Surface-Modified Nanoparticles for Dry Powder Inhalation
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Solution Overview
Problem
Current pharmaceutical compositions in powder form face challenges in achieving efficient and efficacious delivery to the lungs due to particle size and deagglomeration issues, with existing methods requiring additional energy to release drugs from carrier particles and limited efficiency below 5 microns in aerodynamic diameter.
Innovation Solution
Treating active and inactive ingredients with surface-modified nanoparticles to enhance the delivery efficiency of dry powder pharmaceutical compositions, allowing for a higher respirable fraction and reproducible metering, even with a large proportion of inactive ingredient, thereby improving lung deposition.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If drug particles are made smaller than 5 microns to improve lung deposition, then lung deposition efficiency is improved, but deagglomeration efficiency declines markedly
Solution Approach 1:
The patent divides the powder composition into two distinct particle size populations: fine drug particles (<5 microns) for lung deposition and larger carrier particles (5-20 microns) for structural integrity and deagglomeration. This segmentation allows each particle type to fulfill its specific function without compromising the other.
Solution Approach 2:
The patent embeds fine drug particles within or onto the surface of larger carrier particles, creating a core-shell or surface-coated structure. This nesting allows the fine particles to be protected and controlled, releasing them only under appropriate conditions in the respiratory tract.
2Reliability
If larger inert carrier particles are used to provide bulk deagglomeration, then deagglomeration is improved, but additional energy is required to release the drug from the carrier particle surface
Solution Approach 1:
The patent applies different surface properties to different regions of the carrier particles. The outer surface is modified with surfactants or coatings that reduce adhesion strength and facilitate easy drug release, while the core maintains structural integrity for effective deagglomeration.
Solution Approach 2:
The patent modifies surface parameters of the carrier particles by applying surfactant coatings or surface treatments that change the surface energy, wettability, and adhesion characteristics. This reduces the binding strength between drug particles and carrier surfaces, enabling easier release with less energy input.
3Measurement precision
If a large proportion of inactive ingredient is used to enable reproducible metering, then metering precision is improved, but the proportion of active ingredient that can be delivered is reduced
Solution Approach 1:
The patent creates a composite powder system where inactive carrier particles and active drug particles are combined in a specific ratio and structure. The composite structure ensures that even with high carrier content, the drug particles are efficiently delivered through controlled deagglomeration and release mechanisms.
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 use of surface-modified nanoparticles increases the respirable fraction and delivery efficiency by at least 20-75% compared to compositions without nanoparticles, enabling efficient delivery of therapeutic amounts to the lungs while overcoming manufacturing limitations and variability in doses.
Implementation Method 1
mixing the inactive ingredient particles with surface-modified nanoparticles to provide an inactive ingredient comprised of particles having surfaces with the surface-modified nanoparticles deposited on the surfaces
Data Source
AI summary
A method of making a dry powder pharmaceutical composition comprising: providing inactive ingredient particles; providing a micronized active ingredient; mixing the inactive ingredient particles with surface-modified nanoparticles to provide an inactive ingredient comprised of particles having surfaces with the surface-modified nanoparticles deposited on the surfaces; and/or mixing the micronized active ingredient with surface-modified nanoparticles to provide a micronized active ingredient comprised of particles having surfaces with the surface-modified nanoparticles deposited on the surfaces; and then mixing the micronized active ingredient with the inactive ingredient; the dry powder compositions made by the method; a use of said composition for the manufacture of a medicament for being delivered to the lungs of a mammal by administering a therapeutic amount of the dry powder pharmaceutical composition, and a dry powder inhalation device comprising a mouth piece, a powder containment system, and the dry powder pharmaceutical composition are disclosed.