Aqueous Solubilized Ursodeoxycholic Acid for Skin Permeability
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Solution Overview
Problem
Ursodeoxycholic acid (UDCA) has low solubility in water, leading to skin irritation and poor skin permeability, making it ineffective as a topical treatment for inflammatory skin diseases due to its crystalline form, which is difficult to dissolve and emulsify in skin preparations.
Innovation Solution
Aqueous solubilization of UDCA with maltodextrin creates a clear, stable solution that increases skin permeability and prevents self-association, allowing for effective delivery of UDCA as a skin external preparation without causing skin irritation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If UDCA is used in crystalline form for topical treatment, then it has therapeutic potential for inflammatory skin diseases, but it exhibits low solubility in water and causes skin irritation
Solution Approach 1:
The patent uses maltodextrin as a solubilizing agent and intermediary substance to enable UDCA to dissolve in aqueous environments. The maltodextrin forms a complex with UDCA, allowing it to be delivered topically without precipitation or crystallization that would cause skin irritation. This intermediary approach maintains therapeutic efficacy while eliminating the harmful crystalline form.
Solution Approach 2:
The patent changes the physical-chemical parameters of UDCA by converting it from crystalline form to an aqueous solubilized form through pH adjustment and complexation with maltodextrin. This parameter change transforms UDCA into a stable, non-irritating solution that can be effectively applied to skin while maintaining its anti-inflammatory therapeutic properties.
2Stability of the object's composition
If UDCA is used in crystalline form, then it maintains stability, but it has poor skin permeability and is difficult to emulsify in skin preparations
Solution Approach 1:
The patent applies parameter changes by adjusting pH and using maltodextrin complexation to transform UDCA from an insoluble crystalline state to a stable aqueous solution. This enables the substance to be easily emulsified in skin preparations and significantly improves skin permeability while maintaining compositional stability through the protective maltodextrin complex.
Solution Approach 2:
The patent creates a composite system where UDCA is complexed with maltodextrin in an aqueous medium. This composite material combines the therapeutic properties of UDCA with the solubilizing and stabilizing properties of maltodextrin, resulting in a formulation that is both stable and highly permeable to skin.
3Ease of operation
If UDCA is dissolved in water at high concentration, then skin permeability is improved, but UDCA has inherently low water solubility
Solution Approach 1:
The patent introduces maltodextrin as an intermediary solubilizing agent that enables high-concentration aqueous solutions of UDCA. The maltodextrin-UDCA complex allows UDCA to achieve high concentrations in water without precipitation, thereby enabling high skin permeability while overcoming the inherent low water solubility of UDCA.
Solution Approach 2:
The patent changes the solubility parameters of UDCA through pH adjustment and complexation with maltodextrin, enabling it to dissolve at high concentrations in aqueous solutions. This parameter transformation allows the formulation to achieve both high water solubility and high skin permeability 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 aqueous solubilized UDCA composition significantly improves skin permeability and therapeutic efficacy for inflammatory skin diseases like atopic dermatitis, acne, and psoriasis, reducing discomfort and promoting effective treatment with enhanced stability and absorption.
Implementation Method 1
Aqueous solubilization of UDCA with maltodextrin creates a clear, stable solution that increases skin permeability
Implementation Method 2
Aqueous solubilization of UDCA with maltodextrin creates a clear, stable solution that increases skin permeability and prevents self-association
Data Source
AI summary
This disclosure relates to a composition for the prevention or the treatment of inflammatory skin diseases or severe pruritus comprising an aqueous solubilized ursodeoxycholic acid (UDCA). According to this disclosure, inflammatory skin diseases and severe pruritus such as atopic dermatosis, acne, psoriasis, hives, inflammatory skin disease, seborrheic dermatitis and contact dermatitis can be effectively alleviated or treated. Therefore, the composition comprising aqueous solubilized ursodeoxycholic acid of this disclosure can be best used as a pharmaceutical, food or cosmetic composition, and can be used particularly as an external preparation to exhibit its effect.