Transdermal Crosslinkable Agent Delivery Using Microneedling and pH Control
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Solution Overview
Problem
Existing technologies face challenges in effectively delivering crosslinkable agents across the skin barrier for cosmetic or therapeutic purposes, particularly in achieving desired penetration depth and extent, and in situ formation of crosslinked materials.
Innovation Solution
The method involves applying first and second crosslinkable entities at a pH of 3 to 5, followed by microneedling to enhance penetration and in situ formation of crosslinked materials at intradermal sites, utilizing specific parameters such as molecular weight, microneedle dimensions, and administration methods to control the delivery and formation process.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Length of moving object
If crosslinkable agents are applied topically to the skin, then the agents remain on the skin surface, but penetration depth and extent are insufficient
Solution Approach 1:
The patent applies microneedling to the skin before applying the crosslinkable agent formulation. This preliminary mechanical action creates micro-channels in the skin barrier, preparing the tissue to receive and absorb the agent more effectively. The microneedles create controlled injuries that facilitate deeper penetration while the agent is still in its uncrosslinked, penetrable form.
Solution Approach 2:
The patent utilizes pH modification as a key parameter to control the crosslinking timing and location. By formulating the agent at acidic pH (3-5), the crosslinking reaction is delayed until after penetration occurs. This parameter change allows the agent to penetrate deeper into the skin before crosslinking completes, solving the contradiction between penetration and delivery effectiveness.
2Speed
If crosslinking occurs rapidly after application, then crosslinked material forms quickly, but penetration is blocked because the material becomes too large
Solution Approach 1:
The patent employs pH control to modulate the crosslinking reaction rate. By maintaining acidic pH (3-5) in the formulation, the crosslinking kinetics are slowed down significantly. This parameter change creates a time window where the agent can penetrate the skin barrier before crosslinking completes, allowing both deep penetration and subsequent crosslinked material formation.
Solution Approach 2:
The patent performs penetration first (through microneedling and pH-controlled formulation) before crosslinking occurs. This sequential arrangement of events ensures that the agent reaches the intradermal target site in its small, penetrable form, and only then does crosslinking begin to form the larger crosslinked material structure.
3Length of moving object
If microneedling is performed before agent application, then penetration is enhanced, but the agent may crosslink before penetration occurs
Solution Approach 1:
The patent uses pH modification as a protective mechanism. By formulating the agent at acidic pH (3-5), the crosslinking reaction is inhibited until after microneedling and penetration have occurred. This parameter change ensures that even though microneedling creates pathways for penetration, the agent remains in its uncrosslinked state long enough to utilize these pathways effectively.
4Length of moving object
If low pH is used to slow crosslinking, then penetration occurs before crosslinking, but the reaction time is extended
Solution Approach 1:
The patent accepts extended reaction time as a necessary consequence of using low pH (3-5) to control crosslinking. This parameter change slows the crosslinking kinetics sufficiently to allow deep penetration, and the extended time window is utilized effectively through microneedling-enhanced delivery. The trade-off of time is justified by achieving the desired penetration depth.
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
This approach allows for the formation and retention of crosslinked materials at targeted intradermal sites, enhancing penetration and persistence, with the crosslinked material becoming present within 1 minute to 1 hour, and achieving molecular weights several times greater than the initial entities.
Implementation Method 1
applying first and second crosslinkable entities that react to form a crosslinked material
Implementation Method 2
microneedling the skin location after application of at least one of the crosslinkable entities
Data Source
AI summary
The present application describes the delivery, formulation and uses of systems comprising agents capable of penetrating skin.