Pressurized Nanoemulsion Formulation for Temperature-Stable Vesicles

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Solution Overview

Problem

Existing nanoemulsions are not stable under stressed conditions such as high temperatures or freezing, leading to destabilization and loss of pharmaceutical quality, particularly when combined with active agents like 5-aminolevulinic acid (ALA).

Innovation Solution

A formulation comprising an aqueous component, a carrier component with lipophilic components, surfactants, and alcohol, and a propellant, stored in a pressurized container, without fatty alcohols or gelling agents, to maintain stability and vesicle size homogeneity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If nanoemulsions are stored under stressed conditions (high temperature or freezing), then the stability and vesicle size homogeneity deteriorate, but storage is necessary for pharmaceutical distribution and use

Engineering Contradiction:
Improvevesicle size homogeneityVSAvoidstorage temperature stress
Core Design Contradiction:
Stability of the object's compositionVSTemperature

Solution Approach 1:

The patent applies parameter changes by optimizing the surfactant composition (specific HLB values between 8-16), alcohol content (5-20% w/w), and lipophilic component ratios to create a nanoemulsion formulation that maintains vesicle size stability under temperature stress. The specific parameter ranges for each component were adjusted to achieve thermodynamic stability across varying temperatures.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses a composite material approach by combining multiple components (surfactants with specific HLB ranges, alcohols, lipophilic substances, and aqueous phases) into a synergistic formulation. This composite nanoemulsion system leverages the complementary properties of each component to enhance overall thermal and freeze-thaw stability while maintaining vesicle size homogeneity.

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If conventional emulsifiers and stabilizers are added to improve nanoemulsion stability, then the formulation complexity increases, but stability is needed for long-term storage

Engineering Contradiction:
Improvelong-term stabilityVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent reduces formulation complexity by optimizing parameters within a limited component set: surfactants with HLB 8-16, alcohols at 5-20% w/w, and lipophilic components at specific ratios. This parameter optimization achieves long-term stability without requiring multiple different emulsifier types or complex stabilization systems.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention applies multi-functionality by selecting surfactants and alcohols that simultaneously provide emulsification, stabilization, and temperature resistance properties. These components perform multiple functions (emulsifying oil and water phases while also providing thermal stability and freeze-thaw resistance), reducing the need for separate stabilizing agents.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Stability of the object's composition

If nanoemulsions are made thermodynamically stable, then they may lose their metastable properties needed for controlled release and skin penetration, but stability is required for pharmaceutical quality

Engineering Contradiction:
Improvethermodynamic stabilityVSAvoidpharmaceutical quality
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

The patent carefully adjusts parameters to achieve a balance: surfactant HLB values between 8-16 and alcohol concentrations of 5-20% w/w provide sufficient thermodynamic stability for pharmaceutical quality while maintaining the metastable characteristics needed for controlled release. The lipophilic component selection and ratios are optimized to preserve skin penetration capabilities.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The composite nanoemulsion formulation combines components with complementary properties that collectively provide both thermodynamic stability and controlled release characteristics. The synergistic interaction between surfactants, alcohols, and lipophilic substances creates a system that maintains pharmaceutical quality while enabling controlled delivery to skin layers.

Inventive Principle:
Principle #40Composite materials

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 formulation maintains stable nanovesicle sizes and active agent content under stressed conditions, enhancing stability and efficacy in pharmaceutical and cosmetic applications.

Implementation Method 1

a pressurized container, wherein the formulation comprises essentially no fatty alcohol as foam adjuvant

Methodology Applied
Scientific EffectPressurisation: Pressurisation

Data Source

PatentUS12409112B2Pressurized nanoemulsion
Publication Date: 2025.09.09 BIOFRONTERA INC
  • US12409112B2 patent drawing
  • US12409112B2 patent drawing
  • US12409112B2 patent drawing

AI summary

The present invention relates to stabilizing an oil in water nanoemulsion in a pressurized container. The nanovesicles comprised in the nanoemulsion are particularly stable in regard to vesicle size and vesicle size homogeneity after long-term storage at different temperatures.