Lyotropic Liquid Crystal Transdermal Enhancer
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Solution Overview
Problem
Transdermal absorption of active ingredients is limited by the skin's barrier, resulting in low bioavailability, and existing enhancers may cause irritation, making it difficult to effectively deliver various active compounds through the skin.
Innovation Solution
The use of lyotropic liquid crystals as a transdermal absorption enhancer, containing surfactants, water, oil, and polyhydric alcohols, which form a liquid crystal structure that enhances the permeation of active ingredients, including macromolecules and water-soluble substances, by mimicking the skin's natural lipid layers and maintaining stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If transdermal administration is used to deliver active ingredients, then ease of administration and reduced side effects are improved, but bioavailability is worsened due to skin barrier penetration limitations
Solution Approach 1:
The patent uses transdermal absorption enhancers as intermediary substances that facilitate the passage of active ingredients through the skin barrier. These enhancers modify the skin's permeability properties temporarily, allowing drugs to pass through without compromising the skin's overall protective function. The enhancer acts as a mediator between the external application and internal absorption, solving the contradiction between ease of administration and reliable drug delivery.
Solution Approach 2:
The patent employs various transdermal absorption enhancers that temporarily alter the physical and chemical parameters of the skin barrier. Different enhancers modify parameters such as lipid fluidity, protein conformation, or membrane permeability to different extents, enabling controlled changes in skin permeability that allow sufficient drug absorption while maintaining skin integrity and function.
2Reliability
If conventional transdermal absorption enhancers are used to improve bioavailability, then drug penetration is enhanced, but skin irritation is worsened
Solution Approach 1:
The patent applies transdermal absorption enhancers locally and temporarily to the application site, concentrating the enhancer's action only where needed for drug absorption. The enhancer's effect is localized to the stratum corneum and upper epidermis at the application site, allowing enhanced penetration without causing widespread skin irritation. The local application and temporary action minimize harmful effects while achieving the desired bioavailability improvement.
Solution Approach 2:
The patent uses transdermal absorption enhancers at controlled concentrations and for limited durations to achieve sufficient drug penetration without excessive skin disruption. By applying the enhancer at optimal concentrations and allowing it to act only during the drug absorption period, the patent achieves partial action that is sufficient for therapeutic purposes while avoiding the excessive skin damage that would result from stronger or prolonged enhancer application.
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 efficient and sustained transdermal absorption of various active ingredients, including large molecules and water-soluble substances, improving bioavailability and reducing skin irritation, as demonstrated by increased blood concentrations and skin penetration of retinoic acid and other compounds.
Implementation Method 1
lyotropic liquid crystal contains 5% by weight to 80% by weight of a surfactant and 5% by weight to 80% by weight of water
Implementation Method 2
lyotropic liquid crystal has an action of enhancing the transdermal absorption of various active ingredients
Implementation Method 3
lyotropic liquid crystal is an effective ingredient... the lyotropic liquid crystal contains 5% by weight to 80% by weight of a surfactant and 5% by weight to 80% by weight of water
Data Source
AI summary
An object of the present invention is to provide a transdermal absorption enhancer by which various active ingredients are transdermally absorbed. In accordance with a transdermal absorption enhancer of the present invention which effective ingredient is lyotropic liquid crystal which has been utilized as a basic material for pharmaceutical preparations for external application and for cosmetics, transdermal absorption of a macromolecular substance and a water-soluble substance was able to be improved.