Drug Nanoparticle Coating on Microparticles for Solubility Enhancement
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Solution Overview
Problem
Poor water solubility of small-molecule drugs poses a significant challenge in drug formulation, with over 70% of new chemical entities and 40% of marketed drugs exhibiting low solubility, hindering effective therapeutic applications.
Innovation Solution
A method involving vaporizing a therapeutic agent at a predetermined temperature under vacuum pressure to form a vapor, which is then deposited on the surface of a microparticle comprising a pharmaceutically acceptable excipient at a controlled agitation speed and temperature, forming nanoparticles that coat the microparticle surface.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If particle size reduction is used to enhance solubility, then water solubility is improved, but manufacturing complexity increases
Solution Approach 1:
The patent replaces mechanical particle size reduction methods with vapor deposition technology. The therapeutic agent is vaporized and deposited onto microparticle surfaces under controlled vacuum conditions, forming nanoparticles without mechanical grinding or milling processes. This substitution resolves the contradiction by achieving fine particle size (enhanced solubility) through a chemical/physical vapor phase process rather than mechanical means, thereby reducing manufacturing complexity.
Solution Approach 2:
The patent utilizes phase transition of the therapeutic agent from solid to vapor and back to solid nanoparticulate form on the microparticle surface. By controlling the vaporization and deposition phases under vacuum, the process directly forms solubility-enhancing nanoparticles without mechanical size reduction, resolving the contradiction between achieving fine particle size and maintaining simple manufacturing.
2Quantity of substance
If conventional formulation techniques are used, then manufacturing simplicity is maintained, but solubility enhancement is insufficient
Solution Approach 1:
The patent creates a composite structure where therapeutic agent nanoparticles are deposited on excipient microparticle surfaces. This composite architecture provides superior solubility enhancement compared to conventional single-phase formulations, while the vapor deposition process maintains relative manufacturing simplicity by avoiding complex multi-step procedures. The composite material approach resolves the contradiction by achieving enhanced solubility through structural innovation rather than complex processing.
Solution Approach 2:
The patent replaces conventional mechanical formulation techniques (grinding, milling, mixing) with vapor phase deposition. This substitution achieves superior solubility enhancement through controlled nanoparticle formation on microparticle surfaces, while maintaining manufacturing simplicity by eliminating complex mechanical processing steps and reducing the number of unit operations required.
3Quantity of substance
If nanoparticle formation is achieved through vapor deposition, then solubility and bioavailability are improved, but process parameters complexity increases
Solution Approach 1:
The patent utilizes controlled changes in vapor deposition parameters (temperature, vacuum pressure, deposition rate) to optimize nanoparticle formation on microparticle surfaces. By systematically adjusting these parameters within defined ranges, the process achieves consistent solubility and bioavailability enhancement while managing process complexity through parameter optimization rather than adding process steps. This resolves the contradiction by achieving superior bioavailability through controlled parameter variation.
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
Enhances the solubility of poorly soluble drugs by creating a coated particle with nanoparticles, improving therapeutic efficacy and formulation efficiency.
Implementation Method 1
vaporizing the therapeutic agent at a first predetermined temperature under a predetermined vacuum pressure to form a vapor
Implementation Method 2
depositing the vapor on the surfaces of the microparticles at a predetermined agitation speed and a second predetermined temperature under the predetermined vacuum pressure to form the nanoparticles on the surfaces of the microparticles
Implementation Method 3
depositing the vapor on the surfaces of the microparticles at a predetermined agitation speed
Data Source
AI summary
Provided herein is a coated particle comprising: (i) a microparticle that comprises a pharmaceutically acceptable excipient and (ii) nanoparticles of a therapeutic agent, wherein the surface of the microparticle is coated with the nanoparticles. Also provided herein is a pharmaceutical composition comprising the coated particle. Furthermore, provided herein are methods of their preparation.