Soluble Microneedle Delivery for Transdermal Neurotransmitter Control

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Solution Overview

Problem

Current methods for delivering drugs and cosmetics through the skin face challenges due to the skin's low penetrability, particularly for polyphenols and calcium channel blockers, which have limited solubility and poor skin penetration, making it difficult to achieve effective wrinkle-improving effects without pain or side effects.

Innovation Solution

A soluble microneedle system containing polyphenols or calcium channel blockers, made from water-soluble polymers like hyaluronic acid and saccharides, that dissolves in the skin, allowing for stable delivery of these ingredients to modulate neurotransmitter release and improve skin wrinkles without pain.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If polyphenols or calcium channel blockers are included in cosmetic formulations, then wrinkle-improving effect is achieved by modulating neurotransmitter release, but skin penetrability is poor due to low solubility and the skin's barrier structure

Engineering Contradiction:
Improvewrinkle-improving effectVSAvoidskin penetrability
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The cosmetic composition is segmented into multiple functional components including water-soluble polymers (hyaluronic acid, carboxymethyl cellulose), saccharides (trehalose, sucrose), and active ingredients (polyphenols, calcium channel blockers). This segmentation allows each component to perform its specific function - the polymers and saccharides enhance solubility and penetration while the active ingredients provide the wrinkle-improving effect, thereby resolving the contradiction between poor skin penetrability and desired therapeutic effect.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs composite material formulation by combining water-soluble polymers, saccharides, and active ingredients in a synergistic composition. The water-soluble polymers and saccharides form a composite delivery system that enhances the solubility and skin penetrability of the hydrophobic active ingredients (polyphenols and calcium channel blockers), enabling effective delivery while maintaining the wrinkle-improving effect.

Inventive Principle:
Principle #40Composite materials

2Reliability

If the concentration of polyphenols or calcium channel blockers is increased to achieve better wrinkle-improving effect, then efficacy is improved, but solubility decreases making formulation difficult

Engineering Contradiction:
ImproveefficacyVSAvoidsolubility
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

Water-soluble polymers (hyaluronic acid, carboxymethyl cellulose) and saccharides (trehalose, sucrose) serve as intermediary substances that enhance the solubility of hydrophobic active ingredients. These intermediaries form solubilizing complexes with polyphenols and calcium channel blockers, allowing higher concentrations of active ingredients to be incorporated into the cosmetic formulation while maintaining adequate solubility and stability.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If transdermal injection is used to deliver calcium channel blockers to the muscular layer, then muscle contraction is effectively reduced, but pain and limited applicability occur

Engineering Contradiction:
Improvemuscle relaxation effectVSAvoidpain and applicability
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent replaces the mechanical injection system with a topical cosmetic formulation system. Instead of using needles and mechanical force to deliver calcium channel blockers into the muscular layer, the invention uses a chemically formulated cosmetic composition that can be applied topically. The water-soluble polymers and saccharides facilitate penetration of the active ingredient through the skin barrier, achieving muscle relaxation without the pain and limitations of injection.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

4Reliability

If oral administration is used to deliver calcium channel blockers, then muscle contraction is reduced, but side effects occur due to whole body exposure

Engineering Contradiction:
Improvemuscle relaxation effectVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The cosmetic composition enables localized delivery of calcium channel blockers to the facial skin and underlying muscles. The formulation is designed for topical application, creating a local high concentration of the active ingredient at the target site (facial muscles) while minimizing systemic absorption. This local quality approach achieves muscle relaxation effect without the whole-body exposure and associated side effects of oral administration.

Inventive Principle:
Principle #3Local quality

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 soluble microneedle system significantly enhances skin penetrability, delivering active ingredients effectively to improve wrinkles and lines on the face, achieving a higher concentration of polyphenols and calcium channel blockers compared to traditional cosmetic compositions, thereby relaxing muscles and reducing muscle contraction.

Implementation Method 1

A soluble microneedle system containing polyphenols or calcium channel blockers, made from water-soluble polymers like hyaluronic acid and saccharides, that dissolves in the skin

Methodology Applied
Scientific EffectSolubility: Solvation

Implementation Method 2

Through diffusion, only small molecules with molecular weights of 500 Da or smaller can be delivered into the skin

Methodology Applied
Scientific EffectDiffusion: Diffusion

Data Source

PatentUS11577063B2Soluble microneedle containing ingredient for controlling release of neurotransmitters
Publication Date: 2023.02.14 LG HOUSEHOLD & HEALTH CARE LTD
  • US11577063B2 patent drawing
  • US11577063B2 patent drawing
  • US11577063B2 patent drawing

AI summary

The present invention relates to a skin administration system capable of improving the efficiency of skin delivery of an ingredient for controlling release of neurotransmitters and, particularly, to a microneedle containing an ingredient for controlling release of neurotransmitters.