pH-Responsive Block Copolymer for Targeted Immune Cell Drug Delivery

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Solution Overview

Problem

Current anti-cancer therapies, such as chemotherapy and radiotherapy, have poor therapeutic efficiency and cause significant side effects due to non-specific action on the body, while immune cells like T cells and natural killer cells face challenges in effectively targeting cancer cells due to immune evasion and lack of toxicity, necessitating a method to enhance their therapeutic efficiency and specificity.

Innovation Solution

A block copolymer comprising a hydrophilic first block, a hydrophobic second block that becomes cationic at pH 4.5 to 7, and a functional group capable of binding to thiol, which attaches to immune cells and releases a drug only at acidic conditions, thereby potentiating the immune cells' anti-cancer activity while minimizing side effects on normal tissues.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional anti-cancer chemotherapy and radiotherapy are used, then cancer treatment is provided, but non-specific pharmacological action causes poor therapeutic efficiency and significant side effects

Engineering Contradiction:
Improvetherapeutic efficiencyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The block copolymer is designed with hydrophilic and hydrophobic blocks that create pH-responsive properties. The hydrophobic block contains units that become cationic at acidic pH (4.5-7), enabling the polymer to selectively interact with cancer cells in acidic environments while remaining inert in normal physiological conditions, thus achieving local quality differentiation based on pH

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The polymer's charge state changes in response to pH parameter changes. At acidic pH (4.5-7), the hydrophobic block units become cationic, triggering drug release. This parameter-dependent transformation allows the system to respond specifically to the acidic microenvironment of cancer cells without affecting normal cells at physiological pH

Inventive Principle:
Principle #35Parameter changes

2Reliability

If immune cells are used for cancer treatment, then specific recognition and attack of cancer cells is achieved, but immune evasion through genetic variations and lack of individual cell toxicity limit complete treatment

Engineering Contradiction:
Improvespecificity of cancer targetingVSAvoidtherapeutic completeness
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The invention merges immune cell therapy with chemotherapy by attaching chemotherapeutic drugs to the block copolymer that is then bound to immune cells. This combination allows immune cells to specifically target cancer cells while simultaneously delivering a toxic payload, combining the advantages of both immunotherapy and chemotherapy

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The block copolymer is pre-functionalized with thiol-binding groups and drug-loading capabilities before immune cell attachment. This preliminary preparation ensures that when immune cells encounter cancer cells, the drug is already positioned for immediate release and delivery, enhancing the speed and effectiveness of the therapeutic response

Inventive Principle:
Principle #10Preliminary action

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 block copolymer system enhances the therapeutic efficacy of immune cells by selectively releasing drugs at acidic environments, maximizing anti-cancer effects while reducing systemic toxicity and side effects, thereby improving treatment outcomes for cancer and infections.

Implementation Method 1

a functional group capable of specifically binding to thiol

Methodology Applied
Scientific EffectThiol binding: Chemical Bonding

Implementation Method 2

a unit that is decomposed at a condition of pH 4.5 to 7

Methodology Applied
Scientific EffectpH-dependent decomposition: Decomposition (biological)

Implementation Method 3

a unit that becomes cationic at a condition of pH 4.5 to 7

Methodology Applied
Scientific EffectpH-dependent ionization: Ionisation

Data Source

PatentUS12115261B2Block copolymer comprising hydrophilic first block, hydrophobic second block, and functional group capable of specifically binding to thiol
Publication Date: 2024.10.15 GI CELL INC
  • US12115261B2 patent drawing
  • US12115261B2 patent drawing
  • US12115261B2 patent drawing

AI summary

The present invention relates to a block copolymer, comprising a hydrophilic first block, a hydrophobic second block, and a functional group capable of specifically binding to thiol.