Vesicle Formulation for Dermal Delivery and Barrier Protection
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Solution Overview
Problem
Existing skin preparation technologies face challenges in delivering active ingredients effectively to the dermis while maintaining skin barrier function, as conventional methods often impair skin defense or have stability issues with vesicle formulations.
Innovation Solution
A vesicle formulation comprising α,ε-bis(γ-N—(C10-30)acylglutamyl)lysine, ceramide, and glycerin fatty acid esters, which forms a stable bilayer membrane structure, enhancing skin permeability and retaining active ingredients, thereby improving dermal delivery and maintaining skin barrier function.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If conventional percutaneous absorption promotion methods are used, then drug delivery to dermis is improved, but skin barrier function is impaired
Solution Approach 1:
The patent uses a vesicle as an intermediary carrier that transports drugs through the skin barrier without damaging it. The vesicle structure acts as a mediator between the drug and skin, enabling delivery while preserving the skin's protective function, unlike conventional methods that directly compromise the barrier.
Solution Approach 2:
The patent changes the physical-chemical parameters of the drug delivery system by using vesicles with specific surface properties and sizes that match skin penetration requirements, allowing efficient delivery without the harmful effects of conventional chemical or physical methods.
2Stability of the object's composition
If cationic surfactant-based vesicles are used, then vesicle formation is achieved, but stability and application versatility are reduced
Solution Approach 1:
The patent changes the charge parameter of the surfactant from cationic to nonionic, which fundamentally alters the vesicle's stability characteristics and compatibility with different formulations, enabling broader application while maintaining structural integrity.
Solution Approach 2:
The patent uses composite surfactant systems combining multiple nonionic surfactants with complementary properties, creating vesicles that achieve both stability and versatility through synergistic interactions between different material components.
3Stability of the object's composition
If insoluble ingredients are blended in external preparation, then formulation stability is improved, but dermal delivery capability is reduced
Solution Approach 1:
The patent embeds insoluble active ingredients inside the vesicle structure, nesting them within the hydrophilic core or lipid bilayer. This allows the ingredients to remain stable in the formulation while the vesicle transports them to the dermis, solving both stability and delivery problems simultaneously.
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 vesicle formulation effectively delivers active ingredients to the dermis, enhances skin barrier function, and maintains skin health by forming a stable bilayer membrane structure that is compatible with the skin's natural lipid bilayer, improving skin permeability and retaining active ingredients.
Implementation Method 1
a vesicle comprising: 1) an α,ε-bis(γ-N—(C10-30)acylglutamyl)lysine and/or a salt thereof, 2) a ceramide and/or a derivative thereof, and 3) one or more selected from a glycerin fatty acid ester, a polyglycerin fatty acid ester, and a pyroglutamic acid glycerin fatty acid ester
Data Source
AI summary
Disclosed is a technique for allowing an active ingredient as an agent for improving or maintaining the dermal environment to reach a dermis. Specifically disclosed is a vesicle comprising the following components 1) to 3): 1) an α,ε-bis(γ-N—(C10-30)acylglutamyl)lysine and/or a salt thereof; 2) ceramide and/or a derivative thereof; and 3) one or more selected from a glycerin fatty acid ester, a polyglycerin fatty acid ester and a pyroglutamic acid glycerin fatty acid ester. The acyl group in the α,ε-bis(γ-N—(C10-30)acylglutamyl)lysine is preferably a lauroyl group. The ceramide or the derivative thereof is preferably ceramide type-2 or ceramide type-3. The vesicle can encapsulate an active ingredient. The vesicle can be contained in an external preparation for the skin.