Antioxidants for melasma

Antioxidants can be useful as adjunctive therapy in melasma. They include ascorbic acid, polypodium, glutathione, niacinamide, & melatonin. Antioxidants are adjunctive to medical therapy, peels & lasers.

Benefits

Protection against oxidative stress.

When to use

2-4 times daily

Works with

Medical treatments

Caution with

Skin sensitivity

Treatment science score melasma clinic

What is the summary?

  • Antioxidants are adjunctive to medical therapy
  • Oral antioxidants include vitamin B, C, polypodium, glutathione & melatonin
  • Topical antioxidants include vitamin B, C, E, & ferulic acid
  • Oral antioxidants are easier to use for most patients
  • Topical antioxidants can be considered in some patients
  • Skin irritation is the most common side effect of topical antioxidants, esp. Vitamin C
  • Antioxidants can also be supplemented via dietary intake
  • Antioxidants are adjunctive to mainstream melasma treatments

What can antioxidants do for your melasma?

Antioxidants play a significant role in managing melasma by addressing the oxidative stress that contributes to hyperpigmentation. Melasma is influenced by various factors, including UV radiation, inflammation, and hormonal changes, all of which can generate free radicals and lead to oxidative damage in the skin. Here’s how antioxidants help:

1. Neutralizing Free Radicals

Antioxidants like vitamin C, vitamin E, glutathione, and flavonoids neutralize free radicals, reducing cellular damage and inhibiting the overproduction of melanin triggered by oxidative stress.

2. Inhibiting Tyrosinase Activity

Some antioxidants, such as vitamin B, C and glutathione, inhibit tyrosinase, the enzyme responsible for melanin synthesis. This reduces pigmentation and helps even skin tone.

3. Enhancing Skin Repair

Antioxidants support skin barrier repair and collagen production, improving the overall skin texture and resilience against further pigmentary damage.

4. Photoprotection

Antioxidants like Polypodium leucotomos & vitamin E enhance the skin’s resistance to UV-induced damage, a major trigger of melasma. Combining antioxidants with sunscreens can marginally reduce pigmentation recurrence.

5. Reducing Inflammation

Chronic inflammation contributes to the persistence of melasma. Antioxidants such as niacinamide (vitamin B3) and green tea extract have anti-inflammatory properties that help calm the skin and prevent exacerbation of pigmentation.

Is polypodium effective for melasma?

Polypodium leucotomos extract (PLE) is increasingly recognized for its potential in melasma management due to its powerful antioxidant and photoprotective effects. Key benefits and findings include:

  • Antioxidant Action: PLE reduces oxidative stress, a critical factor in melasma, by neutralizing free radicals and minimizing UV-induced inflammation. This helps protect melanocytes, the cells responsible for melanin production, from oxidative damage.
  • Clinical Efficacy: Research published in The Journal of Clinical and Aesthetic Dermatology demonstrated significant improvements in melasma lesions when patients combined oral PLE with sunscreen. Pigmentation intensity was notably reduced.
  • Photoprotective Properties: PLE absorbs UV radiation and fortifies the skin’s defense against UV-induced damage. A study in Photodermatology, Photoimmunology & Photomedicine found that oral supplementation with PLE reduced hyperpigmentation by enhancing the skin’s resilience to UV exposure.
  • Combination Therapies: PLE enhances outcomes when paired with other treatments. A study in the International Journal of Dermatology revealed that combining oral PLE with sunscreen achieved a greater reduction in melasma severity than sunscreen alone. PLE is also effective when used alongside topical hydroquinone, sunscreen, or laser therapies.

The recommended dosage of oral polypodium is 480 mg, taken twice daily. While PLE is not a standalone cure, it provides valuable support as part of a broader melasma treatment plan.

What is glutathione and does it work?

Glutathione, a powerful antioxidant naturally produced in the body, is often explored for its potential in treating melasma due to its skin-lightening properties. It works by inhibiting melanin production, shifting melanin synthesis from darker eumelanin to lighter pheomelanin, and reducing oxidative stress in skin cells.

Research Evidence: Studies, including a randomized controlled trial published in Clinical, Cosmetic and Investigational Dermatology, have shown that oral glutathione (500 mg daily) taken over 8-12 weeks can result in noticeable improvement in melasma severity compared to placebo.

The dose of glutathione: is 500–1000 mg per day, taken over several weeks under professional supervision. We prefer oral supplementation over IV glutathione because tablets are cost effective. IV infusions cost between 890 to 1290 per infusion per week, adding up to over 50,000 AUD per year. 

What about vitamin C supplements for melasma?

The use of vitamin C (ascorbic acid) serums is a well-established and mainstream approach for treating melasma pigmentation. Its effectiveness in reducing pigmentation and improving skin luminosity has been thoroughly discussed in previous studies, however vitamin C supplementation can be useful. 

Evidence. Research by Hayakawa et al. explored the effects of oral vitamins C and E, both individually and in combination, in melasma patients. The combination group demonstrated the most significant improvement in reducing differences in skin luminosity between hyperpigmented and normal areas. Similarly, Handog et al. found that oral combination therapy with vitamins A, C, E, and procyanidin was effective in treating melasma among Filipino women.

Recommended Dosage: The typical oral dosage for vitamin C ranges from 500 mg once or twice daily, with a maximum limit of 2000 mg per day.

Optimal Use: While oral supplementation is beneficial, vitamin C is most effectively utilized in topical formulations. A serum containing 15% L-ascorbic acid combined with ferulic acid offers enhanced skin absorption and targeted benefits. Incorporating both topical and oral vitamin C can yield synergistic results in managing melasma. The rate limiting factor is skin irritation & the patient’s knowledge about how to modulate usage. 

What is niacinamide?

Vitamin B3 has been shown to reduce melasma pigmentation. Niacinamide’s ability to regulate pigment transfer and antioxidants’ role in protecting the skin from environmental triggers complement each other. B3 works by- 

  1. Niacinamide inhibits the transfer of melanosomes (pigment-containing organelles) from melanocytes to keratinocytes, which helps reduce hyperpigmentation, including melasma.  
  2. Barrier Strengthening: It enhances the production of ceramides and free fatty acids, improving the skin’s barrier function and retaining moisture.  
  3. Protection from Free Radicals: Antioxidants like vitamin C, vitamin E, and glutathione neutralize free radicals caused by UV radiation and pollution, preventing oxidative stress that can worsen pigmentation and accelerate aging. 
  4. Reduction of Inflammation: They decrease oxidative-induced inflammation, which can help with acne and skin redness.  

Clinical Evidence: Studies have demonstrated that a combination of niacinamide and antioxidants in topical formulations significantly improves skin texture, reduces pigmentation, and protects against UV-induced damage. Incorporating both into a skincare routine provides comprehensive protection & repair.  

Dosage: 500 mg niacinamide once to twice daily. 

What is Melatonin, and is it effective for Melasma?

Melatonin is a hormone naturally produced in the pineal gland that primarily regulates the body’s sleep-wake cycle or circadian rhythm. It is also found in certain foods, such as tart cherries, grapes, and tomatoes. Melatonin production peaks during nighttime in response to darkness, promoting restful sleep.  

In addition to its role in sleep regulation, melatonin exhibits antioxidant properties and has been studied for its potential benefits in treating pigmentation disorders like melasma. Research suggests that oral melatonin, at doses of 2–5 mg taken at night, can significantly reduce the Melasma Area Severity Index (MASI) score. When used in combination with other medical treatments, melatonin has been shown to enhance the overall effectiveness of melasma therapies by reducing oxidative stress and inhibiting melanin production.  

Dosage: 2-4 mg melatonin nightly. 

How long does it take for antioxidants to work?

Pigment reduction takes between 8 to 16 weeks. It takes time to reduce oxidative stress & pigment reduction internally. 

Glycolic acid, arbutin, azelaic acid, kojic acid, thiamidol & vitamin C can speed up pigment clearance. The fastest results are seen with novel chemical peels & pico lasers for melasma.

*Antioxidants alone will not be effective in the majority of melasma cases.

Should I start on antioxidants? What is the timing?

Here are some approaches to starting melasma antioxidants

  1. Holistic Approach:

Supplements can be an option for those preferring natural or alternative skincare methods. This pathway is often chosen by individuals looking to avoid science-based or medical treatments. This is known as the ‘fluffy’ side of melasma treatment. The effectiveness of such an approach, particularly in achieving a significant reduction in pigmentation, tends to be limited. If your focus is on “natural remedies” for melasma, this strategy may not align with the results-driven focus we emphasize.

  1. Complementary to Medical Treatments:


Supplements can be introduced alongside conventional therapies like topical treatments, peels, and lasers early in the treatment process. This is our PREFERRED way of adding antioxidants. 

Antioxidant supplementation may support faster results, however, adding supplements at this stage may increase the complexity of the regimen, requiring patients to be diligent and consistent in their approach. For those who are comfortable incorporating oral supplements, this can be a relatively straightforward enhancement to their clearance of melasma. 

  1. Advanced or Resistant Cases:


For patients with stubborn or dermal melasma unresponsive to standard treatments (approximately 15–20% of cases), supplements may be considered a “last resort” intervention. This approach is reserved for cases where other therapies have not delivered sufficient results.

The decision to incorporate supplements depends on clinical evaluations, the patient’s commitment & their understanding of melasma management. 

What is an example of a melasma skin care routine using antioxidants?

AM: Vitamin C & VItamin E, SPF, polypodium 480 mg 

Midday: Sunscreen reapplication, polypodium 480 mg

PM: Melatonin 2-4 mg taken nightly

The combination of choice will be determined by your physician at The Melasma Clinic.

Supplement

Dose Efficacy

Vitamin C tablets

500 mg twice daily *

Polypodium tablets

500 mg twice daily ***

Melatonin tablets

4 mg at night **

Glutathione tablets

500 - 1000 mg daily *

Note: The greatest traction of any melasma skincare routine is the correct application of sunscreen. This has a much greater impact on melasma clearance compared to antioxidant supplementation. 90% of melasma sufferers have not optimised their photoprotection prior to exploring other treatment modalities. How to use? Tinted, SPF 50+, twice daily, regardless of sun exposure. 

What is better, topical antioxidants vs oral antioxidant supplements?

For most patients, it will be supplements (if I had to pick one). In the ideal world it is both. Oral supplements get around skin irritation, which, for most patients, is the rate limiting step. Over-cooking your antioxidant use on the skin can lead to frictional melasma or irritant melasma (accounts for 20-25% of flare ups). 

Oral antioxidants such as vitamin C, polypodium, glutathione & niacinamide by-passes the skin’s barrier. Additionally research has shown that serum antioxidant levels play a role in some, but not all cases of melasma. 

What about antioxidants in sunscreen?

Once you get your sunscreen application correct (90% of melasma patients still can’t get this right), you can move on to the finer things, namely looking for sunscreens with antioxidants such as polypodium (Fernblock) & niacinamide. 

You can knock yourself out by shopping online for Heliocare here. 

*Get your sunscreen application correct before worrying about brands & antioxidants. Here is how to use sunscreen; SPF 50+, tinted, twice daily, 2 fingerlengths, regardless of sunexposure. 

Can antioxidants alone treat melasma?

Best results are seen when antioxidants are combined with medical therapies, sunscreen, lasers & chemical peels. 

Melasma treatment is all about probability, namely to come up with a melasma program unique to the individual in order to increase the hit rate of treating pigment. Antioxidant supplementation may marginally increase the success rate. 

How long do I take antioxidants for?

Indefinitely. Antioxidant supplements such as topical vitamin C, E & ferulic acid can be used lifelong. Studies have shown that antioxidants can be beneficial for health & longevity as your body is constantly in oxidative stress.  

What antioxidants are safe in pregnancy?

Though there are no controlled studies on the effects of antioxidants in pregnancy, here are our recommendations based upon logic & science. 

Safe antioxidants include; niacinamide, vitamin C, green tea, & polypodium. Sensible, supplement your diet rich in antioxidants.

Can I treat melasma with a diet high in antioxidants?

Yes, but chances are diet alone won’t suffice, however dietary supplementation can have benefits. In the best case scenario your melasma pigment improves. In the worst case scenario, you will reduce your chances of stroke & a heart attack, but your melasma is still present. 

Foods high in antioxidants include a wide variety of fruits, vegetables, nuts, seeds, and beverages. Here’s a breakdown by category:

Fruits

Berries (Rich in anthocyanins and vitamin C):

  • Blueberries
  • Strawberries
  • Raspberries
  • Blackberries

Citrus Fruits & miscellaneous

  • Oranges
  • Grapefruits
  • Lemons
  • Pomegranate
  • Apples
  • Grapes (especially dark varieties)

Vegetables

  • Kale
  • Spinach
  • Broccoli
  • Brussels sprouts
  • Carrots
  • Sweet potatoes
  • Red bell peppers

Nuts and Seeds

  • Almonds
  • Walnuts
  • Sunflower seeds
  • Flaxseeds
  • Chia seeds

Legumes and Whole Grains

  • Lentils
  • Black beans
  • Kidney beans
  • Quinoa
  • Oats

Herbs and Spices

  • Turmeric (Curcumin)
  • Ginger
  • Cinnamon
  • Garlic

Beverages- Green tea (Catechins)

  • Black tea
  • Coffee
  • Red wine (in moderation)

A Summary | Davin’s viewpoint on supplements for melasma & pigmentation

Dr Davin Lim | Dermatologist
The Melasma Clinic, Brisbane | Sydney

Supplementation with antioxidants is a novel but not primary approach in managing melasma. It is reserved for cases of resistant or dermal melasma or as adjunctive therapy in primary patients who have insight not to just rely on fluffy ‘natural antioxidants.’ 

Here is the summary- 

Higher Success Rates with Conventional Treatments: Mainstream therapies statistically yield better outcomes. My approach involves an objective assessment to identify the treatment with the highest likelihood of success, typically starting with established methods, thereby adding supplements based upon the insight of the patient. 

Complexity in Patient Understanding and Compliance: Many patients struggle with foundational aspects of melasma treatment, such as effective photoprotection, proper sunscreen use, and understanding radiation sources like blue light, HEV, and infrared. Adding supplements to an already intricate regimen of topicals, skin cycling, and physical therapies (e.g., lasers, peels) can overwhelm patients.  In 90% of melasma cases, the use of sunscreen is inadequate, this needs rectifying prior to any antioxidant therapy. 

To simplify, my supplementation strategy is structured in layers:  

First-Line: I select one, or all three of the following- vitamin C orally, melatonin & or polypodium extract. The dose are oral vitamin C (500 mg twice daily) and melatonin (2–4 mg nightly). Topical antioxidants such as CE ferulic acid can be considered in selected cases when patients understand the role of sunscreens & primary pigment correctors. Again, this factor is limited by patient insight (the hardest thing to get across in treating melasma). Polypodium leucotomos extract (480 mg twice daily).  

Third-Line: Glutathione tablets (500 mg two to three times daily).  Oral supplementation is more cost effective compared to IV glutathione. 

Tips: Don’t even think of antioxidants unless you get your melasma sun protection correct. You’re wasting your time, effort and money if you are not on first base. How to use sunscreens? Two fingerlengths, twice daily, tinted regardless of sun exposure. Read this page three times, revisit in 4 weeks time, then read it again.