Sugar-Functionalized Nanoparticle Compositions for Nucleic Acid Uptake

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Solution Overview

Problem

Existing nucleic acid delivery systems face challenges in achieving high cellular uptake, biocompatibility, low toxicity, and high transfection efficiency, necessitating a balance that current non-viral carriers fail to achieve effectively.

Innovation Solution

Development of sugar-functionalized nucleic acid carriers, such as dendron or dendrimer systems chemically conjugated with saccharides, to enhance delivery efficiency and biocompatibility, incorporating amine linkers, hydrophobic units, and conjugated lipids for improved intracellular delivery and nanoparticle stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional non-viral nucleic acid carriers are used, then manufacturing simplicity is maintained, but transfection efficiency and cellular uptake are insufficient

Engineering Contradiction:

Improvetransfection efficiencyVSAvoidcarrier structure complexity

Core Design Contradiction:

ProductivityVSDevice complexity

Solution Approach 1:

The patent employs composite material structures by combining dendron/dendrimer cores with sugar moieties and hydrophobic units to create multifunctional nucleic acid carriers. This composite approach enables simultaneous achievement of high transfection efficiency through cellular receptor interaction and adequate manufacturing feasibility through modular assembly processes.

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The nucleic acid carriers are designed with multi-functional properties: the dendron/dendrimer core provides structural framework and nucleic acid binding, sugar moieties enable cellular uptake through receptor interaction, and hydrophobic units facilitate membrane interaction. This multi-functionality resolves the contradiction by achieving high transfection efficiency without requiring entirely new complex carrier systems.

Inventive Principle:

Principle #6Universality (Multi-functionality)

2Reliability

If sugar-functionalized carriers with complex structures are implemented, then cellular uptake and transfection efficiency improve, but manufacturing complexity increases

Engineering Contradiction:

Improvecellular uptake efficiencyVSAvoidcarrier synthesis ease

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The carrier structure is segmented into distinct functional modules: dendron/dendrimer core, sugar moieties, and hydrophobic units. Each module can be synthesized separately and then assembled, which maintains manufacturing feasibility while achieving the complex functionality needed for high cellular uptake efficiency and reliable gene delivery.

Inventive Principle:

Principle #1Segmentation

3Productivity

If high loading capacity and cellular uptake are pursued, then delivery effectiveness improves, but biocompatibility and toxicity concerns increase

Engineering Contradiction:

Improvedelivery efficiencyVSAvoidtoxicity

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent utilizes parameter changes in the carrier structure, specifically incorporating biocompatible sugar moieties and controlled hydrophobic units, to achieve high delivery efficiency while maintaining low toxicity. The amine linker pKa and hydrophobic unit composition are optimized to balance cellular uptake efficiency with biocompatibility, resolving the contradiction between delivery effectiveness and safety.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS12410448B2Nanoparticle compositions containing sugar functionalized nucleic acid carriers

Publication Date: 2025.09.09 TIBA BIOTECH LLC

AI summary

Nanoparticle compositions for delivery of nucleic acids to subjects including carriers comprising sugar functionalized nucleic acid carriers, and therapeutic or immunogenic nucleic acid agents enclosed within the delivery molecules are described. Methods for treating or preventing diseases or conditions in a subject by administering the nanoparticle compositions that provide immune responses and synergistic therapeutic or preventive effects are provided.