Skin-Permeating Peptide Design for Transdermal Delivery
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Solution Overview
Problem
Current drug delivery through the skin faces challenges due to the skin's low permeability, with existing skin-permeable peptides being consumed by the circulation system, preventing targeted effects on the skin.
Innovation Solution
Development of isolated peptides with specific amino acid sequences (SEQ ID NOs. 1 to 10) that exhibit both skin permeability and retention, allowing for transdermal delivery of various cargos such as peptides, proteins, and polynucleotides, and forming peptide-cargo complexes for enhanced skin targeting.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If conventional skin-permeable peptides are used for transdermal delivery, then skin permeability is improved, but the peptides are consumed by the circulation system and cannot remain in the skin to exert targeted effects
Solution Approach 1:
The patent modifies the amino acid sequence parameters of existing skin-permeable peptides (such as changing specific residues in the KALA peptide sequence) to create variant peptides that maintain transdermal penetration capability while gaining skin retention properties. This parameter optimization allows the peptide to balance both permeation speed and retention reliability.
2Reliability
If the skin's protective cornified layer structure is maintained, then skin barrier function is improved, but permeability for drug delivery deteriorates
Solution Approach 1:
The patent uses specially designed peptides as intermediary carriers that can interact with the skin's cornified layer structure. These peptides temporarily disrupt or interact with the lipid matrix of the stratum corneum, facilitating drug passage while ultimately releasing the cargo within the skin tissue, thus mediating between the barrier function and permeability requirements.
3Productivity
If peptides are designed for high skin permeability, then transdermal delivery efficiency is improved, but the peptides lack the ability to retain cargo within the skin tissue
Solution Approach 1:
The patent segments the peptide structure into distinct functional domains: an N-terminal region responsible for skin permeation and a C-terminal region responsible for cargo binding and retention. This segmentation allows each domain to optimize its specific function while working together, enabling both efficient delivery and effective cargo retention within the skin.
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 peptides demonstrate excellent skin permeability and retention, enabling effective transdermal delivery of therapeutic agents and cosmetics, maintaining their functionality within the skin tissue.
Implementation Method 1
Only molecules having low molecular weight of 500 Da or less can pass through the skin by diffusion, mainly, through the intracellular lipid layer of the mortar structure
Data Source
AI summary
The present invention relates to a skin-permeating peptide, and more particularly, the present invention relates to an isolated peptide capable of permeating the skin to deliver a drug to the skin, to an isolated polynucleotide coding the peptide, to a composition for transdermal delivery comprising the peptide, and to a peptide/cargo composite comprising the peptide and cargo.