Cell-Permeable Peptide Sequences for Intracellular Drug Delivery

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Solution Overview

Problem

The hydrophobicity of the plasma membrane in higher animal cells makes it difficult for most peptides, proteins, nucleotides, and liposomes to penetrate, inhibiting effective drug delivery methods.

Innovation Solution

A peptide with specific amino acid sequences, represented by SEQ ID NO: 1, exhibits cell permeability and allows penetration even when modified at the N-terminus, C-terminus, or between amino acids, and can be used in a composition for drug delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the plasma membrane is made hydrophobic to provide cytoprotection, then cell protection against foreign substances is improved, but peptide penetration into the cell becomes difficult

Engineering Contradiction:
Improvecell protectionVSAvoidpeptide penetration
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent introduces a cell-permeable peptide as an intermediary substance that facilitates the penetration of drugs into cells. This peptide acts as a mediator between the hydrophobic plasma membrane and the hydrophilic drug molecules, enabling drug delivery without compromising the protective function of the membrane.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the chemical parameters of the peptide sequence to optimize cell permeability. By carefully selecting and arranging amino acids (including specific patterns of hydrophobic and hydrophilic residues), the peptide achieves optimal balance between membrane penetration capability and biological functionality.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If conventional drug delivery methods are used, then drug delivery is achieved, but limitations and side effects occur

Engineering Contradiction:
Improvedrug delivery efficiencyVSAvoidside effects and limitations
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and isolates the critical cell-permeable peptide sequence from complex delivery systems. By focusing on a specific peptide motif (with patterns like X1-X7 as defined in the patent), the invention simplifies the delivery mechanism while maintaining efficiency, thereby reducing the side effects associated with more complex conventional methods.

Inventive Principle:
Principle #2Taking out (Extraction)

3Adaptability or versatility

If peptide sequences are modified at N-terminus or C-terminus, then peptide functionality is maintained, but cell permeability may be compromised

Engineering Contradiction:
Improvepeptide functionalityVSAvoidcell permeability
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies local quality by identifying specific regions within the peptide sequence that are critical for cell permeability. The invention defines particular amino acid positions (X1-X7) that maintain permeability function even when other regions are modified for specific biological activities, allowing independent optimization of different peptide functions.

Inventive Principle:
Principle #3Local quality

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 peptide achieves efficient intracellular delivery of drugs by maintaining cell permeability even with modifications, as demonstrated by confocal microscopy and flow cytometry results.

Implementation Method 1

the hydrophobicity of a phospholipid bilayer that makes up the plasma membrane makes most peptides, proteins, nucleotides, and liposomes almost impossible to move into the cell

Methodology Applied
Scientific EffectPassive diffusion: Diffusion

Data Source

PatentUS20250333442A1Novel cell-permeable peptide and use thereof
Publication Date: 2025.10.30 AJOU UNIV IND ACADEMIC COOP FOUND
  • US20250333442A1 patent drawing
  • US20250333442A1 patent drawing
  • US20250333442A1 patent drawing

AI summary

The present invention pertains to a novel cell-permeable peptide and a use thereof, wherein a peptide having the amino acid sequence set forth in SEQ ID NO: 1 was found to exhibit cell permeability, maintain the cell permeability even when one amino acid sequence of the peptide is substituted with another amino acid, and be able to penetrate plasma membranes even when a non-cell-permeable peptide is connected to the N-terminus, to the C-terminus, or between the amino acids of the peptide, and thus can be advantageously used for a drug delivery composition.