PEG-bl-PPS Polymeric Particles for Targeted Immunomodulator Delivery

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for systemic lupus erythematosus (SLE) and other autoimmune diseases are limited by delayed therapeutic efficacy and severe side effects, necessitating the development of more effective and targeted drug delivery systems.

Innovation Solution

Self-assembled di-block copolymer particles, specifically PEG-bl-PPS polymers forming micelles, filomicelles, or polymersomes, are used to deliver immunomodulatory drugs like chloroquine, enabling shape-based targeting of immune cells and tumor cells, thereby enhancing drug efficacy and reducing toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If systemic immunosuppressive drugs are used to treat SLE, then disease progression is controlled, but severe side effects and limited long-term efficacy occur

Engineering Contradiction:
Improvedisease control efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention segments the treatment approach by dividing the drug delivery into targeted particles that specifically deliver immunosuppressive agents to activated immune cells (such as dendritic cells and T cells) rather than systemic administration. This segmentation allows localized suppression of pathogenic immune responses while sparing other tissues from drug toxicity, thereby maintaining disease control efficacy while reducing side effects

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent applies local quality by creating drug particles with specific surface properties and sizes that enable selective accumulation at sites of immune activation. The particles are designed to be preferentially taken up by activated immune cells through mechanisms like enhanced permeability and retention or specific receptor recognition, thereby concentrating the therapeutic effect where it is most needed while minimizing exposure of healthy tissues to the drug

Inventive Principle:
Principle #3Local quality

2Duration of action of moving object

If conventional drug delivery systems are used, then drugs are administered systemically, but therapeutic efficacy is delayed and toxicity increases

Engineering Contradiction:
Improvetherapeutic efficacy timingVSAvoidtoxicity
Core Design Contradiction:
Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The invention implements preliminary action by pre-targeting the drug particles to immune cells before administering the full therapeutic dose. The particles are designed with surface characteristics that allow them to home in on activated immune cells in advance, ensuring that the immunosuppressive drug is delivered directly to the pathogenic cells as they become activated, thereby accelerating therapeutic efficacy and reducing the time to achieve disease control

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent uses the drug particles themselves as intermediaries that mediate between the administered drug and the target immune cells. These particles serve as carriers that protect the drug from premature degradation, facilitate selective delivery to immune cells through their specific physical and chemical properties, and enable controlled release of the immunosuppressive agent directly at the site of immune activation, thereby improving efficacy timing and reducing systemic toxicity

Inventive Principle:
Principle #24Intermediary (Mediator)

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 polymeric delivery system accelerates drug activity by directly targeting immune cells and tumor cells, increasing efficacy per dose and reducing side effects, as demonstrated by enhanced chloroquine delivery to plasmacytoid dendritic cells and B cells in SLE and specific cell types in cancer.

Implementation Method 1

self-assembled di-block copolymer particles

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 2

PEG-bl-PPS di-block polymer formed in a micelle, filomicelle, or polymersome

Methodology Applied
Scientific EffectAmphiphilic block copolymer formation: Amphiphiles

Data Source

PatentUS11311485B2Self-assembled particles for targeted delivery of immunomodulators to treat autoimmunity and cancer
Publication Date: 2022.04.26 NORTHWESTERN UNIV
  • US11311485B2 patent drawing
  • US11311485B2 patent drawing
  • US11311485B2 patent drawing

AI summary

The present invention provides for delivery of therapeutic drug in a polymeric delivery system comprising a PEG-bl-PPS di-block polymer formed in a micelle, filomicelle, or polymersome structure, wherein the structure effectively binds and/or interacts through shape-based targeting with a targeted cell type.