Tranexamic-Mandelic Ionic Salt for Skin Permeability With Low Irritation
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Solution Overview
Problem
Conventional topical formulations of mandelic acid face challenges in penetrating the stratum corneum barrier, leading to low bioavailability and limited application due to difficulty in skin permeability.
Innovation Solution
The formation of a supramolecular tranexamic acid-mandelic acid ionic salt through ionization of tranexamic acid and mandelic acid, which enhances skin permeability and bioavailability while maintaining efficacy and reducing skin irritation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional topical formulations of mandelic acid are used, then the formulation is simple and easy to manufacture, but the skin permeability and bioavailability of mandelic acid are low
Solution Approach 1:
The patent creates a composite ionic salt formulation by combining mandelic acid with tranexamic acid in a specific molar ratio (1:1 to 1:10). This composite structure enhances skin permeability through synergistic effects while maintaining formulation simplicity. The ionic salt formation allows both active ingredients to work together, improving bioavailability without significantly complicating the manufacturing process.
Solution Approach 2:
The patent changes the chemical state of mandelic acid by converting it into an ionic salt form through reaction with tranexamic acid. This parameter change (from neutral acid to ionic salt) fundamentally alters the permeability characteristics of mandelic acid, enabling it to penetrate the stratum corneum more effectively while maintaining the simplicity of topical application.
2Reliability
If the concentration of mandelic acid is increased to improve efficacy, then the therapeutic effect is enhanced, but skin irritation increases
Solution Approach 1:
The patent introduces tranexamic acid as an intermediary substance that mediates between mandelic acid and the skin. Tranexamic acid acts as a permeation enhancer and skin protective agent, allowing mandelic acid to achieve therapeutic concentrations while reducing direct irritation to the skin. The intermediary facilitates controlled delivery of mandelic acid at effective doses.
Solution Approach 2:
The ionic salt composite of mandelic acid and tranexamic acid provides synergistic effects where tranexamic acid mitigates the irritating effects of mandelic acid while enhancing its penetration. This composite approach allows maintenance of therapeutic efficacy at lower, less irritating concentrations of mandelic acid.
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 supramolecular tranexamic acid-mandelic acid ionic salt improves skin permeability and bioavailability of mandelic acid, maintaining its anti-oxidation, inhibition of melanocyte activity, and inhibition of tyrosinase activity with low skin irritation.
Implementation Method 1
the supramolecular tranexamic acid-mandelic acid ionic salt shown in Formula 1 is obtained by using tranexamic acid and mandelic acid as precursors through ionization to form a salt
Data Source
AI summary
Provided are a supramolecular tranexamic acid-mandelic acid ionic salt as well as a preparation method therefor and a use thereof, relating to the technical field of pharmaceutical and cosmetic compounds. The supramolecular tranexamic acid-mandelic acid ionic salt has a structural formula as shown in formula I. Tranexamic acid and mandelic acid undergo reaction and bonding to form a supramolecular salt. The skin permeability of mandelic acid can be effectively improved and less irritation is caused to the skin while the efficacy of mandelic acid is well maintained.