Lipophilic Nutrient Formulations via Cyclodextrin Inclusion Complexes

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current methods for enhancing the oral bioavailability of lipophilic substances, such as edible oils and vitamins, face challenges due to low solubility and stability issues, with existing solubility enhancers often compromising intestinal membrane permeability, and there is a need for a more inclusive and adaptable approach applicable to a wide range of nutritionally relevant actives in the food industry.

Innovation Solution

The development of micro- and nanonization technologies to create solid microparticulate compositions comprising sugars, polysaccharides, surfactants, and lipophilic nanospheres, which are fully dispersible in water, providing a high loading capacity and long-term stability, and allowing for differential bioavailability through controlled release profiles.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If surfactants are used to enhance solubility of lipophilic actives, then solubility is improved, but intestinal membrane permeability is compromised

Engineering Contradiction:

Improvesolubility of lipophilic activesVSAvoidintestinal membrane permeability

Core Design Contradiction:

Quantity of substanceVSReliability

Solution Approach 1:

The patent uses cyclodextrins as intermediary molecules that form inclusion complexes with lipophilic actives. The cyclodextrin structure provides a hydrophilic exterior for solubility enhancement while maintaining a hydrophobic interior cavity that protects the active, thereby improving solubility without compromising intestinal membrane permeability

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates composite formulations combining cyclodextrins with lipophilic actives, sugars, and other excipients. This composite approach allows simultaneous optimization of solubility, stability, and permeability properties that cannot be achieved with single-component systems

Inventive Principle:

Principle #40Composite materials

2Quantity of substance

If cyclodextrins are used to assist solubility of lipophilic actives, then solubility is improved, but absorption is reduced for some actives

Engineering Contradiction:

Improvesolubility of lipophilic activesVSAvoidabsorption of actives

Core Design Contradiction:

Quantity of substanceVSReliability

Solution Approach 1:

The patent optimizes the molecular weight, degree of substitution, and structure of cyclodextrin derivatives to achieve the right balance between solubility enhancement and absorption promotion. By adjusting these parameters, the formulation maintains improved solubility while ensuring adequate intestinal permeability and absorption

Inventive Principle:

Principle #35Parameter changes

3Quantity of substance

If emulsion-based technologies are used for lipophilic bio-actives, then water-dispersibility is improved, but oral bioavailability remains limited

Engineering Contradiction:

Improvewater-dispersibilityVSAvoidoral bioavailability

Core Design Contradiction:

Quantity of substanceVSReliability

Solution Approach 1:

The patent replaces mechanical emulsion systems with molecular-level inclusion complexation. Instead of relying on physical emulsion droplets that may not be preserved in gastric acid, the cyclodextrin inclusion complexes provide molecular-level solubilization that is thermodynamically stable and maintains bioavailability across the gastrointestinal pH range

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

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 compositions achieve enhanced bioavailability and stability of lipophilic substances, with high loading capacity and prolonged release profiles, improving the absorption and retention of nutrients, and are applicable to various food products, including those requiring micronized sugar for texture and solubility.

Implementation Method 1

encapsulation technologies to improve water-dispersibility, chemical stability, and handling of hydrophobic ingredients

Methodology Applied

Scientific EffectEncapsulation:

Implementation Method 2

The compositions achieve enhanced bioavailability and stability of lipophilic substances

Methodology Applied

Scientific EffectSolubility enhancement: Solvation

Implementation Method 3

Recently, a number of additional applications have been identified based on the ability of surfactants to form micelles

Methodology Applied

Scientific EffectMicelle formation:

Implementation Method 4

Traditionally, small molecule surfactants have been used in the food industry to enhance the formation and stability of emulsions

Methodology Applied

Scientific EffectSurfactant action: Surfactant

Implementation Method 5

Another popular approach to assist solubility of lipophilic actives is the use of cyclodextrins

Methodology Applied

Scientific EffectInclusion complexation:

Implementation Method 6

cyclodextrin-based formulations have gained widespread attention in the pharmaceutical industries

Methodology Applied

Scientific EffectHost-guest interaction:

Implementation Method 7

allowing for differential bioavailability through controlled release profiles

Methodology Applied

Scientific EffectControlled release:

Data Source

PatentUS20230345992A1Oral compositions of lipophilic diety supplements, nutraceuticals and beneficial edible oils

Publication Date: 2023.11.02 KARNAK TECHNOLOGIES LLC

AI summary

The invention provides compositions that increase oral bioavailability of edible lipophilic substances such as beneficial edible oils, oil-soluble vitamins, and nutraceuticals. The compositions and methods of the invention are highly applicable to food industries in the production of foods, beverages, supplements, and food additives.