Mixed Butyric-Formic Esters of Acid Polysaccharides

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Solution Overview

Problem

Current cosmetic and dermatological applications of hyaluronic acid and other glycosaminoglycans lack effective derivatives that provide simultaneous moisturizing, elasticizing, and protective properties against enzymatic degradation and radiation-induced skin damage, with limited use of hydroxyl esters with organic acids.

Innovation Solution

Development of mixed butyric-formic esters of acid polysaccharides, specifically hyaluronic acid, chondroitin sulfate, dermatan sulfate, and heparan sulfate, through a process involving dissolution in formamide, reaction with butyric anhydride and a base, followed by purification and freeze-drying, which introduces butyrate and formate residues, enhancing their chemico-physical and biological characteristics.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If hyaluronic acid is used in native form for cosmetic moisturizing, then moisturizing effect is achieved, but resistance to enzymatic degradation is insufficient

Engineering Contradiction:
Improveresistance to enzymatic degradationVSAvoidchemical modification complexity
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of hyaluronic acid through esterification at hydroxyl groups with butyric and formic acids. This changes the molecular parameters (adding ester groups) to improve enzymatic resistance while maintaining the base polymer structure, resolving the contradiction between enhanced reliability and manufacturing complexity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite derivatives by combining hyaluronic acid with butyric and formic acid esters. This composite structure integrates the moisturizing properties of HA with the degradation resistance of ester groups, achieving both improved reliability and controlled manufacturability through the specific synthesis process

Inventive Principle:
Principle #40Composite materials

2Strength

If crosslinking agents are used to improve viscoelasticity, then elasticizing effect is enhanced, but product complexity increases

Engineering Contradiction:
ImproveviscoelasticityVSAvoidproduct formulation complexity
Core Design Contradiction:
StrengthVSDevice complexity

Solution Approach 1:

The patent modifies the viscoelastic parameters of hyaluronic acid through esterification rather than crosslinking. By changing the chemical parameters (adding butyrate and formate esters at hydroxyl groups), the patent achieves enhanced elasticizing effects without introducing external crosslinking agents, thus improving strength while controlling product complexity

Inventive Principle:
Principle #35Parameter changes

3Reliability

If hydroxyl esters with organic acids are synthesized, then enzymatic degradation resistance improves, but manufacturing process complexity increases

Engineering Contradiction:
Improveenzymatic degradation resistanceVSAvoidsynthesis process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent systematically changes the chemical parameters of hyaluronic acid by esterifying hydroxyl groups with specific organic acids (butyric and formic). This parameter change approach improves enzymatic degradation resistance through controlled chemical modification, managing synthesis complexity through a defined two-step process

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses an intermediary approach by first dissolving hyaluronic acid in formamide, then sequentially adding base followed by butyric anhydride. This intermediary solvent system and stepwise addition method facilitates the esterification process, improving enzymatic resistance while managing synthesis complexity through controlled reaction conditions

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 resulting derivatives exhibit improved resistance to enzymatic degradation, significant elasticizing and moisturizing effects, and protective benefits against radiation-induced dermatitis, demonstrated through in vivo studies and instrumental measurements, offering a versatile solution for skin treatments and cosmetic applications.

Implementation Method 1

the acid polysaccharide derivatives are obtained by a process that comprises: a) dissolving the acid polysaccharide, salified with sodium or other alkali metals, in formamide by heating; b) adding to the resulting solution, at room temperature, an organic base, followed, after 15 minutes, by butyric anhydride

Methodology Applied
Scientific EffectEsterification: Chemical Bonding

Implementation Method 2

purifying the dilute reaction mixture by dialysis or tangential filtration

Methodology Applied
Scientific EffectDialysis: Semipermeable Membrane

Implementation Method 3

purifying the dilute reaction mixture by dialysis or tangential filtration

Methodology Applied
Scientific EffectTangential filtration: Filter (physical)

Implementation Method 4

freezing the purified polysaccharide solution and recovering the product by freeze-drying or spray-drying

Methodology Applied
Scientific EffectFreezing: Freezing

Implementation Method 5

recovering the product by freeze-drying or spray-drying

Methodology Applied
Scientific EffectFreeze-drying: Freeze Drying

Data Source

PatentEP2222713B1Mixed butyric-formic esters of acid polysaccharides, and their preparation and use as skin cosmetics
Publication Date: 2018.01.10 SIGEA SRL
  • EP2222713B1 patent drawingFigure 1~2

AI summary

Disclosed are acid polysaccharides characterised by the concomitant presence of alcohol groups esterified with butyric and formic acids.