Tranexamic acid, a synthetic derivative of the amino acid lysine, is renowned for its dual – functional applications in the medical and cosmetic fields. Chemically, it is known as trans – 4 – aminomethylcyclohexanecarboxylic acid and was first introduced as an antifibrinolytic agent.
In the cosmetics industry, tranexamic acid has emerged as a powerful skin – lightening ingredient. Its action on the skin is based on its ability to inhibit the activation of melanocytes, the cells responsible for producing melanin, the pigment that causes skin darkening. By blocking the interaction between plasminogen and keratinocytes, which can trigger melanin production, tranexamic acid effectively reduces the formation of dark spots, hyperpigmentation, and melasma. This makes it a key component in a wide range of skincare products, including serums, creams, and masks, aimed at achieving a more even – toned and radiant complexion.
Benefits of Tranexamic acid
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Targeted Pigmentation Improvement: TXA effectively inhibits melanin overproduction by interfering with the signaling between keratinocytes and melanocytes, which is triggered by factors like UV damage or inflammation. This makes it particularly adept at reducing stubborn issues such as melasma, sun spots, post-inflammatory hyperpigmentation (e.g., acne scars), and uneven skin tone, resulting in a brighter, more uniform complexion.
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Stability and Compatibility: Unlike some other brightening ingredients (e.g., vitamin C, which is prone to oxidation), TXA is highly stable. It remains effective under light, heat, and air exposure, ensuring longer shelf life for formulations and consistent performance when applied to the skin. It also blends well with common skincare actives like niacinamide, hyaluronic acid, and retinol, allowing for versatile use in serums, creams, masks, and lotions without compromising efficacy.
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Gentle on Skin: Compared to harsher lightening agents (e.g., hydroquinone, which may cause irritation or sensitivity), TXA is generally well-tolerated, even by sensitive or dry skin types. Its mild nature reduces the risk of redness, peeling, or discomfort, making it suitable for long-term use in daily skincare routines.
- Anti-Inflammatory Properties: Beyond brightening, TXA exhibits mild anti-inflammatory effects, helping to calm irritated skin and reduce redness. This adds value in formulations targeting conditions like rosacea or post-sun exposure inflammation, where both pigmentation and irritation are concerns.
Tranexamic acid mechanism of Action
- Blocking melanocyte activation: UV damage, inflammation, or injury can trigger keratinocytes (skin cells) to release plasminogen. When plasminogen converts to plasmin, it activates melanocytes (cells that produce melanin), leading to excess pigmentation (e.g., melasma, sun spots). TXA inhibits this plasminogen-to-plasmin conversion, reducing melanocyte stimulation.
- Interfering with melanin transport: It disrupts the transfer of melanin from melanocytes to keratinocytes, preventing pigment from accumulating in the skin’s upper layers.
- Suppressing tyrosinase activity: Tyrosinase is a key enzyme in melanin synthesis. While less direct than its effect on plasminogen, TXA may weakly inhibit tyrosinase, further reducing pigment production.
Key Advantage: Stability
Advantages of tranexamic acid
- Targeted Pigmentation Control: Effectively fades dark spots, melasma, hyperpigmentation, and post-inflammatory marks by inhibiting melanin production and transport, resulting in a more even skin tone.
- Stability: Unlike unstable brightening ingredients (e.g., vitamin C), TXA resists oxidation and degradation from light/heat, ensuring consistent efficacy in formulations over time.
- Gentleness: Causes minimal irritation, making it suitable for sensitive, dry, or acne-prone skin—unlike harsher alternatives like hydroquinone.
- Compatibility: Blends well with other skincare actives (e.g., niacinamide, hyaluronic acid) to enhance results, offering combined benefits like hydration and brightening.
Tranexamic acid technical parameters
Technical Parameters | Specification Range |
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Chemical Name | trans-4-Aminomethylcyclohexanecarboxylic Acid |
Molecular Formula | C₈H₁₅NO₂ |
Molecular Weight | 157.21 g/mol |
Appearance | White crystalline powder |
Melting Point | 233-236°C (decomposes) |
Solubility | Freely soluble in water (~1g/10mL), slightly soluble in ethanol, insoluble in ether, chloroform, etc. |
Purity (by HPLC) | ≥99.0% |
Loss on Drying | ≤0.5% (at 105°C for 2 hours) |
Residue on Ignition | ≤0.1% |
pH Value (1% aqueous solution) | 6.0-7.5 |
Heavy Metals (as Pb) | ≤10 ppm |
Arsenic (As) | ≤2 ppm |
Sulfate (as SO₄²⁻) | ≤0.02% |
Chloride (as Cl⁻) | ≤0.02% |
Specific Optical Rotation ([α]²⁰_D, 1% in water) | +88° to +91° |
Tranexamic acid applications
- Treating Hyperpigmentation
- Brightening and Evening Skin Tone
- Enhancing Skincare Formulations
- Synergizing with Other Ingredients
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