Bioactive Lipophilic Emulsion Stability via Composite Solubilizers

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Solution Overview

Problem

Existing formulations of water-soluble compositions, such as those containing polyoxyethanyl-α-tocopheryl sebacate (PTS) and lipophilic bioactives like CoQ10, suffer from instability issues, particularly when used in emulsions, which limits their commercialization in food, beverage, and supplement products.

Innovation Solution

Incorporating a bioactive lipophilic compound, an oil, and a compound of Formula (I) where X is a hydrophobic moiety and Y is a hydrophilic moiety, with specific ratios, to form a homogeneous melt that is then combined with water, enhancing emulsion stability through heating and homogenization processes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If water-soluble compositions comprising lipophilic bioactives and solubilizing agents like PTS are used, then solubilization of lipophilic compounds is achieved, but emulsion stability is insufficient

Engineering Contradiction:

Improvesolubilization capacityVSAvoidemulsion stability

Core Design Contradiction:

Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent combines multiple solubilizing agents (PTS and PEG-40 hydrogenated castor oil) with lipophilic bioactives and oils to create a composite emulsion system. This composite approach leverages the synergistic effects of different surfactants and lipid components to achieve both solubilization and enhanced stability, resolving the contradiction between solubilization capacity and emulsion stability.

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The patent optimizes the concentration ratios of solubilizing agents, bioactives, and oils to achieve stable emulsions. By adjusting parameters such as the ratio of PTS to PEG-40 hydrogenated castor oil (e.g., 1:1, 2:1, or 1:2) and controlling the amount of oil (1-50% w/w), the system achieves both adequate solubilization and improved emulsion stability.

Inventive Principle:

Principle #35Parameter changes

2Quantity of substance

If lipophilic bioactive compounds are combined with solubilizing agents without oil, then solubilization is achieved, but emulsion stability is poor

Engineering Contradiction:

Improvesolubilization efficiencyVSAvoidemulsion stability

Core Design Contradiction:

Quantity of substanceVSReliability

Solution Approach 1:

The patent introduces oil components specifically to the hydrophobic phase of the emulsion system, creating local structural improvements. The oil (1-50% w/w of total composition) localizes within the lipid domains, providing structural support and stability to the emulsion droplets without compromising the overall solubilization efficiency of the hydrophilic-hydrophobic interface.

Inventive Principle:

Principle #3Local quality

3Adaptability or versatility

If rigid molecules like CoQ10 are used in emulsions, then bioactive delivery is achieved, but emulsion stability is compromised

Engineering Contradiction:

Improvebioactive delivery capabilityVSAvoidemulsion stability

Core Design Contradiction:

Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent uses a combination of PTS and PEG-40 hydrogenated castor oil as intermediary solubilizing agents that mediate between the rigid bioactive molecules (like CoQ10) and the aqueous phase. These intermediaries form stable micellar structures that encapsulate the rigid bioactives, allowing them to be delivered in liquid form while maintaining emulsion stability through the cooperative action of multiple surfactants.

Inventive Principle:

Principle #24Intermediary (Mediator)

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 method significantly improves the stability of emulsions containing lipophilic bioactives, allowing for the creation of stable pharmaceutical, cosmetic, and dietary supplement formulations that do not require pill form, suitable for diverse consumer needs.

Implementation Method 1

a solubilizing agent can be polyoxyethanyl-α-tocopheryl sebacate (PTS)... to solubilize lipophilic compounds and bioactives

Methodology Applied

Scientific EffectMicelle formation: Surfactant

Implementation Method 2

heating a composition comprising the bioactive lipophilic compound, the oil and the compound of Formula (I) to form a homogeneous melt

Methodology Applied

Scientific EffectMelting: Melting

Implementation Method 3

combining the homogeneous melt with water using either blending or high shear mixing, optionally followed by homogenization by use of a microfluidizer

Methodology Applied

Scientific EffectEmulsion formation: Emulsion

Data Source

PatentUS20230049050A1Emulsions of bioactive lipophilic compounds including oils

Publication Date: 2023.02.16 MICILLIC LDA

AI summary

The present application relates to compositions corn-sing a bioactive lipophilic compound, an oil and at least one solubilizing agent that is a compound of Formula (I), to emulsions comprising such compositions and to uses thereof. The present application also relates to methods of preparing such emulsions. The methods comprise heating such compositions to form a homogeneous melt and combining the homogeneous melt with water to obtain the emulsion.