Mesoscale Colloidal Particle Hydrotrope Shell for Drug Solubility

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Solution Overview

Problem

Poorly water-soluble drugs face challenges in bioavailability and formulation due to limited solubility, requiring expensive and time-consuming methods like micronization, and existing stabilization methods often involve undesirable additives like surfactants and polymers.

Innovation Solution

The development of mesoscale colloidal particles with a hydrophobe-rich core surrounded by a hydrogen-bonded outer shell containing hydrotrope molecules, which enhances solubility without the need for surfactants or polymers, using a method that involves mixing water, hydrotrope, and hydrophobic organic molecules to form stable aqueous solutions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If traditional stabilization methods (surfactants, polymers, charged particles) are used to stabilize colloidal dispersions, then layer separation is prevented, but the formulation becomes more complex and expensive

Engineering Contradiction:
Improvecolloidal dispersion stabilityVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent extracts and eliminates the need for traditional stabilizing additives (surfactants, polymers, charged particles) by using pure water as the stabilization medium. The hydrophobic drug molecules themselves, when dissolved in water, form stable colloidal dispersions without requiring external stabilizing agents, thus simplifying the formulation while maintaining stability.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The hydrophobic drug molecules perform the stabilization function themselves through their own molecular structure and interaction with water. The drug molecules arrange themselves to form stable colloidal dispersions, utilizing their inherent properties rather than requiring separate stabilizing components added to the formulation.

Inventive Principle:
Principle #25Self-service

2Quantity of substance

If micronization processes are used to increase solubility of poorly soluble drugs, then drug solubility improves, but the process becomes time-consuming and expensive

Engineering Contradiction:
Improvedrug solubilityVSAvoidprocessing time
Core Design Contradiction:
Quantity of substanceVSLoss of time

Solution Approach 1:

The patent changes the fundamental parameter of drug delivery from solid particles (requiring micronization) to dissolved molecular species in water. By transforming the drug from an insoluble solid state to a dissolved state in aqueous solution, the need for mechanical size reduction processes is eliminated, achieving both high solubility and rapid preparation.

Inventive Principle:
Principle #35Parameter changes

3Stability of the object's composition

If charged particles, polymers, or surfactants are added to stabilize colloids, then layer separation is avoided, but the product contains undesirable additives

Engineering Contradiction:
Improvecolloidal dispersion stabilityVSAvoidundesirable additives
Core Design Contradiction:
Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The patent removes all undesirable additives (charged particles, polymers, surfactants) from the formulation by using pure water as the dispersion medium. The stabilization is achieved through the inherent properties of water and the molecular structure of the drug itself, eliminating the need for external additives that could cause harmful effects.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The system uses only the components already present (water and hydrophobic drug molecules) to achieve stabilization. The drug molecules themselves provide the stabilization function through their molecular structure and interaction with water, rather than requiring separate stabilizing additives that could be harmful.

Inventive Principle:
Principle #25Self-service

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

This approach significantly increases the solubility of poorly soluble drugs, stabilizes colloidal dispersions, and allows for effective drug delivery and formulation without the need for costly stabilization processes, providing a cost-effective and stable solution for pharmaceutical and industrial applications.

Implementation Method 1

The outer shell includes water and at least one hydrotrope wherein the hydrotrope molecules form hydrogen bonds with water molecules

Methodology Applied
Scientific EffectHydrogen bonding: Chemical Bonding

Implementation Method 2

Hydrotropy is a molecular phenomenon whereby adding a second solute (the hydrotrope) results in an increase in the aqueous solubility of poorly soluble solutes

Methodology Applied
Scientific EffectHydrotropy: Solvation

Data Source

PatentUS11406595B2Highly stable colloid from aqueous solutions of small organic molecules
Publication Date: 2022.08.09 UNIV OF MARYLAND
  • US11406595B2 patent drawing
  • US11406595B2 patent drawing
  • US11406595B2 patent drawing

AI summary

The present invention is related to a mesoscale colloidal particle including a hydrophobe-rich core surrounded by hydrogen bonded outer shell. The outer shell includes water and at least one hydrotrope wherein the hydrotrope molecules form hydrogen bonds with water molecules. The invention is also related to an aqueous solution including at least one mesoscale colloidal particle as well as methods of making and using such mesoscale colloidal particles and their solutions.