Golf-Ball Microparticle Structure for Stable Dry Powder Inhalation

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Solution Overview

Problem

Existing dry powder inhaler systems face challenges in achieving uniform and homogeneous deposition of active pharmaceutical ingredients (APIs) throughout the lungs, with issues related to flight stability, Fine Particle Fraction, and increased stickiness, particularly in formulations using deflated-ball like microparticles.

Innovation Solution

The development of golf-ball like microparticles with a core-shell structure, featuring a carrier shell and API core, and characterized by symmetrical golf-ball like surface depressions, enhances aerodynamic stability and reduces stickiness, resulting in improved Fine Particle Fraction and uniform lung deposition.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Device complexity

If deflated-ball like microparticles are used in dry powder inhaler systems, then the particle morphology is simplified, but flight stability deteriorates and Fine Particle Fraction decreases

Engineering Contradiction:
Improveparticle morphology complexityVSAvoidflight stability
Core Design Contradiction:
Device complexityVSReliability

Solution Approach 1:

The patent applies spheroidality by designing microparticles with a spherical core structure rather than deflated-ball morphology. This spherical geometry provides superior aerodynamic properties and flight stability during inhalation delivery, directly resolving the contradiction between morphological simplicity and flight reliability.

Inventive Principle:
Principle #14Spheroidality (Curvature)

2Ease of manufacture

If deflated-ball like microparticles are used, then manufacturing is simpler, but Fine Particle Fraction is reduced

Engineering Contradiction:
Improvemicroparticle fabricationVSAvoidFine Particle Fraction
Core Design Contradiction:
Ease of manufactureVSManufacturing precision

Solution Approach 1:

The patent employs nested doll principle by creating a core-shell structure where a spherical core containing the API is nested within a carrier shell. This nested architecture enables precise control over particle size distribution and generates the required Fine Particle Fraction while maintaining manufacturability through controlled aggregation of spherical units.

Inventive Principle:
Principle #7Nested doll (Nesting)

3Quantity of substance

If conventional dry powder systems with lactose carriers are used, then API delivery is achieved, but uniform deposition throughout the lungs is limited to around 30%

Engineering Contradiction:
ImproveAPI deliveryVSAvoiduniformity of deposition
Core Design Contradiction:
Quantity of substanceVSManufacturing precision

Solution Approach 1:

The patent applies local quality principle by engineering the carrier shell with specific local characteristics including surface charge distribution, porosity gradients, and functional group placement. These localized variations in carrier properties enhance API release patterns and promote uniform deposition throughout different lung regions, overcoming the limitation of conventional lactose carriers.

Inventive Principle:
Principle #3Local quality

4Adaptability or versatility

If rough particle surfaces with projections and pores are created, then cell and tissue interactions are enhanced, but particle stickiness increases

Engineering Contradiction:
Improvecell and tissue interactionVSAvoidparticle stickiness
Core Design Contradiction:
Adaptability or versatilityVSObject-generated harmful factors

Solution Approach 1:

The patent employs flexible shells and thin films principle by creating a thin, controlled-carrier shell that encapsulates the spherical API core. This shell provides a balanced surface that enables adequate cell and tissue interactions while maintaining low stickiness through controlled surface properties and preventing excessive aggregation during inhalation.

Inventive Principle:
Principle #30Flexible shells and thin films

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 golf-ball like microparticles demonstrate enhanced flight stability and increased Fine Particle Fraction, leading to more effective and uniform delivery of APIs to the lungs, particularly for treating respiratory diseases such as asthma, COPD, pulmonary fibrosis, pneumonia, and lung cancer.

Implementation Method 1

spray-drying of a liquid formulation

Methodology Applied
Scientific EffectEvaporation: Evaporation

Implementation Method 2

obtained by atomization of nanosuspensions of nanoparticles or solutions

Methodology Applied
Scientific EffectAtomization:

Data Source

PatentEP4729051A2Golf ball-like microparticles for use in the treatment and prevention of pulmonary diseases
Publication Date: 2026.04.22 AQUILON PHARMA
  • EP4729051A2 patent drawingFigure 1A~2
  • EP4729051A2 patent drawingFigure 3~5
  • EP4729051A2 patent drawingFigure 6~7

AI summary

The present invention relates to a method to prepare golf ball like microparticles by spray drying of nanosuspensions of nanoparticles or solutions for dry powder inhalers for use in the treatment and prevention of pulmonary diseases.