pH-Responsive Polymer for Tumor-Specific Drug Delivery

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Existing polymers with stealth properties for drug delivery suppress interactions with both normal tissue and tumor tissue, leading to inefficient drug accumulation and incorporation in cancer cells.

Innovation Solution

A pH-responsive polymer that remains electrically neutral at pH above 7 but becomes cationic at pH 7 or lower, specifically interacting with tumor tissue while avoiding normal tissue, is developed. This polymer is biocompatible, biodegradable, and includes groups such as carboxyl, sulfo, or phosphonic groups, with a weight-average molecular weight of 1,000 to 200,000, allowing efficient drug delivery to tumor sites.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a stealth polymer (e.g., PEG) is used to suppress interaction with blood components and normal tissue, then blood retention and toxicity suppression are improved, but drug accumulation and incorporation into tumor tissue deteriorate

Engineering Contradiction:
Improveblood retention and toxicity suppressionVSAvoiddrug accumulation and incorporation into tumor tissue
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The polymer's charge state is made dynamic and pH-dependent. At physiological pH (7.4), the polymer maintains a neutral state for stealth properties. At tumor tissue pH (6.5-6.8), the polymer transitions to a cationic state to enhance cellular uptake. This dynamic charge transition resolves the contradiction between stealth and tumor accumulation.

Inventive Principle:
Principle #15Dynamics

Solution Approach 2:

The invention changes the charge parameter of the polymer based on pH conditions. By incorporating pH-responsive groups (carboxyl, sulfo, or phosphonic groups) that transition from neutral to cationic at lower pH, the polymer adapts its electrostatic properties to different microenvironments, achieving both stealth in blood and enhanced accumulation in tumor tissue.

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If a polymer maintains electrical neutrality to avoid interaction with normal tissue, then biocompatibility is improved, but interaction with and incorporation into tumor cells deteriorates

Engineering Contradiction:
Improveinteraction with normal tissueVSAvoidincorporation into tumor cells
Core Design Contradiction:
Object-affected harmful factorsVSProductivity

Solution Approach 1:

The polymer exhibits different charge qualities in different locations (pH environments). In normal tissue (pH 7.4), it maintains neutrality to minimize harmful interactions. In tumor tissue (pH 6.5-6.8), it becomes cationic to enhance cellular incorporation. This local quality differentiation resolves the contradiction between biocompatibility and tumor cell uptake.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention exploits the harmful acidic microenvironment of tumor tissue (pH 6.5-6.8) as a beneficial trigger. The low pH that characterizes tumor pathology is converted into a signal that activates the polymer's cationic state, enhancing tumor cell uptake while maintaining neutrality in normal physiological conditions.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

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 pH-responsive polymer effectively accumulates and incorporates drugs into tumor cells while minimizing damage to normal tissues, enhancing the stealth property and drug delivery efficiency to tumor tissues.

Implementation Method 1

a group which is electrically neutral under pH environments of more than 7 and which changes to be cationic at pH 7 or less

Methodology Applied
Scientific EffectpH-responsive charge transition:

Data Source

PatentUS11890347B2PH-responsive polymer and drug delivery system
Publication Date: 2024.02.06 TOKYO INST OF TECH
  • US11890347B2 patent drawing
  • US11890347B2 patent drawing
  • US11890347B2 patent drawing

AI summary

A pH-responsive polymer formed of a biocompatible polymer to which a group which is electrically neutral under pH environments of more than 7 and which changes to be cationic at pH 7 or less is bonded.