Nanoparticle Pharmaceutical Coating for Solubility

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Solution Overview

Problem

Existing pharmaceutical formulations face challenges in enhancing the bioavailability and solubility of therapeutic agents, which are crucial for effective disease treatment.

Innovation Solution

A process involving milling a pharmaceutical composition in a ball milling apparatus to produce nanoparticle form, followed by coating with one or more polymers, to enhance bioavailability and solubility.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If the particle size of the pharmaceutical composition is reduced to nanoparticle form, then the solubility and bioavailability of the therapeutic agent is significantly increased, but the manufacturing complexity and equipment requirements are increased

Engineering Contradiction:
Improvesolubility and bioavailability of therapeutic agentVSAvoidmanufacturing equipment and process complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The pharmaceutical composition is segmented into nanoparticle form through ball milling, dividing the bulk material into numerous fine particles. This segmentation dramatically increases the total surface area and solubility of the therapeutic agent while maintaining the same chemical composition, thereby resolving the contradiction between particle size reduction and manufacturing feasibility

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent introduces an intermediary coating layer around the nanoparticles to stabilize them and prevent aggregation. This coating acts as a mediator that maintains nanoparticle dispersion and solubility benefits while enabling practical manufacturing and storage, thus resolving the complexity issue associated with nanoparticle production

Inventive Principle:
Principle #24Intermediary (Mediator)

2Area of stationary object

If ball milling is used to reduce particle size to nanoparticle form, then the surface area and solubility are dramatically increased, but the energy consumption and processing time are increased

Engineering Contradiction:
Improvesurface area of pharmaceutical compositionVSAvoidenergy consumption during milling
Core Design Contradiction:
Area of stationary objectVSUse of energy by moving object

Solution Approach 1:

The ball milling process is designed with preliminary considerations for energy efficiency, including optimizing ball size distribution, mill speed, and milling time to achieve nanoparticle formation with minimal energy input. The process parameters are pre-optimized to reach the desired nanoparticle size range without excessive energy consumption or prolonged processing time

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent employs parameter changes during the milling process, such as varying mill speed, ball-to-powder ratio, and milling duration, to achieve efficient nanoparticle formation. By dynamically adjusting these parameters, the process maximizes surface area generation while minimizing energy consumption and processing time

Inventive Principle:
Principle #35Parameter changes

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 process significantly increases the bioavailability and solubility of therapeutic agents by 2 to 20 folds, leading to improved therapeutic outcomes.

Implementation Method 1

milling a pharmaceutical composition in a ball milling apparatus to produce a nanoparticle form of the pharmaceutical composition

Methodology Applied
Scientific EffectMechanical force: Mechanical Force

Implementation Method 2

coating the nanoparticle form of the pharmaceutical composition with one or more polymers

Methodology Applied
Scientific EffectAdsorption: Adsorption

Data Source

PatentUS12268786B2Methods of improving the solubility and bioavailability of therapeutic agents
Publication Date: 2025.04.08 MM LAB INC
  • US12268786B2 patent drawing
  • US12268786B2 patent drawing
  • US12268786B2 patent drawing

AI summary

This invention relates to methods of preparing nanotherapeutic compounds and compositions comprising nanotherapeutic compounds. The nanotherapeutic compounds prepared according to the methods provided herein are useful for the treatment of disease, for example, cancer, in a subject in need thereof.