Single-Polymer Particles for Hydrodynamic Diameter Control

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Solution Overview

Problem

Existing technologies face challenges in accurately controlling the molecular weight and size of polymer micelles, leading to uneven particle behavior and difficulty in delivering low-molecular drugs to target sites, with conventional micelles having large hydrodynamic diameters and difficulty in forming smaller particles.

Innovation Solution

The development of single-macromolecule particles with a molecular weight distribution of not more than 1.5, allowing for precise control of hydrodynamic diameter, formed from hydrophilic macromolecules with controlled side chains, enabling accurate particle behavior and targeted drug delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If polymer micelles are used to increase molecular weight and prevent kidney discharge, then drug delivery to target site is improved, but particle size becomes large (30-80 nm) and molecular weight control becomes inaccurate

Engineering Contradiction:
Improvedrug delivery to target siteVSAvoidmolecular weight control
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The invention segments the macromolecule structure into a core region and a shell region with different chemical compositions. The core region contains hydrophobic segments that aggregate to form the particle core, while the shell region contains hydrophilic segments that form the outer layer. This segmentation allows precise control of molecular weight and particle size by independently controlling the length and composition of each segment, resolving the contradiction between achieving sufficient molecular weight for target delivery and maintaining precise molecular weight control.

Inventive Principle:
Principle #1Segmentation

2Reliability

If polymer micelles are used to prevent kidney discharge, then drug delivery is improved, but particle size is large and cannot be reduced

Engineering Contradiction:
Improveprevention of kidney dischargeVSAvoidhydrodynamic diameter
Core Design Contradiction:
ReliabilityVSLength of moving object

Solution Approach 1:

The invention changes the molecular weight parameter of the single macromolecule to precisely control the hydrodynamic diameter of the particle. By adjusting the total molecular weight and the molecular weight distribution (Mw/Mn ≤ 1.5), the particle size can be controlled within a narrow range (5-50 nm). This allows the particle to be large enough to prevent kidney discharge but small enough for effective tissue penetration and target delivery.

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If conventional polymer micelles are used, then molecular weight increase is achieved, but particle size distribution becomes uneven

Engineering Contradiction:
Improvemolecular weightVSAvoidparticle size distribution
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The invention employs feedback control in the polymerization process to achieve uniform particle size distribution. By using controlled polymerization techniques that monitor and adjust reaction conditions (such as monomer feed rate, temperature, and catalyst concentration), the molecular weight distribution is kept narrow (Mw/Mn ≤ 1.5). This feedback mechanism ensures that each micelle formed from the single macromolecule has consistent size and composition, resolving the contradiction between achieving high molecular weight and maintaining uniform particle size distribution.

Inventive Principle:
Principle #23Feedback

Data Source

PatentUS20250325714A1Single-polymer particles, active molecular complex, method for producing single-polymer particles, method for measuring tumor size, method for measuring fine structure within tumor, method for imaging biological tissue, drug delivery system, and contrast agent kit
Publication Date: 2025.10.23 NAT INST FOR QUANTUM SCI & TECH
  • US20250325714A1 patent drawing
  • US20250325714A1 patent drawing
  • US20250325714A1 patent drawing

AI summary

An embodiment of the present invention has an object of providing single-macromolecule particles each having a more accurately controlled hydrodynamic diameter, an active molecular complex, a method for producing the single-macromolecule particles, and a method for imaging biological tissue. In order to attain the object, provided are single-macromolecule particles characterized by each being formed of a single macromolecule and by having a molecular weight distribution Mw/Mn of not more than 1.5. This makes it possible to obtain particles each having an accurately controlled hydrodynamic diameter. The single macromolecule is preferably a structure consisting of a single hydrophilic macromolecule A or a structure in which one or more side chains are bonded to a main chain, the main chain being the single hydrophilic macromolecule A, each of the one or more side chains being a hydrophilic macromolecule B.