVSLoss of time

Solution Approach 1:

Nanoparticle carriers serve as intermediaries that extend the circulation time of UA in the bloodstream and maintain sustained therapeutic concentrations. This reduces the frequency of dosing while maintaining therapeutic benefits, addressing the time loss associated with frequent high-dose administration

Inventive Principle:

Principle #24Intermediary (Mediator)

3Ease of operation

If nanoparticle compositions are formulated for oral administration, then delivery of UA to patients is improved, but formulation complexity increases

Engineering Contradiction:

Improveoral administration capabilityVSAvoidnanoparticle formulation

Core Design Contradiction:

Ease of operationVSDevice complexity

Solution Approach 1:

The patent employs composite nanoparticle formulations combining UA with biocompatible polymers, surfactants, and targeting ligands. These composite structures integrate multiple functions (protection, solubilization, targeting) into a single oral formulation, improving ease of administration while managing formulation complexity through standardized manufacturing approaches

Inventive Principle:

Principle #40Composite materials

Data Source

PatentUS11504339B2Compositions comprising urolithin a and uses thereof in treating kidney injury

Publication Date: 2022.11.22 TEXAS A&M UNIVERSITY

AI summary

The present disclosure provides nanoparticle compositions comprising i) a polymeric nanoparticle, ii) one or more ligands conjugated to the polymeric nanoparticle, and iii) urolithin A. The disclosure also provides methods and pharmaceutical compositions comprising the nanoparticle compositions for use in treating patients with various disease states.