Microneedle Array With Localized Medicament Concentration

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Solution Overview

Problem

Current methods for administering medications, such as injections and topical applications, face challenges in achieving sufficient drug efficacy due to barriers like the horny layer of the skin and are often associated with pain or infection risks, especially in larger animals where skin thickness complicates effective delivery.

Innovation Solution

A microneedle array with a sheet portion and needles, where the needle tips contain a high concentration of medicament and a water-soluble polymer, occupying at least 50% of the needle's mass, to enhance puncture properties and drug efficacy, allowing for efficient administration through the skin.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If a microneedle array with high water-soluble polymer content (≥50%) is used to improve puncture properties, then the needle flexibility and skin penetration ability improve, but the structural strength and stability during handling may deteriorate

Engineering Contradiction:
Improvepuncture propertiesVSAvoidneedle structural strength
Core Design Contradiction:
Ease of operationVSStrength

Solution Approach 1:

The patent optimizes the water-soluble polymer content to be 50% or more of the total needle mass, which provides sufficient flexibility for skin penetration while maintaining adequate structural integrity. This parameter optimization resolves the contradiction by finding the optimal balance point where the needle is soft enough to penetrate skin easily but strong enough to maintain its shape during handling and insertion.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If the needle tip region contains high concentration of medicament to improve drug efficacy, then the therapeutic effect improves, but the manufacturing precision and uniformity of drug distribution may deteriorate

Engineering Contradiction:
Improvedrug efficacyVSAvoidmedicament distribution uniformity
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The patent concentrates the medicament in the needle tip region (the region 20% height from the needle tip) rather than uniformly distributing it throughout the entire needle. This local concentration strategy ensures high drug efficacy at the administration site while the manufacturing process controls the overall distribution uniformity. The local quality principle allows different regions of the needle to have different functions: the tip region for drug delivery and the shaft region for structural support.

Inventive Principle:
Principle #3Local quality

3Reliability

If the water-soluble polymer content is increased to enhance solubility and drug release, then the drug dissolution and absorption improve, but the needle manufacturing complexity and process control difficulty increase

Engineering Contradiction:
ImprovesolubilityVSAvoidmanufacturing process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent specifies that water-soluble polymer should constitute 50% or more of the total needle mass, which ensures sufficient solubility and drug release performance. This clear parameter specification simplifies the manufacturing process by providing a definitive guideline for formulation, reducing the need for complex trial-and-error optimization while maintaining reliable drug dissolution and absorption characteristics.

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 microneedle array achieves high drug efficacy similar to subcutaneous injection by improving puncture properties and solubility, ensuring effective medicament delivery and minimizing pain and infection risks, particularly in larger animals.

Implementation Method 1

a self-dissolving microneedle array that uses a substance having solubility in vivo as a base material... the base material being self-dissolved during insertion of microneedles into the skin

Methodology Applied
Scientific EffectDissolution: Solvation

Implementation Method 2

microneedles penetrating a horny barrier layer using a microneedle array in which microneedles (needle-like projections) which contain a medicament

Methodology Applied
Scientific EffectMechanical penetration: Mechanical Force

Data Source

PatentEP3348256B1Microneedle array
Publication Date: 2020.10.21 FUJIFILM CORP
  • EP3348256B1 patent drawingFigure 1
  • EP3348256B1 patent drawingFigure 2A~2C
  • EP3348256B1 patent drawingFigure 3~5

AI summary

An object of the present invention is to provide a microneedle array which is formed of a sheet portion and needles and is capable of achieving high drug efficacy. According to the present invention, provided is a microneedle array including: a sheet portion; and a plurality of needles present on an upper surface of the sheet portion, in which the needle contains a water-soluble polymer and a medicament, the water-soluble polymer occupies 50% by mass or greater of the total solid content of the needle, the water-soluble polymer and the medicament are present at a mass ratio of Formula 1, in a needle tip region which includes a needle tip of each needle and has a height corresponding to 20% of the total height of each needle, and the sheet portion contains a water-soluble polymer. water−soluble polymer:medicament=0.05 to 0.9:1