Polysaccharide-Peptide Carrier for Low-Toxicity Cell Uptake
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Solution Overview
Problem
Existing methods for introducing water-soluble polymer substances like nucleic acids, proteins, or medicines into cells or mucous membranes face challenges with high cytotoxicity, mucous membrane irritation, and low efficiency, particularly with polymer compounds having membrane-permeable peptides in a side chain.
Innovation Solution
A polysaccharide derivative with a membrane-permeable peptide group in its side chain, characterized by specific molecular structure and composition, is used to introduce these substances efficiently with low cytotoxicity and irritation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If a polymer compound having a membrane-permeable peptide in a side chain is used to introduce target compounds into cells, then the introduction efficiency is improved and the method is simplified, but the cytotoxicity increases and the concentration usage is limited
Solution Approach 1:
The patent changes the chemical parameters of the polymer by replacing conventional synthetic polymers with natural polysaccharides (hyaluronic acid, chitosan, dextran, cellulose). This parameter change maintains the membrane-permeable peptide functionality while reducing cytotoxicity, allowing higher concentrations to be used safely for improving introduction efficiency
Solution Approach 2:
The patent creates composite structures by combining polysaccharide backbones with membrane-permeable peptide side chains. This composite approach leverages the biocompatibility of natural polysaccharides while incorporating the cell-penetrating capability of peptides, achieving both high introduction efficiency and low cytotoxicity
2Productivity
If a polymer having a membrane-permeable peptide in a side chain is applied to promote medicine absorption from epithelium, then absorption is enhanced, but mucous membrane irritation occurs
Solution Approach 1:
The patent changes the chemical composition parameters from synthetic polymers to natural polysaccharides, which are inherently biocompatible and less irritating to mucous membranes. This allows the absorption-enhancing function to be maintained while reducing harmful irritation effects
Solution Approach 2:
The patent uses naturally occurring, biodegradable polysaccharides that are safely metabolized or excreted by the body, eliminating long-term accumulation issues and reducing chronic irritation risks associated with synthetic polymers
3Object-affected harmful factors
If a target compound and membrane-permeable peptide are covalently bound for introduction, then cell damage is reduced, but complex pretreatment is required
Solution Approach 1:
The patent segments the introduction system into a polysaccharide backbone (providing biocompatibility) and peptide side chains (providing penetration function), allowing the compound to be introduced without complex pretreatment while maintaining low cell damage
Solution Approach 2:
The polysaccharide acts as an intermediary carrier that facilitates the introduction of target compounds without requiring direct covalent bonding between the compound and peptide, thereby simplifying the pretreatment process while protecting cells from damage
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The polysaccharide derivative allows for high-efficiency introduction of poorly membrane-permeable compounds into cells and mucous membranes without complex pretreatment, reducing cytotoxicity and mucous membrane irritation.
Implementation Method 1
the membrane-permeable peptide method is a method that utilizes macropinocytosis of a cell induced by a membrane-permeable peptide
Data Source
AI summary
A polysaccharide derivative of the present invention has a partial structure represented by Formula (1) below. It is preferable that at least one of the amino acids that constitute X2 in Formula (1) below is a basic amino acid. (In the formula, X1 represents a residue obtained by removing the terminal amino group and the terminal carboxyl group from a neutral amino acid or an ω-aminoalkanoic acid, X2 represents a residue obtained by removing the terminal amino group and the terminal carboxyl group from a membrane-permeable peptide, X3 represents a hydroxyl group, an amino group, an alkoxyl group having 1 to 4 carbon atoms, or a benzyloxy group, a represents a number of 0 or 1, and b represents a number of from 0 to 50.)