Recombinant Botulinum Toxin with Cell-Penetrating Peptides for Transdermal Delivery
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Solution Overview
Problem
Current methods for delivering botulinum toxin for cosmetic and therapeutic purposes require frequent injections, which can cause side effects and are limited by the skin's barrier properties, making it difficult to achieve efficient transdermal delivery of macromolecules like proteins.
Innovation Solution
Development of cell-penetrating peptides (CPPs) that combine with botulinum toxin to enhance skin and cell penetration, using novel CPPs with higher cargo delivery efficiency, such as Cargo Delivery Peptides (CDPs), fused to the botulinum toxin light chain or heavy chain, and incorporated into a cosmetic composition with transdermal penetration enhancers like glyceryl monostearate.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If botulinum toxin is administered by injection every 3-5 months, then the cosmetic and therapeutic effects are maintained, but side effects such as bruises, allergies, and wounds increase with frequent administration
Solution Approach 1:
The patent uses cell-penetrating peptides as intermediary carriers to deliver botulinum toxin directly into skin cells through non-invasive topical application. The CPPs facilitate the transport of the large botulinum toxin molecule across the skin barrier and cell membrane, eliminating the need for repeated injections while maintaining therapeutic efficacy
Solution Approach 2:
The patent replaces the mechanical injection method with a biochemical delivery system. Instead of physically injecting the toxin through needles, the invention uses cell-penetrating peptides to mediate the transdermal and intracellular delivery of botulinum toxin through topical application, thereby eliminating injection-related side effects
2Ease of operation
If botulinum toxin is delivered transdermally without cell-penetrating peptides, then non-invasive application is achieved, but the skin barrier prevents effective delivery of macromolecules
Solution Approach 1:
The patent introduces cell-penetrating peptides as intermediary carriers that bridge the gap between the skin barrier and botulinum toxin delivery. These peptides facilitate the transport of the large toxin molecule across the stratum corneum and into cells, enabling effective non-invasive transdermal delivery of macromolecules
Solution Approach 2:
The patent creates a composite delivery system combining cell-penetrating peptides with botulinum toxin. This composite structure leverages the cell-penetrating capability of the peptides and the therapeutic function of the toxin, enabling the large macromolecule to penetrate the skin barrier effectively through topical application
3Reliability
If conventional cell-penetrating peptides are used with botulinum toxin, then skin penetration is improved, but cargo delivery efficiency is insufficient
Solution Approach 1:
The patent optimizes the parameters of cell-penetrating peptides, specifically using peptides with 11-15 arginine residues at the N-terminus. This parameter optimization enhances the peptides' ability to bind and deliver botulinum toxin into cells, significantly improving cargo delivery efficiency while maintaining skin penetration capability
Solution Approach 2:
The patent introduces a linker sequence between the cell-penetrating peptide and botulinum toxin that contains cysteine residues. This local modification in the linker region enables disulfide bond formation, creating a stable yet releasable connection that enhances the overall delivery efficiency of the cargo
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 CPP-botulinum toxin recombinant proteins demonstrate improved skin and cell penetration, maximizing the intrinsic efficacy of botulinum toxin for cosmetic and therapeutic applications while reducing the need for frequent injections and minimizing side effects.
Implementation Method 1
a peptide that is capable of mediating the transport of an active molecule into a cell
Implementation Method 2
cosmetic composition with transdermal penetration enhancers like glyceryl monostearate
Data Source
AI summary
Disclosed herein is a recombinant protein including botulinum toxin and cell penetrating peptides and cosmetic composition. The cell penetrating peptide according to the present disclosure may be actively used as a topical agent for various disease treatment, aesthetic, or cosmetic purposes, especially for a cosmetic composition, by securing better convenience as well as maximizing the intrinsic in vivo efficacy of the botulinum toxin through the cell penetrating recombinant proteins that combines the botulinum toxin and a cell penetrating peptide by making skin penetration and/or cell penetration for botulinum toxin more efficient.