Therapeutic Agent Nanoparticle Coating via Vacuum Vapor Deposition
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Poor water solubility of small-molecule drugs poses a significant challenge in drug formulation, with existing techniques failing to effectively enhance solubility for therapeutic applications.
Innovation Solution
A method involving vaporizing a therapeutic agent at a predetermined temperature under vacuum pressure and depositing the vapor onto the surface of a microparticle excipient to form nanoparticles, creating a coated particle with enhanced solubility.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional formulation techniques (particle size reduction, crystal engineering, salt formation, solid dispersion, surfactant use, complexation) are used to enhance solubility, then some solubility improvement may be achieved, but poor water solubility remains a major hurdle and therapeutic efficacy is insufficient
Solution Approach 1:
The drug substance is segmented into nanoscale particles (1-100 nm) through vapor deposition, creating numerous small particles that dramatically increase surface area and improve solubility. This segmentation approach transforms the bulk drug into a nanodispersed system with enhanced dissolution characteristics.
Solution Approach 2:
The invention changes the physical state and size parameters of the drug by depositing it as nanoparticles onto microparticle surfaces. This parameter transformation from bulk solid to nanoscale coating fundamentally alters solubility properties and dissolution rate, enabling therapeutic efficacy for previously insoluble drugs.
2Quantity of substance
If the therapeutic agent is vaporized and deposited to form nanoparticles, then solubility is enhanced, but the process requires vacuum equipment and temperature control
Solution Approach 1:
The invention replaces conventional mechanical mixing and wet coating methods with vapor-phase deposition. This substitution uses thermal energy and vacuum conditions to directly deposit drug nanoparticles onto excipient surfaces, eliminating the need for solvents and complex mechanical processing equipment.
Solution Approach 2:
The process exploits phase transitions of the therapeutic agent by vaporizing it under vacuum and then condensing it onto microparticle surfaces. This phase change mechanism (solid/liquid → vapor → solid nanoparticle coating) enables direct formation of nanodispersed drug layers without mechanical intervention.
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 method results in coated particles with improved solubility, addressing the solubility issues of poorly soluble drugs and enhancing their therapeutic efficacy.
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
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.