Polymer Nanocapsules for Systemic RNAi Delivery in Cerebral Ischemia

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Solution Overview

Problem

Current treatments for brain ischemia, particularly through systemic delivery of microRNA, face challenges in delivering miRNA effectively to treat ischemic diseases due to poor delivery efficiency and invasive methods, with existing viral and non-viral vectors being ineffective.

Innovation Solution

Development of nucleic acid nanocapsules that encapsulate microRNA molecules, allowing for effective systemic delivery to brain ischemia sites, enhancing delivery efficiency and targeting specificity through polymer nanocapsules with a cross-linked polymer shell.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If systemic delivery of microRNA is used to treat brain ischemia, then the acceptability and ease of operation are improved, but the delivery efficiency and therapeutic efficacy deteriorate

Engineering Contradiction:
Improveease of administrationVSAvoiddelivery efficiency
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent employs a polymer nanoparticle vector as an intermediary carrier to deliver microRNA molecules systemically. The nanoparticle encapsulates the microRNA, protecting it from degradation and facilitating its transport across the blood-brain barrier to reach ischemic brain tissue. This mediator approach enables systemic administration (improving ease of operation) while achieving effective delivery to the target site (maintaining delivery efficiency).

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physical and chemical parameters of the microRNA delivery system by formulating it into polymer nanoparticles with specific size, charge, and surface properties. These parameter changes enable the microRNA to be delivered systemically with improved stability and targeting capability, resolving the contradiction between ease of administration and delivery efficiency.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If local administration of microRNA is used to treat brain ischemia, then the delivery efficiency and therapeutic efficacy are improved, but the device complexity and operational difficulty increase due to requiring multiple injections

Engineering Contradiction:
Improvedelivery efficiencyVSAvoidprocedure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The polymer nanoparticle delivery system is designed with multi-functionality: it can be administered through a single systemic injection, protects the microRNA from degradation, facilitates blood-brain barrier penetration, and enables targeted delivery to ischemic regions. This universal platform eliminates the need for multiple invasive injections while maintaining high delivery efficiency.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The nanoparticle acts as an intermediary that enables single-injection systemic delivery to reach brain tissue effectively. Instead of requiring direct local injections into the brain, the nanoparticle mediator transports the microRNA through the bloodstream to the target site, simplifying the procedure while maintaining delivery efficiency.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If viral vectors are used for systemic delivery of microRNA, then the delivery efficiency is improved, but the safety and toxicity profile deteriorate

Engineering Contradiction:
Improvedelivery efficiencyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs non-viral polymer nanoparticles as disposable, biodegradable carriers for microRNA delivery. These synthetic particles avoid the immunogenicity and safety concerns of viral vectors while providing sufficient delivery efficiency. The polymer materials can be designed to degrade after delivering their cargo, eliminating long-term toxicity concerns.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The delivery system uses composite polymer materials that combine biocompatibility, biodegradability, and effective microRNA encapsulation capabilities. This composite approach provides an alternative to viral vectors, achieving delivery efficiency without the associated safety and toxicity problems.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP3562511B1Rnai therapies for cerebral ischemia
Publication Date: 2025.08.06 VIVIBABA INC
  • EP3562511B1 patent drawingFigure 1a~1b
  • EP3562511B1 patent drawingFigure 2a~2i
  • EP3562511B1 patent drawingFigure 3a~3c

AI summary

Provided herein are novel methods of treating cerebral ischemia, comprising administering a polymer nanocapsule or a composition thereof. Said nanocapsules comprise a polymer shell and an RNAi (e.g., miRNA) molecule, wherein the polymer shell comprises a) at least one positively charged monomer, b) at least one degradable cross-linker, and c) at least one neutral monomer; and the RNAi molecule provides therapeutic benefits to a subject suffering from cerebral ischemia. Also disclosed herein are compositions of said polymer nanocapsules.