Sphingosine Lipid Carriers for Nucleic Acid Delivery

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current nucleic acid drugs have low delivery efficiency due to inefficient delivery carriers, limiting their therapeutic effectiveness.

Innovation Solution

The use of sphingosine lipids and their derivatives as carriers to efficiently deliver small RNAs into cells, enhancing delivery efficiency and medicinal value without toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional delivery carriers are used for nucleic acid drugs, then the drugs can be administered, but the delivery efficiency is low

Engineering Contradiction:
Improvedelivery efficiencyVSAvoidtherapeutic effectiveness
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent modifies the chemical structure of sphingosine lipids by changing parameters such as chain length, saturation, and functional groups to optimize delivery efficiency. Specific derivatives like C18-sphingosine and its modified forms are synthesized to enhance nucleic acid binding and cellular uptake, directly addressing the low delivery efficiency of conventional carriers

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite structures where sphingosine lipid derivatives form complexes with nucleic acids. These composite materials combine the properties of lipids (membrane interaction, cellular uptake) with nucleic acids (therapeutic function), resulting in enhanced delivery efficiency and therapeutic effectiveness compared to using nucleic acids alone

Inventive Principle:
Principle #40Composite materials

2Ease of operation

If injection administration is used for nucleic acid drugs, then the drugs can be delivered, but the delivery efficiency is relatively low

Engineering Contradiction:
Improveadministration methodVSAvoiddelivery efficiency
Core Design Contradiction:
Ease of operationVSProductivity

Solution Approach 1:

The patent introduces sphingosine lipid derivatives as intermediary carriers between the nucleic acid drug and the cell. These lipid intermediaries facilitate the transfer of nucleic acids across cell membranes through their ability to interact with both aqueous environments and lipid membranes, significantly improving delivery efficiency while maintaining ease of administration

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS11974969B2Artificially synthesized sphingosine derivative lipoid monomer and use of same for delivering nucleic acid
Publication Date: 2024.05.07 BEIJING BAISHIHEKANG PHARMACEUTICAL TECHNOLOGY (BSJPHARMA) CO LTD
  • US11974969B2 patent drawing
  • US11974969B2 patent drawing
  • US11974969B2 patent drawing

AI summary

The invention provides an artificially synthesized single sphingosine lipid and use of delivering a nucleic acid thereof. More particularly, the invention provides Use or method for delivering a nucleic acid to a cell or a subject using a compound of Formula (I), a stereoisomer or a pharmaceutical acceptable salt thereof, or a combination comprising a compound of Formula (I), a stereoisomer or a pharmaceutical acceptable salt thereof,