Negatively Charged Phospholipid Dispersion for Stable Hot Drinks

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Solution Overview

Problem

Existing formulations of lipophilic and poorly water-soluble biologically active compounds face challenges in absorption due to limited solubility and stability issues, requiring high-shear homogenization and synthetic surfactants for stable colloidal dispersions, which are not feasible for household use.

Innovation Solution

A premix formulation containing a fraction of negatively charged phospholipids, which can be deprotonated by weak basic salts, allowing for the formation of a stable phospholipid dispersion in warm water without high-shear homogenization or high HLB surfactants, using an air- or oxygen-impermeable container for storage and preparation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If conventional formulations use synthetic surfactants with high HLB values and high-shear homogenization, then stable colloidal dispersions are achieved, but the complexity of equipment and process increases making household use infeasible

Engineering Contradiction:
Improvestability of colloidal dispersionVSAvoidcomplexity of homogenization equipment
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The invention changes the chemical parameters of the surfactant system by using phospholipids with specific HLB values (8-16) instead of conventional high HLB synthetic surfactants. This parameter change allows stable colloidal dispersion formation without requiring high-shear homogenization equipment, making the formulation suitable for household use while maintaining dispersion stability

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention replaces complex, expensive industrial homogenization equipment with simple, disposable mixing containers that can be used in household settings. The single-use mixing container approach eliminates the need for specialized equipment while achieving the desired colloidal dispersion through simple mixing actions

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

2Reliability

If bioactives are formulated in concentrated premixes with oils and phospholipids, then bioavailability is enhanced, but protection from hydrolysis and oxidation during storage becomes challenging

Engineering Contradiction:
Improvebioavailability of bioactivesVSAvoidhydrolysis and oxidation during storage
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention uses an inert or oxygen-impermeable mixing container to create a protective environment that prevents oxidation of the oil and bioactive components during storage and mixing. This inert environment atmosphere approach maintains the stability of the formulation while preserving bioavailability

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

Solution Approach 2:

The invention performs preliminary protection by formulating the bioactives in a concentrated premix with oils and phospholipids before use, and storing it in a protected environment. This preliminary action prevents degradation during storage while maintaining the ability to enhance bioavailability when activated by adding water or aqueous beverage

Inventive Principle:
Principle #10Preliminary action

3Stability of the object's composition

If significant amounts of carrier oil are used to deliver lipophilic bioactives, then solubility is improved, but the quantity of substance administered increases beyond feasible doses

Engineering Contradiction:
Improvesolubility of lipophilic bioactivesVSAvoidamount of carrier oil
Core Design Contradiction:
Stability of the object's compositionVSQuantity of substance

Solution Approach 1:

The invention uses phospholipids as an intermediary substance between the lipophilic bioactives and the aqueous environment. The phospholipids form colloidal structures that solubilize the bioactives without requiring large amounts of carrier oil, thus improving solubility while keeping the total quantity of substances administered at feasible levels

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite colloidal system consisting of phospholipids, oils, and bioactives in specific ratios. This composite material approach allows efficient delivery of lipophilic bioactives with reduced carrier oil content by leveraging the emulsifying and solubilizing properties of the phospholipid-bioactive complex

Inventive Principle:
Principle #40Composite materials

4Reliability

If phospholipids are used as natural colloid-forming excipients, then bioaccessibility is improved, but phospholipids themselves are sensitive to hydrolysis and oxidation when not properly stored

Engineering Contradiction:
Improvebioaccessibility of bioactivesVSAvoidstability of phospholipids
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The invention stores phospholipids in an inert or oxygen-impermeable mixing container that protects them from oxidation and hydrolysis during storage. This protected environment maintains phospholipid stability while preserving their ability to enhance bioaccessibility when activated for use

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

Solution Approach 2:

The invention uses phospholipids that can self-assemble into colloidal structures when water or aqueous beverage is added, eliminating the need for complex external stabilization systems. The phospholipids serve themselves by forming protective colloidal structures that simultaneously protect the bioactives and maintain their own stability

Inventive Principle:
Principle #25Self-service

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

Enables the preparation of a homogeneous, stable colloidal phospholipid dispersion suitable for oral intake, enhancing bioavailability and bioaccessibility of bioactive ingredients without specialized equipment, using a mixture of phospholipids, oils, and polyols in a container that can be easily mixed with warm water.

Implementation Method 1

Phospholipids can help form liposomes (phospholipid bilayer vesicles) but also micro- or nanoemulsions, as well as (mixed) micelles that can protect and carry a range of delicate bioactives

Methodology Applied
Scientific EffectColloid formation: Colloid

Implementation Method 2

Phospholipids are natural lipidic colloid-forming excipients that are capable of creating high quality stable lipid dispersions

Methodology Applied
Scientific EffectEmulsion: Emulsion

Implementation Method 3

The key element of the invention that allows for this to be achieved is the improved dispersion capacity of the phospholipids in the premix that is obtained and ensured by having a certain fraction of negatively charged phospholipids in the premix, which can be added to the premix and/or be created by treating deprotonable phospholipids present in the premix with weak basic salt

Methodology Applied
Scientific EffectDeprotonation:

Implementation Method 4

many biologically actives—and in particular those that are of natural origin—are not only vulnerable to degradation once ingested but are prone to hydrolysis and oxidation when formulated and stored in the form of a comestible aqueous health product

Methodology Applied
Scientific EffectOxidation prevention: Oxidation

Implementation Method 5

phospholipids are sensitive to hydrolysis and oxidation when not properly stored and preserved

Methodology Applied
Scientific EffectHydrolysis prevention: Hydrolysis

Data Source

PatentUS20240382598A1Lipid formulations for the preparation of health ingredient-containing hot drinks
Publication Date: 2024.11.21 LIPOSOMA HEALTH BV
  • US20240382598A1 patent drawing

AI summary

The invention relates to mixtures comprising one or more phospholipids, wherein at least 2 wt % of the phospholipids bears a net negative charge, and/or is deprotonable, whereby the mixture comprises a weak basic salt; one or more oils, butters and/or triglycerides; one or more lipophilic or poorly water-soluble biologically active ingredients; and one or more liquid or solid polyols, sugars, monohydric and/or poly hydric alcohols. The invention further relates to sealed and air- or oxygen-impermeable and liquid-im-permeable containers comprising such mixture and the preparation thereof.