RNA Nanoparticle Motion Elements for Targeted Drug Delivery

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Solution Overview

Problem

Current therapeutic delivery methods often result in high doses of drugs being required, leading to toxicity and side effects due to non-specific distribution in the body, with a lack of targeted delivery systems for small chemical drugs, particularly for cancer treatment.

Innovation Solution

The development of therapeutic RNA complexes that incorporate a motion element and small chemical drugs like camptothecin, paclitaxel, and methotrexate, which can specifically target tumor vasculature, allowing for controlled delivery and reduced systemic toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high doses of drugs are used for therapeutic delivery, then therapeutic efficacy is improved, but toxicity and side effects increase due to non-specific distribution

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidtoxicity and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by functionalizing nanoparticles with specific ligands (antibodies, peptides, aptamers, or small molecules) that recognize and bind to receptors overexpressed on tumor cells. This creates localized high-affinity binding at the tumor site while maintaining low affinity elsewhere in the body, enabling high therapeutic efficacy at the target with reduced systemic toxicity and side effects.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses ligand-functionalized nanoparticles as intermediaries to deliver therapeutic drugs specifically to tumor cells. The ligand-nanoparticle-drug complex acts as a mediator that transports the therapeutic agent from systemic circulation directly to the target cells through receptor-mediated endocytosis, improving efficacy while reducing the need for high systemic doses that cause toxicity.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Quantity of substance

If targeted delivery systems are developed for small chemical drugs, then local drug concentration at tumor site increases, but system complexity increases

Engineering Contradiction:
Improvelocal drug concentrationVSAvoidsystem complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent employs a universal nanoparticle platform that can be functionalized with different types of ligands (antibodies, peptides, aptamers, small molecules) to target various tumor types. The same core nanoparticle structure and delivery mechanism are used across different applications, with only the surface ligand needing to be changed. This multi-functional approach enables targeted delivery of small chemical drugs to achieve high local concentrations without developing entirely new complex systems for each drug or tumor type.

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

3Reliability

If ligand conjugation is used on nanoparticle surface, then tumor targeting affinity is improved, but nanoparticle stability may be affected

Engineering Contradiction:
Improvetumor targeting affinityVSAvoidnanoparticle stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent segments the nanoparticle structure into distinct functional domains: a stable core structure that maintains nanoparticle integrity and a surface layer where ligands are conjugated. This segmentation allows the core to remain stable while the surface is optimized for high-affinity tumor targeting through ligand-receptor interactions, resolving the contradiction between stability and targeting affinity.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent uses linker molecules as intermediaries between the nanoparticle surface and the targeting ligands. These linkers provide stable attachment points for ligands while maintaining the structural integrity of the nanoparticle. The intermediary linkers allow high-affinity binding to tumor receptors without compromising the stability of the nanoparticle core composition.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS20240165241A1Targeted delivery of drug molecules with drug ligands conjugated to RNA nanoparticle motion elements
Publication Date: 2024.05.23 OHIO STATE INNOVATION FOUND
  • US20240165241A1 patent drawing
  • US20240165241A1 patent drawing
  • US20240165241A1 patent drawing

AI summary

Disclosed herein is a therapeutics structure containing a motion element, an methotrexate (MTX), N—[N—[(S)-1,3-dicarboxypropyl]carbamoyl]-(S)-lysine (DCL), or UAMC-1110 ligand, and a plurality of drugs selected from the group consisting of camptothecin (CPT), paclitaxel (PTX), podophyllotoxin (PTOX), 7-Ethyl-10-hydroxycamptothecin (SN38), BMS1, BMS8, BMS27, BMS242, LY294002, PI3K-IN-20, and methotrexate (MTX).