Microneedle Array Coated with Submicron Particles for Uniform Drug Loading

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Microneedle arrays coated with poorly water-soluble or water-insoluble particles face challenges in achieving consistent drug loading and maintaining puncturability due to surface roughness and variation in drug amount, which is not suitable for pharmaceutical formulations.

Innovation Solution

A microneedle array is developed with microneedles coated using a composition comprising poorly water-soluble or water-insoluble particles with a mean particle size of 1 μm or less, 60% by weight of water, and 2% to 20% by weight of a binding agent, such as saccharides or polyvinyl alcohol compounds, ensuring smooth surfaces and sharp tips for consistent drug loading.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If a solution comprising poorly water-soluble or water-insoluble particles is coated on microneedles, then the microneedles can be loaded with such particles, but the microneedle surface becomes rough and the amount of drug loaded varies significantly

Engineering Contradiction:
Improveamount of particle loadedVSAvoidreproducibility of drug loading
Core Design Contradiction:
Quantity of substanceVSManufacturing precision

Solution Approach 1:

The patent applies parameter changes by controlling the particle size of poorly water-soluble or water-insoluble particles to be 1 μm or less. This size parameter control ensures that particles can be uniformly distributed in the coating solution and evenly deposited on microneedle surfaces, achieving both adequate drug loading quantity and high reproducibility without causing surface roughness

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies local quality by ensuring uniform distribution of particles across the microneedle array surface. By controlling particle size and using appropriate binding agents, the coating achieves homogeneous local quality throughout the array, preventing both surface roughness and variation in drug loading amounts across different microneedles

Inventive Principle:
Principle #3Local quality

2Quantity of substance

If the microneedle surface is roughened by coating, then particles can be loaded, but the puncturability of microneedles is reduced and coated drug may be removed when punctured into skin

Engineering Contradiction:
Improveparticle loading capacityVSAvoidpuncturability
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent applies parameter changes by strictly controlling particle size to be 1 μm or less. This size parameter ensures that particles do not create surface roughness that would compromise puncturability, while still providing adequate loading capacity. The small particle size allows smooth surface coating that maintains microneedle sharpness and puncture performance

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies composite materials by combining particles with specific binding agents (such as hydroxypropyl cellulose, sodium carboxymethyl cellulose, trehalose, or sucrose) to form a coating composition. This composite approach ensures particles are firmly attached to microneedle surfaces without creating roughness, maintaining both loading capacity and puncturability

Inventive Principle:
Principle #40Composite materials

3Ease of manufacture

If additives are used to improve coating solution properties, then flowability and drying properties can be enhanced, but the type of additives is limited due to compatibility requirements with drugs and safety requirements

Engineering Contradiction:
Improvecoating processabilityVSAvoidadditive selection range
Core Design Contradiction:
Ease of manufactureVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by optimizing the particle size parameter to 1 μm or less and controlling the binding agent content at 2-20% by weight. These parameter optimizations provide the coating solution with adequate flowability and drying properties without requiring additional additives, thus maintaining broad compatibility and safety while achieving good coating processability

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses binding agents as intermediaries between particles and microneedle surfaces. The binding agents (such as hydroxypropyl cellulose, sodium carboxymethyl cellulose, trehalose, or sucrose) mediate the attachment process, providing coating processability and ensuring firm particle attachment without requiring additional additives that might have compatibility or safety issues

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 approach results in a microneedle array with reduced variation in drug loading and improved puncturability, making it suitable for pharmaceutical applications.

Implementation Method 1

a microneedle array having microneedles coated with a composition comprising a poorly water-soluble or water-insoluble particle with a mean particle size of 1 μm or less, 2% to 20% by weight of a binding agent

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 2

60% by weight or more of water, and 2% to 20% by weight of a binding agent

Methodology Applied
Scientific EffectDispersion: Dispersion (of waves)

Data Source

PatentUS20230414912A1Microneedle Array Coated with Composition Containing Particles
Publication Date: 2023.12.28 MEDRX CO LTD
  • US20230414912A1 patent drawing
  • US20230414912A1 patent drawing

AI summary

The present invention provides a microneedle array having microneedles coated with a composition comprising a poorly water-soluble or water-insoluble particle with a mean particle size of 1 μm or less, 2% to 20% by weight of a binding agent and 60% by weight or more of water in which the poorly water-soluble or water-insoluble particle is loaded on the microneedles in equal amounts that shows good puncturability.