PPAR Modulator Micelle Composition for Aqueous Solubility

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Solution Overview

Problem

Many PPAR modulators suffer from poor aqueous solubility and/or bioavailability, limiting their therapeutic utility, particularly in the treatment of neurodegenerative conditions, retinal disorders, and brain disorders.

Innovation Solution

Formulations incorporating PPAR modulators within polymeric nanocarriers, such as PEG and poloxamer-based micelles, enhance solubility and bioavailability, allowing for neuroprotective effects in vivo models of Central Nervous System Injury and the retina.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If PPAR modulators are used as therapeutic agents, then therapeutic efficacy is improved, but aqueous solubility and bioavailability deteriorate

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidaqueous solubility

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent employs polymeric nanocarriers as intermediary carriers to transport PPAR modulators through aqueous environments. These nanocarriers act as mediators between the hydrophobic drug molecules and the aqueous biological environment, enabling improved solubility and bioavailability while maintaining therapeutic efficacy. The nanocarriers facilitate drug delivery across biological membranes without requiring high concentrations of harmful solvents.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Quantity of substance

If harmful solvents like DMSO are used to solubilize PPAR modulators, then aqueous solubility is improved, but safety and toxicity worsen

Engineering Contradiction:

Improveaqueous solubilityVSAvoidtoxicity

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent replaces harmful solvents like DMSO with polymeric nanocarriers as the solubilizing intermediary. These nanocarriers are composed of biocompatible polymers that can solubilize hydrophobic PPAR modulators in aqueous media without requiring toxic solvents. The nanocarriers maintain drug solubility while eliminating the harmful effects associated with traditional solvent systems.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical-chemical parameters of the drug delivery system by transitioning from small-molecule solvent-based formulations to nanoscale carrier systems. This parameter change enables the system to achieve high drug solubility and bioavailability through surface area and interface effects at the nanoscale, eliminating the need for harmful solvents while maintaining therapeutic efficacy.

Inventive Principle:

Principle #35Parameter changes

3Ease of operation

If PPAR modulators are administered alone, then simplicity of administration is maintained, but neuroprotective efficacy deteriorates

Engineering Contradiction:

Improveadministration simplicityVSAvoidneuroprotective efficacy

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent merges the PPAR modulator with polymeric nanocarriers to create a combined delivery system. This combination enhances neuroprotective efficacy by protecting the drug from degradation, improving its delivery to target tissues, and enabling sustained release. The merged system maintains ease of administration through single-dose formulations while significantly improving therapeutic outcomes.

Inventive Principle:

Principle #5Merging (Combining)

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 polymeric nanocarrier compositions exhibit greater neuroprotective efficacy than PPAR modulators alone, providing sustained release and protection against hydrolytic degradation, with enhanced delivery across biological membranes.

Implementation Method 1

the polymeric nanocarrier component is capable of solubilising the PPAR modulators in an aqueous medium

Methodology Applied

Scientific EffectSolubilization: Solvation

Implementation Method 2

providing sustained release and protection against hydrolytic degradation

Methodology Applied

Scientific EffectPhysical containment: Physical Containment

Implementation Method 3

enhanced delivery across biological membranes

Methodology Applied

Scientific EffectPermeation: Permeation

Data Source

PatentUS20250332101A1Composition

Publication Date: 2025.10.30 CORDEIRO MARIA FRANCESCA

AI summary

The present invention provides a pharmaceutical composition comprising a peroxisome proliferator activated receptor (PPAR) modulator and an polymeric nanocarrier component, wherein the polymeric nanocarrier component is capable of solubilising the PPAR modulator in an aqueous medium and, wherein in the polymeric nanocarrier component is a micelle forming non-ionic surfactant. Uses of the same in therapy are also provided.