Hyaluronic Acid Hydrogels with Vitamin A Cyclodextrin Complexes

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Solution Overview

Problem

Skin aging is challenging due to endogenous and exogenous factors, leading to collagen breakdown and reduced mechanical tension in the dermal connective tissue, which existing treatments like hyaluronic acid compositions with retinol face solubility and stability issues, especially in aqueous environments.

Innovation Solution

A composition combining hyaluronic acid with a cyclodextrin complexed to vitamin A, including retinol and its esters, to enhance solubility and sustained release, thereby stimulating collagen production and regulating collagen-degrading enzymes, while maintaining stability in dermal fillers.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If vitamin A esters are used in dermal fillers, then they provide sustained release and stability, but they become insoluble in aqueous environments

Engineering Contradiction:
ImprovestabilityVSAvoidsolubility
Core Design Contradiction:
Stability of the object's compositionVSQuantity of substance

Solution Approach 1:

Cyclodextrin acts as a mediator between vitamin A esters and the aqueous environment. The cyclodextrin forms inclusion complexes with the hydrophobic vitamin A esters, enabling them to be dispersed and delivered in aqueous dermal filler compositions while maintaining their stability and sustained release properties

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical-chemical parameters of vitamin A esters by forming inclusion complexes with cyclodextrin. This transformation allows the ester forms to become water-soluble while maintaining their stability and sustained release characteristics, resolving the contradiction between solubility and stability

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If retinol is used in dermal fillers, then it can be metabolized to retinoic acid, but it faces solubility issues in aqueous environments

Engineering Contradiction:
Improvemetabolism to retinoic acidVSAvoidsolubility
Core Design Contradiction:
Adaptability or versatilityVSQuantity of substance

Solution Approach 1:

Cyclodextrin serves as an intermediary carrier for retinol in aqueous dermal filler compositions. The inclusion complex formation enables retinol to be delivered in water-based formulations while maintaining its ability to be metabolized by skin into retinoic acid

Inventive Principle:
Principle #24Intermediary (Mediator)

3Strength

If collagen synthesis is stimulated to prevent skin aging, then mechanical tension is improved, but matrix metalloproteins formation increases

Engineering Contradiction:
Improvemechanical tensionVSAvoidmatrix metalloproteins formation
Core Design Contradiction:
StrengthVSObject-generated harmful factors

Solution Approach 1:

The patent utilizes the parameter of vitamin A metabolism - when delivered via cyclodextrin inclusion complexes, vitamin A is metabolized to retinoic acid which selectively stimulates collagen synthesis while downregulating matrix metalloproteins, changing the balance between collagen production and degradation

Inventive Principle:
Principle #35Parameter changes

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 composition effectively stimulates collagen production, downregulates collagen-degrading enzymes, and improves skin elasticity and hydration, addressing the challenges of skin aging by providing a stable and effective dermal filler solution.

Implementation Method 1

a cyclodextrin and vitamin A complexed to the cyclodextrin

Methodology Applied
Scientific EffectInclusion complexation: Absorption (physical)

Implementation Method 2

improve sustained release of vitamin A

Methodology Applied
Scientific EffectSustained release: Diffusion

Data Source

PatentEP2903588B1Dermal filler hydrogels with vitamin a/cyclodextrin inclusion complexes
Publication Date: 2020.02.19 ALLERGAN INC
  • EP2903588B1 patent drawing
  • EP2903588B1 patent drawing
  • EP2903588B1 patent drawing

AI summary

Compositions, such as hydrogel compositions, that include a hyaluronic acid, a vitamin A, and a cyclodextrin may be used as medical or cosmetic fillers, implants, or creams. For example, the compositions may be used as dermal fillers.