Charged Polyester Polyplexes for Lower-Toxicity Biologic Delivery

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Solution Overview

Problem

Current nanoparticle delivery systems for biologics face challenges such as cytotoxicity, instability under physiological conditions, immune response, and limited targeting capabilities, leading to inefficient and potentially harmful delivery of nucleic acids and other biologics.

Innovation Solution

A polymeric delivery system using polyester copolymers of polyols and polycarboxylic acids, modified with charged moieties, forms polyplexes with biologics to create stable, biocompatible nanoparticles that can be tuned for specific degradation kinetics and targeted delivery, reducing immune response and cellular stress.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If cationic polymers are used to deliver nucleic acids, then delivery efficiency is improved, but cytotoxicity increases

Engineering Contradiction:

Improvedelivery efficiencyVSAvoidcytotoxicity

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the polymer structure by changing parameters such as incorporating biodegradable esters, adjusting molecular weight, controlling degree of branching, and modifying charge density to reduce cytotoxicity while maintaining delivery efficiency

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention uses composite polymer structures combining different functional groups (e.g., cationic groups for nucleic acid binding, biodegradable ester groups for controlled degradation, and hydrophilic groups for reduced toxicity) to achieve both efficient delivery and reduced cytotoxicity

Inventive Principle:

Principle #40Composite materials

2Adaptability or versatility

If conventional nanoparticle delivery systems are used, then targeted delivery is achieved, but immune response increases

Engineering Contradiction:

Improvetargeted deliveryVSAvoidimmune response

Core Design Contradiction:

Adaptability or versatilityVSObject-generated harmful factors

Solution Approach 1:

The patent removes or minimizes immune-stimulating components from the nanoparticle formulation while retaining the essential targeted delivery functionality through careful selection of biocompatible polymer materials

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The invention adjusts physical and chemical parameters of the nanoparticle system, including surface charge, hydrophobicity, and degradation rate, to reduce immune recognition and response while maintaining targeting capabilities

Inventive Principle:

Principle #35Parameter changes

3Quantity of substance

If cationic polymers with high charge density are used, then nucleic acid condensation is improved, but cellular toxicity increases

Engineering Contradiction:

Improvenucleic acid condensationVSAvoidcellular toxicity

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the charge density parameter of the polymer by incorporating biodegradable ester linkages and adjusting the ratio of cationic to neutral groups, enabling sufficient nucleic acid condensation while reducing cellular toxicity through controlled degradation

Inventive Principle:

Principle #35Parameter changes

4Reliability

If legacy synthetic biodegradable polymers are used, then biocompatibility is improved, but inflammatory response increases

Engineering Contradiction:

ImprovebiocompatibilityVSAvoidinflammatory response

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent fine-tunes the degradation products and degradation rate of the polyester copolymer by selecting specific polyol and polycarboxylic acid components, thereby reducing inflammatory response while maintaining biocompatibility

Inventive Principle:

Principle #35Parameter changes

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 system provides enhanced stability, increased blood residency time, and reduced inflammatory response, enabling efficient and targeted delivery of biologics with minimal cellular toxicity.

Implementation Method 1

combining charged polymers and biologics in a solvent to electrostatically associate the charged polymers and the biologics as the polyplexes

Methodology Applied

Scientific EffectElectrostatic association: Electrostatics

Data Source

PatentUS12440446B2Polymeric delivery systems

Publication Date: 2025.10.14 SECANT GROUP LLC

AI summary

A polymeric delivery system delivers a biologic to cells. In some embodiments, the polymeric delivery system includes polyplexes. Each polyplex includes at least one charged polymer and at least one biologic. The at least one charged polymer includes a polyester copolymer of a polyol and a polycarboxylic acid modified with at least one charged moiety having an opposite charge from a net charge of the at least one biologic. In other embodiments, the polymeric delivery system includes self-assembled particles including a block copolymer and a biologic associated with the block copolymer. The block copolymer includes a first block of a polyester copolymer of a polyol and a polycarboxylic acid and a second block of a second monomer or a second polymer.