Carnitinoid Carrier Antioxidant Mitochondrial Delivery

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Solution Overview

Problem

Current therapies fail to effectively target and deliver antioxidants to mitochondria, leading to inadequate bioavailability and toxicity issues, which complicates the treatment of mitochondrial-associated diseases and disorders.

Innovation Solution

Development of chiral, non-racemic carnitinoid analog carrier molecules that reversibly attach and transport antioxidants across mitochondrial membranes, ensuring targeted delivery and release within the mitochondria to combat reactive oxygen species.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antioxidants are used to treat mitochondrial diseases, then antioxidant activity is provided, but bioavailability is inadequate and toxicity issues occur

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses carnitinoid analog carrier molecules as intermediaries to transport antioxidants across mitochondrial membranes. The carrier acts as a mediator that facilitates the delivery of antioxidants to their target site (mitochondria) while controlling their release, thereby improving therapeutic effectiveness and reducing toxicity through targeted delivery rather than systemic exposure

Inventive Principle:
Principle #24Intermediary (Mediator)

2Quantity of substance

If antioxidants are delivered systemically, then antioxidant activity is available, but selective uptake by mitochondria is insufficient

Engineering Contradiction:
Improveantioxidant availabilityVSAvoidtargeting precision
Core Design Contradiction:
Quantity of substanceVSLength of moving object

Solution Approach 1:

The patent applies local quality by designing carriers with specific properties (carnitinoid analog structure) that enable selective accumulation in mitochondria. The carrier molecules are engineered to have affinity for mitochondrial membranes, ensuring that antioxidants are concentrated locally at the target site rather than being uniformly distributed throughout the body

Inventive Principle:
Principle #3Local quality

3Ease of operation

If antioxidants are attached to carriers, then targeted delivery is improved, but release efficiency within mitochondria must be optimized

Engineering Contradiction:
Improvetargeted deliveryVSAvoidrelease efficiency
Core Design Contradiction:
Ease of operationVSProductivity

Solution Approach 1:

The patent employs dynamic attachment mechanisms where antioxidants are reversibly bound to carriers through ester bonds or other labile linkages. This dynamic system allows the antioxidant-carrier complex to remain stable during transport to mitochondria, then automatically release the antioxidant once inside the target organelle, optimizing both delivery and release efficiency

Inventive Principle:
Principle #15Dynamics

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 solution enables selective uptake and effective blocking of oxidative damage in mitochondria, maintaining antioxidant activity and avoiding toxicity, thus providing a therapeutic approach for mitochondrial-associated diseases and disorders.

Implementation Method 1

a carrier molecule which (i) is a biocompatible carnitinoid analog composition which does not exist in nature, (ii) is comprised of three to seven carbon atoms, (iii) presents and maintains the stereochemistry of at least one hydroxyl group similar to that of the beta-hydroxyl group in natural L-carnitine for on-demand reaction with and reversible attachment to a biologically active antioxidant

Methodology Applied
Scientific EffectReversible attachment: Chemical Bonding

Implementation Method 2

introducing said coupled antioxidant-carrier complex to a living cell; permitting said introduced coupled antioxidant-carrier complex to target and become localized within the mitochondria of the living cell

Methodology Applied
Scientific EffectSelective uptake:

Implementation Method 3

allowing said localized coupled antioxidant-carrier complex to release the antioxidant within the mitochondria for reaction with such reactive oxygen species as may then be present

Methodology Applied
Scientific EffectAntioxidant reaction: Oxidation

Data Source

PatentUS8741853B2Mitochondria-targeting antioxidant therapeutics
Publication Date: 2014.06.03 STELIOU KOSTA
  • US8741853B2 patent drawing
  • US8741853B2 patent drawing
  • US8741853B2 patent drawing

AI summary

The instant invention constitutes an unique subject matter as a whole which has four individual aspects: (1) a class of chiral, non-racemic, synthetic carnitinoid analog carrier molecules which constitute biocompatible transport compounds not found in nature; (2) a subsequently formed, mitochondria-targeting, coupled antioxidant-carrier complex comprising an antioxidant reversibly attached to and releasable from the synthetic carrier molecule; (3) a method for introducing a biologically active antioxidant into the interior of mitochondria of a living cell for subsequent reaction with such reactive oxygen species may then be present; and (4) a system for delivering a biologically active antioxidant to the interior of mitochondria within a living cell.