Amorphous Nano-Molecular Aggregates for Lipid Membrane Permeability
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Solution Overview
Problem
Conventional methods for delivering pharmacologically active ingredients across cell membranes face challenges due to low aqueous solubility and hydrophobic membrane permeability, often requiring structural modifications that alter the drug's efficacy and increase production costs, while top-down methods are costly and inefficient, and bottom-up methods are limited to crystalline products.
Innovation Solution
An amorphous nano-molecular association is created by dissolving organic or inorganic materials in a solvent and applying shear stress to form close molecular associations, reducing particle size to 50 nm or less, maintaining the drug's original structure and enhancing hydrophobicity for improved permeability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional encapsulation methods using surfactant/polymer structures are used, then drug delivery is enabled, but the encapsulation process becomes difficult and encapsulation yield decreases
Solution Approach 1:
The invention removes the third material (surfactant/polymer) from the encapsulation system, using only the drug molecule's own structure to form micelles. This eliminates the complex encapsulation process and improves encapsulation yield while maintaining drug delivery capability.
Solution Approach 2:
The drug molecules self-assemble into micellar structures through their own amphiphilic properties without requiring external surfactants or polymers. This self-service mechanism simplifies the manufacturing process and improves encapsulation efficiency.
2Quantity of substance
If hydrophilic drugs are used, then aqueous solubility is improved, but permeability through hydrophobic phospholipid membranes decreases
Solution Approach 1:
The micelle structure segments the drug into a hydrophobic core and hydrophilic exterior. The hydrophobic core accommodates the drug in a way that maintains its lipophilic character for membrane permeation, while the hydrophilic exterior ensures aqueous solubility.
Solution Approach 2:
The micelle creates a composite structure combining hydrophobic and hydrophilic regions, allowing the drug to exhibit both water solubility (through the hydrophilic exterior) and membrane permeability (through the hydrophobic core).
3Reliability
If molecular structure modification is applied to improve solubility or permeability, then drug delivery is enhanced, but the original drug efficacy is altered and production costs increase
Solution Approach 1:
The invention extracts the amphiphilic character from the drug molecule itself rather than adding external modifiers. This eliminates the need for structural modification and associated production costs while maintaining improved drug delivery performance.
Solution Approach 2:
The invention changes the physical state and aggregation behavior of the drug (forming micelles) without altering its chemical structure. This maintains the original drug efficacy while improving delivery performance and avoiding modification costs.
4Length of moving object
If top-down methods such as high pressure homogenization are used, then particle size is reduced, but manufacturing cost increases and product damage occurs
Solution Approach 1:
Instead of using top-down methods to break down particles, the invention uses bottom-up self-assembly where molecules spontaneously form micelles of desired size. This reverses the conventional approach, reducing manufacturing cost and avoiding product damage while achieving nanometer-scale particle sizes.
5Ease of manufacture
If bottom-up methods such as crystal growth are used, then preparation process is simplified, but only crystalline products can be obtained and surfactants are required for excessive crystal growth
Solution Approach 1:
The invention changes the aggregation state from crystalline to amorphous by controlling the self-assembly process. This allows bottom-up preparation without crystalline constraints and eliminates the need for surfactants to control crystal growth, while maintaining process simplicity.
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 increases permeability through the phospholipid membrane, maintains the drug's original efficacy, and reduces production costs by forming amorphous, non-crystalline nanoparticles with enhanced solubility and stability, suitable for nanomedicine applications.
Implementation Method 1
when drug molecules, whether organic, inorganic, or salts thereof, are dissolved in a solvent and brought into close proximity to each other, the polar groups within the molecules interact to form molecular associations
Implementation Method 2
applying a shear stress to an organic/inorganic material or a salt thereof, and thus has excellent solubility and permeability to a lipid membrane
Data Source
AI summary
The present invention relates to an amorphous nano-molecular association composed of an organic/inorganic material or a salt thereof, and more specifically, to an amorphous nano-molecular association, which is prepared by applying a shear stress to an organic/inorganic material or a salt thereof, and thus has excellent solubility and permeability to a lipid membrane.