*Please note: the thumbnail pic for this blog and corresponding video was made black and white and with contrast to show the pigment irregularities (much like a woods lamp would).
Up until recently, the most effective at-home ‘toolkit’ to clear hyperpigmentation involved a combination of hydroquinone and tretinoin - both in strengths available only with a prescription. I know from personal experience in treating both clients and my own melasma that the Obagi Nuderm works. But there’s a high price tag (in excess of $400). It also isn’t without risks - studies show that longer use of hydroquinone in higher strengths poses some problems. And, of course, not all people can tolerate higher strength retinoids.
It’s been my mission in the past several years to come up with other options that would tackle pigmentation in the same efficient way, but without the high financial and skin irritation costs. This is especially relevant to skin of color because more irritation can actually worsen pigment...Finding products that are non-irritating benefits people across the melanin spectrum. In the past, I’ve reported on my success in managing ongoing pigmentation issues with tranexamic acid. I’m happy to say that, while the product Tranex is still an important part of my repertoire, it now has an increasingly interesting set of partners to work with.
FIRST Tyrosinase:
Tyrosinase is a copper containing enzyme that plays a critical role in pigment production in our skin.
In a nutshell: tyrosine is converted into melanin. Tyrosinase inhibitors slow the conversion of tyrosine into pigment. This happens in the melanocyte (pigment-producing cell) in the dermis.
Don't get too caught up in that ... what's important to know is that this enzyme (tyrosinase) is very, very crucial in the regulation of pigment. Neutralizing or inhibiting this enzyme (tyrosinase) will effectively limit the unwanted pigment that we see on/in our skin.
Until now hydroquinone has been the best tyrosinase inhibitor used topically. The good news is...there are other ingredients making their way onto the affordable scene, and I am excited to share them with you here!
Three Anti-pigmentation Ingredients
to have on your Radar
1. TRANEXAMIC ACID
Topical tranexamic acid is effective at treating all types of hyperpigmentation. This includes PIH (the discoloration some of us are left with after a pimple or mosquito bite disappears), scarring, and the residual spottiness after too much sun exposure. All of that as well as that difficult-to-treat condition melasma that’s often brought on by hormonal changes. Tranexamic acid is a bit of a mystery in that it is not fully understood how it works. It is thought to have the effect on tyrosinase that we want (inhibiting it) as well as changing the way that our pigment cells (melanocytes) "talk" to our skin cells (keratinocytes). There is also the effect that tranexamic acid has on blood that is still being studied. No matter how it works, it does indeed work. It is a great topical alternative to hydroquinone and also a great option to explore in-office with treatments like microneedling and laser. More on that to come!
2. TOPICAL GLUTATHIONE
Glutathione is one of the body's most potent antioxidants. Like other antioxidants, glutathione keeps cells healthy by neutralizing free radicals and removing toxins. It also improves energy production, boosts our immune system, and according to some studies, can delay early signs of skin aging. When applied topically, glutathione attacks hyperpigmentation in three ways:
1. Glutathione indirectly inactivates tyrosinase (in a process that is mind-blowing if you are not a bio-chemist lol...but suffice it to say glutathione affects a "switch" that then impacts the production of eumelanin to phaeomelanin... as well as affecting cysteine levels. I know. We all need a Ph.D. to absorb this info).
2. Glutathione directly inactivates tyrosinase by binding with the copper-containing site of that enzyme.
3. Glutathione works as an antioxidant - neutralizing free radicals, and essentially de-rusting the cells...
To read more check out this article (one of the many articles where I sourced my info):
https://pubmed.ncbi.nlm.nih.gov/18492181/ Glutathione can be used in other ways- via IV infusion (which I DO NOT recommend) and also in the form of a supplement. I'm taking supplemental liposomal glutathione from LivOn labs - but I suggest that you speak with your healthcare provider before starting a glutathione supplement regimen. Read more about liposomal glutathione here:
3. 4-N-BUTYLRESORCINOL (AKA 4-BUTYLRESORCINOL)
This tricky to pronounce ingredient recently came onto my radar. Studies have shown that 4-butylresorcinol is better at inhibiting tyrosinase activity than most other topicals, exceeding
by far the potency of hydroquinone, arbutin, and kojic acid. While I'm in my early stages of evaluating 4-Butylresorcinol, I'm super excited about what I'm learning
The above photos are from a study of skin that was treated with 1% 4‐butylresorcinol for four months. Below we can see the impressive efficacy of 4‐butylresorcinol compared with some of the other OTC anti-pigmentation ingredients.
Other Pigmentation Busters
1. SPF SPF SPF
I would be remiss to leave this basic concept out of this blog. The importance of sun protection can not be understated. A tip for choosing a good sunscreen if you are battling pigmentary issues: choose a sunscreen with broad-spectrum protection, antioxidants, and iron oxides (if possible.) I'll soon be doing a full blog post on the benefits of iron oxides, but just know that their presence in sunscreen is thought to help block visible light - a part of the light spectrum thought to greatly contribute to excessive pigmentation. Antioxidants are known to boost the effects of sunscreen. You will often find more protection from visible light with tinted sunscreens.
My top 3 tinted sunscreens with iron oxides and/or antioxidants are:
Drmtlgy universal tinted moisturizer SPF 46 code Penn gets 20% off (antioxidants in this one are great for most skin types, and good for rosacea-prone skin and acne-prone skin)
CeraVe hydrating SPF 30 tinted sunscreen (iron oxides in this one-great for dry skin)
Tizo 3 Primer Sunscreen SPF 40 (antioxidants and iron oxides-great for most skin types ((including sensitive)) but if you are super dry you would need to hydrate a bit more before using this mousse-like, matte SPF)
A great option if you're in the UK is the ISDN Tinted SPF. I have used and loved this one for it's sheer tint and lightweight texture.
Quick tip: If you can see the product (because it's tinted), it is more likely to block the light you see (that is contributing to the excess pigment).
2. RETINOIDS
I'll l cover retinoids and pigment in an upcoming post! Just know, they are an important weapon in our arsenal. This post would be 10 pages long if I included everything relevant LOL. In the meantime, have a look at my Retinoids blog for an overview.
RESOURCES
Below are some tried-and-true pigmentation busters as well as some new ones that incorporate my recent ingredient finds.
*Penn Smith Skincare is a participant in the Amazon Services LLC Associates Program, an affiliate program. Many links are affiliate links, meaning I am compensated when you shop through these at no extra fee to you.
SkinMedica Lytera 2.0
Lytera has a fantastic reputation. I've only just started testing it, but it has Tranexamic acid high in the ingredient list alongside some other tried and true pigment inhibitors. I'd say if money is no object this is a good one to try.
Dearskin Tranex
I've been talking about this serum for a couple of years now. It not only has Tranexamic acid, but it has a great cocktail of other fantastic pigmentation-taming ingredients like kojic acid and licorice extract. The only problem with Dearskin Tranex is that it's oftentimes sold out (and isn't widely available outside the US!!)
This has not only tranexamic acid but glutathione, plus niacinamide and vitamin C for brightening. I really like this - the only issues are that it is lightly fragranced (a problem for some, but not all) and also that it's often out of stock and not available outside the US.
Naturium Tranexamic acid 5%
This is another new serum I've been testing out. It's got a great range of ingredients for treating pigmentation. It also has great packaging and price point. It does take a few minutes to absorb but apart from that I really love this serum.
Essy Naturals Brightening Serum
I'm excited about this one because it contains 4-Butylresorcinol, quite high in the ingredient deck. I've been using it for a few months and really like it so far. Sadly, this is another serum that has fragrance in the ingredient list, so watch out if you're sensitive (but it is the very last in. Do note that this also contains 2% hydroquinone as one of it's pigment inhibitors.
Another daily lightweight serum that has an impressive ingredient deck. Boasting
4-Butylresorcinol, Kojic Acid, Lactic Acid, Salicylic Acid, and Morinda Citrifolia extract, this vegan, cruelty-free, and gluten-free formula is great for use every morning as long as no irritation arrises. I will say it again...SPF for sure!!
FAQ
Q1. Can I combine the above serums?
A1. Yes, you can but be careful combing multiple serums with AHAs. One serum in the mix with AHAs and BHAs is fine, but I wouldn't be layering several exfoliants on top of each other (especially because I know that many of you will still use your AHA toners and your L-ascorbic acid vitamin C serums...keep the additional AHAs and BHAs limited to avoid irritation). It is especially important if you have skin of color- added irritation can lead to more pigment...exactly what you don't want!
Q2. Is it best to use these ingredients morning or night?
A2. The products without AHAs may be used morning and night. I like to use the products with AHAs in the morning with other antioxidants and vitamin C. Sunscreen is a must as always. For example: I use my Queen 7-1 both AM and PM as one of the first products on my skin after cleansing (this product does not contain any AHAs or BHAs). Then I go on with my routine as usual, altering nothing to accommodate that serum.
Q3. How do I layer them with my other ingredients?
A3. Most of these products layer well with other acids (vitamin C included) and antioxidants. Be sure to check the labels of every product and take care when combining with retinoids as some of these do contain AHAs (which I recommend be used in a separate part of the routine than retinoids).
Q4. I'm using green LED for my hyperpigmentation. Can I apply any of these before LED for better activation?
A4. I would apply these after. There is no added benefit to applying these prior to LED in my opinion.
Q5. Can I use these actives in conjunction with cosmetic microneedling? Which one is best for that?
A5. I can only attest to tranexamic acid. In fact, one of the studies I sourced actually compared transdermal tranexamic acid (needled) to topical hydroquinone. The tranexamic acid performed quite well and is an accepted topical combined with needling. Remember though: the rest of the formula matters. Often what makes a product no good for needling is what is IN IT, not what isn't. You still need to do your due diligence and ensure that you are not needling anything in to the skin that you shouldn't. Tranexamic acid or not. I will research more thoroughly the use of glutathione with needling as well as butylresorcinol with needling and report back.
Q6. Are these ingredients likely to be effective on pigmentation on other areas of my body in addition to my face?
A6. Yes!!
I sure hope this helps you!
XOPenn
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Disclaimer: This post is not intended to provide diagnosis, treatment or medical advice. Content provided on this blog is for informational and entertainment purposes only. Please consult with a physician or other healthcare professional regarding any medical or skin related diagnosis or treatment options. Information on this website should not be considered as a substitute for advice from a healthcare/skin professional. The statements made about specific products throughout this website are not to diagnose, treat, cure or prevent disease. It is important that you check labels to determine if a product is right for you. Before starting any treatment at home consult a health care or skin care professional to determine if it’s right for you.