Liposomal Polyphenol Delivery Using Cyclodextrin Inclusion Complexes

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Existing technologies face challenges with the stability, solubility, penetration depth, and duration of action of polyphenols derived from vine leaves and propolis, which are affected by degradation, toxicity of solvents, and limited bioavailability, hindering their effective use in cosmetics and pharmaceuticals.

Innovation Solution

A combinatorial delivery system using liposome-cyclodextrin carriers encapsulates vine leaf and propolis polyphenols, providing controlled release and enhanced bioavailability, utilizing a method that includes simultaneous extraction and encapsulation in a single container with natural components, ensuring stability and controlled release.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If polyphenols are extracted using conventional methods, then extraction efficiency is improved, but stability and degradation resistance deteriorate

Engineering Contradiction:
Improveextraction efficiencyVSAvoidpolyphenol stability
Core Design Contradiction:
ProductivityVSStability of the object's composition

Solution Approach 1:

The patent introduces cyclodextrins as intermediary carriers that form inclusion complexes with polyphenols during extraction. These cyclodextrin-polyphenol complexes act as stable intermediaries that protect polyphenols from degradation while being extracted, solving the contradiction between extraction efficiency and stability

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite delivery system combining liposomes and cyclodextrins. The liposome-cyclodextrin combinatorial carriers integrate two different encapsulation mechanisms, forming a composite material that provides both efficient extraction and enhanced stability against degradation

Inventive Principle:
Principle #40Composite materials

2Productivity

If solvents are used to extract polyphenols, then extraction effectiveness is improved, but toxicity increases

Engineering Contradiction:
Improveextraction effectivenessVSAvoidsolvent toxicity
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the extraction parameter from conventional organic solvents to a water-based system with cyclodextrins. This parameter change maintains extraction effectiveness through cyclodextrin-polyphenol complexation while eliminating solvent toxicity, as the system uses water and natural cyclodextrins instead of toxic organic solvents

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If polyphenols are applied directly, then immediate availability is improved, but penetration depth and duration of action deteriorate

Engineering Contradiction:
Improvepolyphenol availabilityVSAvoidpenetration depth and duration
Core Design Contradiction:
Quantity of substanceVSDuration of action of moving object

Solution Approach 1:

The patent employs a nested dual-encapsulation structure where polyphenols are first encapsulated by cyclodextrins to form inclusion complexes, and then these complexes are further encapsulated within liposomes. This nested structure enhances penetration depth and prolongs duration of action while maintaining polyphenol availability

Inventive Principle:
Principle #7Nested doll (Nesting)

Solution Approach 2:

The liposome-cyclodextrin combinatorial carriers create a composite delivery system that combines the advantages of both encapsulation types. The composite structure provides controlled release mechanisms that extend duration of action and improve penetration depth while maintaining adequate polyphenol availability

Inventive Principle:
Principle #40Composite materials

4Stability of the object's composition

If polyphenols are encapsulated for protection, then stability is improved, but release control and bioavailability may deteriorate

Engineering Contradiction:
Improvepolyphenol stabilityVSAvoidrelease control and bioavailability
Core Design Contradiction:
Stability of the object's compositionVSProductivity

Solution Approach 1:

The cyclodextrin inclusion complexes serve as intermediaries between the polyphenols and the liposome environment. These intermediaries protect polyphenols from degradation (improving stability) while also facilitating their controlled release and enhancing bioavailability through the hydrophilic-hydrophobic balance provided by cyclodextrins

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 system effectively protects and controls the release of polyphenols, maintaining stability for a year and enhancing penetration and bioavailability, suitable for dermatological and pharmaceutical uses without the need for preservatives, while ensuring safety and efficacy.

Implementation Method 1

the components of the system are extracted and simultaneously encapsulated in liposomes, cyclodextrins as well as combinatorial liposome-cyclodextrin carriers, showing a controlled release of the components

Methodology Applied
Scientific EffectEncapsulation: Physical Containment

Implementation Method 2

cyclodextrins as well as combinatorial liposome-cyclodextrin carriers

Methodology Applied
Scientific EffectInclusion complexation: Adsorption

Implementation Method 3

showing a controlled release of the components

Methodology Applied
Scientific EffectControlled release: Diffusion

Data Source

PatentUS20250339373A1Production method of a combinatorial delivery system of vine leaves and propolis polyphenols for various uses
Publication Date: 2025.11.06 APIVITA SA
  • US20250339373A1 patent drawing
  • US20250339373A1 patent drawing
  • US20250339373A1 patent drawing

AI summary

A production method of a combinatorial delivery system of vine leaves and propolis polyphenols comprising vine leaves in a ratio of 25-50%/25-50%/25-50% asyrtiko/athiri/aidani are used which are chopped into parts <0.8 mm, mixed until completely homogenized dispersed at a rate of 1 kg/min in a container that contains an extraction solvent system, in agitation at 500-3000 rpm, and propolis with a ratio of 75-25% to 50-50%, without prior treatment as long as it contains total polyphenols >1800 mg/l gallic acid equivalent after dissolving 10% per weight of propolis in ethanol, which is crushed into particles <1 mm, after cooling for 24 hours at a temperature of −20° C. and it is dispersed at a rate of 1 kg/min in another container that contains an extraction solvent system, in agitation at 500-3000 rpm they are placed together in a container that has already produced a liposomal system.