Nanoparticle Formulation for Short-Chain Fatty Acid Delivery

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Solution Overview

Problem

Current methods for delivering short-chain fatty acids, such as butyrate, to treat metabolic and oncogenic diseases face challenges due to their rapid metabolism and low concentrations in peripheral circulation, making it difficult to achieve a non-toxic and effective therapeutic effect.

Innovation Solution

Nanoparticle formulations comprising a cationic cholesterol derivative, neutral phospholipid, cholesterol, and a PEGylated saturated fatty acid derivative are used to encapsulate short-chain fatty acids, allowing for controlled delivery to target organs and prolonged therapeutic effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If short-chain fatty acids are administered directly to achieve therapeutic effects, then metabolic and oncogenic diseases can be treated, but the compounds are rapidly metabolised and achieve very low concentrations in peripheral circulation

Engineering Contradiction:
Improvetherapeutic effectVSAvoidconcentration maintenance
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent uses nanoparticle carriers as intermediaries to deliver short-chain fatty acids to target organs. These nanoparticles protect the fatty acids from rapid metabolism by colonocytes and the liver, enabling sustained release and maintaining therapeutic concentrations in peripheral circulation. The nanoparticle formulation acts as a mediator between the administered compound and the target tissue, solving the problem of rapid clearance.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If high concentrations of short-chain fatty acids are administered to overcome rapid metabolism, then therapeutic effects can be achieved, but toxicity increases

Engineering Contradiction:
Improvetherapeutic effectVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The nanoparticle formulation enables local delivery of short-chain fatty acids to target organs such as the liver and adipose tissue. By targeting specific organs rather than distributing systemically at high concentrations, the therapy achieves effective local concentrations while minimizing whole-body toxicity. The nanoparticles concentrate the therapeutic agent where it is needed most.

Inventive Principle:
Principle #3Local quality

3Duration of action of moving object

If nanoparticle formulations are used to deliver short-chain fatty acids, then sustained delivery and reduced toxicity are achieved, but the formulation complexity increases

Engineering Contradiction:
Improvedelivery durationVSAvoidformulation complexity
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent employs composite nanoparticle formulations combining lipid materials with short-chain fatty acids. These composite structures integrate the therapeutic agent within a biocompatible carrier system, achieving sustained delivery through the controlled release properties of the composite material while maintaining manufacturability through established nanoparticle preparation techniques.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP2890365B1Nanoparticle formulation
Publication Date: 2019.11.20 UNITED KINGDOM RESEARCH AND INNOVATION
  • EP2890365B1 patent drawingFigure 1~3
  • EP2890365B1 patent drawingFigure 4~6
  • EP2890365B1 patent drawingFigure 7~9

AI summary

The present invention concerns nanoparticle formulations suitable for the delivery of one or more therapeutic agents, the formulations comprising: a cationic cholesterol derivative; a neutral phospholipid; cholesterol or a neutral cholesterol derivative; and a saturated fatty acid, PEGylated neutral derivative of phosphatidylethanolamine or phosphatidylcholine.