Getting under the skin of hyperpigmentation and dark spots

There are two key actives required for managing hyperpigmentation (dark spots, age spots, or whatever you want to call them): patience and diligence. A third requirement is to have realistic expectations. I haven’t yet found the killer app for hyperpigmentation, but I have finally come to the breakthrough conclusion that there is a regimen, rather than a single product application, that is required to make any inroads on fading dark spots. If I’m right then I hope to make greater advances in the coming months. But I’ll come back to that in a second.

First, you need to appreciate that hyperpigmentation is stubborn. It has taken years, probably most of your adult life, to form. Mostly it comes down to melanocyte activity. There are typically between 1000 and 2000 melanocytes per square millimeter of skin and make up about 5% to 10% of the cells in the basal layer of epidermis (incidentally, black and white skins possess the same number of melanocytes).

Freckles, for example, are red patches due to hyperactive melanocytes that start in infancy, particularly in fair skins, and on exposed areas of the epidermis. Chloasma, also known as pregnancy mask, is due to excessive melanocyte activity forming symmetrical patches on the face in pregnancy or as a result of oestrone/progesterone therapy. Senile-lentigines or liver spots are brown patches on the forearms, face and hands due to a proliferation of melanocytes.

After doing a fair amount of reading on the subject, I have come to the conclusion that my approach which has been try to tackle dark spots with some kind of melanin or tyrosinase inhibitor is limited. And that’s certainly been my experience. I try fading and brightening creams, successful fading is limited, I get bored and give up. The better approach is a regimen: 1) exfoliate the damaged skin, 2) protect new skin from further sun damage, 3) use a melanin inhibitor and 4) give the regimen a big boost a few times a week with green LED light therapy.

Come to think of it, Lumixyl has a glycolic peel, brightening cream and a sunscreen. I now think all those stages are necessary. However, I do understand that most of us don’t like to feel locked into an entire range and I think its fine to mix and match with your favorite exfoliator (some kind of glycolic peel - Juice Beauty, La Vie Celeste, Reviva, to name a few - or an antioxidant/exfoliator such as Your Best Face Prep would be ideal) and sunscreen.

Regarding the melanin inhibitor, there are a confusing number of actives to choose from and so here’s a rundown of some of the most common.

Hydroquinone is an effective inhibitor of melanogenesis. But it achieves this by being cytoxic to melanocytes. Concerns about cancer have restricted the use of hydroquinone in Europe and Japan. Generally, these days, people try to find alternatives.

Tyrosinase inhibitors are alternatives to hydroquinone that are considered safer. Melanin forms through a series of oxidative reactions involving the amino acid tyrosine in the presence of the enzyme tyrosinase. Hence, some actives focus on inhibiting tyrosinase.

One such active is decapeptide-12, a synthetic peptide comprising a sequence of amino acids developed by dermatological researchers at Stanford University, and used in Lumixyl’s Brightening Crème.

SymWhite 37 (phenylethyl resorcinol) is a synthetic compound partly derived from natural lightening compounds in scotch pine bark. Studies have shown that it is effective at brightening skin without harmful side effects.  Used in Lumixyl Brightening Creme.

Arbutin (hydroquinone-beta-D-glucopyranoside) A glycosylated hydroquinone found at high concentrations in certain plants and capable of surviving extreme and sustained dehydration, arbutin has been shown to inhibit melanin synthesis by inhibition of tyrosinase activity. A one-month study on 80 Chinese women, using a 1% alpha arbutin concentration, resulted in a “skin lightening effect”. It was faster and more effective than kojic acid (see below). Used in Restore by Your Best Face.

Glabridin (licorice extract) inhibits tyrosinase activity of melanocytes without cytotoxicity. Having said that, most of the research on licorice extract is on its antioxidant properties.

Magnesium ascorbyl phosphate is a non-irritating, stable form of vitamin C. It can be used at concentrations as low as 10% to suppress melanin formation.

Hexylresorcinol: In vivo studies conducted on .5% hexylresorcinol in 2007 demonstrated lightening results that were just as effective as 2% hydroquinone over an eight-week period. Used in Prescribed Solutions A Bolt of Lightening.

Cinnamomum subavenium is one to look out for. As Sarah reported, two chemicals have been isolated from this plant that can block tyrosinase at only a 1% concentration. As far as we know, it hasn’t yet made it into cosmetic products, but we will be excited to try it out when it does.

Some hyperpigmentation actives that, for various reasons, might be best avoided include:

Azelaic acid is a rather weak competitive inhibitor of tyrosinase in vitro. In addition, azelaic acid has an antiproliferative and cytotoxic effect on melanocytes.

Kojic acid decreases melanin content, but it is dose dependent (at 1% or less, it doesn’t work) and at higher doses can be a strong irritant.

Retinoids such as tretinoin and adapalene are derivatives of vitamin A. The mechanisms for reducing pigmentation include inhibition of tyrosinase induction, interference with pigment transfer, and acceleration of epidermal turnover. They also have the ability to disperse pigment granules within keratinocytes. Retinoids may act as penetration enhancers when used with other lightening agents such as hydroquinone and mequinol. The most common adverse effects include burning, stinging, erythema, dryness, and scaling. Although the adverse effects are reversible, retinoid use may result in hyperpigmentation, especially in dark-skinned individuals.

I'm going to be working on my exfoliate, protect, inhibit and light therapy hyperpigmentation regimen and will report back as I find (hopefully) combinations of products that work.

  • talia says:

    One ingredient that also seems to help with hyperpigmentation is myristyl nicotinate and/or niacinimde. The 5% concentration in Nia24 seems to work well at inhibiting brown spots.

    Posted on September 28, 2011 at 11:39 am

  • Darrell says:

    Another natural antioxidant and brightening ingredient that holds good promise, and is worth keeping an eye out for, is trans-resveratrol.

    You'll also sometimes see trans-resveratrol listed in products by the trade name Regu-Fade.

    -Darrell

    Posted on September 28, 2011 at 12:21 pm

  • Howard says:

    Please for
    give my ignorance but how does
    trans-resveratrol compare to resveratrol?

    Posted on September 28, 2011 at 12:34 pm

  • Darrell says:

    Hi Howard,
    Trans-resveratrol is produced from another plant (called Japanese Knotweed, which is high in resveratrol) whereas traditional resveratrol comes from grapes.

    Trans-resveratrol is often marketed as free(er) of contaminants, though I have not seen anything that would indicate regular (grape-produced) resveratrol poses any contaminant concern.

    -Darrell

    Posted on September 28, 2011 at 12:42 pm

  • In the REVERSE Regimen of Rodan & Fields Dermatologists products, two of the four products each have 2% Hydroquinone. In three weeks, my sun/dark/age spots began to fade and by eight weeks were significantly faded to my satisfaction. Please peruse my website for more information.
    http://cassieskincare.myrandf.com (Cassie Fishbein)

    Posted on September 28, 2011 at 2:07 pm

  • Carol says:

    I got a brown spot the size of my fingertip on my cheek below my right eye last summer after being on a sailboat for a few days. It was extremely noticeable in photographs even with makeup on. One night after I washed my face before bed, I dabbed on some glycolic acid cream (15%) and after that dried I dabbed on a mandelic acid 15% serum. It began to sting so I rinsed it off after a few minutes. The next day, it looked like I had burned my skin in that spot but after a few days the skin peeled away and the spot was gone! This summer, the spot reappeared and I repeated the process. It works!!! Yes, it looks ugly for a few days but it is perfectly gone afterwards! It is probably similar to what a dermatologist would do to remove it but it didn't cost me anything.

    Posted on September 28, 2011 at 5:21 pm

  • patrice says:

    Well I hate to sound so basic but just plain ole apple cider vinegar is what has tamed my age spots down to barely visible. Then my 88 year old mother who had a large one on her left forearm rubbed vinegar over her arms, she said for 3 days, but I suspect it was a bit longer and she said she could not believe but it just faded away and the others on her arm have lessened. So what's there to lose nothing but saving lots of money.

    Posted on September 28, 2011 at 6:23 pm

  • Dennis says:

    I had some faint hyper pigmentation after a TCA peel, which was my fault for not being patient and picking at the scabs. I managed to completely clear it all up in roughly two months by alternating a glycolic cream, retin-a, and a vitamin c (tetrahexlydecyl ascorbate) serum.

    Posted on September 28, 2011 at 10:31 pm

  • jc says:

    sorry darrell, the difference of resveratrol and trans-resveratrol does not lie with the source. my regular resveratrol product uses japanese knotweed as it's source, yet the company sells a trans-res product. my understanding is trans-res(a metabolite of resveratrol) is more 'bio available' meaning more readily accepted and incorporated into our system. it doesn't lose any potency going through whatever processes it takes for our bodies to make resveratrol useful to them. so in essence taking trans resveratrol should give you the full effects of the dose, whereas you would lose some by taking a 'regular' resveratrol product.

    Posted on September 29, 2011 at 3:43 am

  • Darrell says:

    Hi JC,
    Thank you -- I've only seen that trans-resveratrol is sourced from Japanese Knotweed, but that's just my context as it has to do with ingredients sourced for topical use. I know that the form of trans-resveratrol we use is sourced from Japanese Knotweed.

    However, you've highlighted a great bit of info about internal use and bio availability of trans vs resveratrol for those taking supplements.

    -Darrell

    Posted on September 29, 2011 at 6:30 am

  • Marta says:

    Patrice, I am heading for the apple cider vinegar right now

    Posted on September 29, 2011 at 6:41 am

  • Jaysie says:

    Patrice, I'm right behind Marta going for the apple cider vinegar. Did you use the plain old stuff from the grocery store, or that organic brand, Mrs. Bragg's I think it's called?

    Posted on September 29, 2011 at 3:29 pm

  • Karen says:

    Hi Martha,

    May you please explain a bit about the green led light therapy?I would like to buy one and have a try..Does it works and which one would you recomend?Much appreciated if you could reply!

    Thanks

    Posted on September 29, 2011 at 4:57 pm

  • Kim says:

    Can you point us to anything that explains exactly how the green light diminishes the brown spots from the melanocytes. I've been lemming the Sirius Aurora for some time now, particularly because it has a green light as well. I'm just having trouble understadning- is it killing melanocytes? Deactivating the production of melanin? Dispersing already existing melanin? So far I use exfoliation plus sun protection and have experimented with fading serums without additional effects. The green light seems interesting, but I'd like to know more before I purchase. The Sirius site doesn't cite studies about how it breaks up the visible melanin spots. Thanks so much- this is such a stubborn issue!

    Posted on September 30, 2011 at 7:56 am

  • imelda says:

    Hi, Marta!
    Do you do step 2 (protect with Sun screen) first before applying the melanin inhibitor? I just assumed the sun screen goes last, which I've been doing in the past when I tried the Lumixyl system, following their steps. Please advise. Thanks!

    Posted on September 30, 2011 at 7:57 am

  • Marta says:

    Good point Imelda. I would put the sunscreen after the inhibitor - unless I was not putting that on immediately after the glycolic (in which case, I'd put the sunscreen after the peel).

    Posted on September 30, 2011 at 9:45 am

  • Marta says:

    Hi Kim, you are right there isn't much research on the green LED. This is how it theoretically works: green light targets melanocytes, melanin-producing cells located in the bottom layer of the skin’s epidermis. According to Sirius, it inhibits the production of excess melanin, prevents it from traveling to the skin’s surface, and breaks up melanin clusters to diminish existing discoloration. I wrote about it here: http://truthinaging.com/face/green-its-the-new-red

    In practice, I have seen results and a friend also had great results on her hands.

    Posted on September 30, 2011 at 9:51 am

  • Hi Marta,
    Have you had a chance to try La Isha's Natural Age Spot Eraser? We have had phenomenal results with age spots as well as melasma and the hormonally-induced "mask-of-pregnancy". Our solution to this problem is a blend of clinical-grade essential oils that work to gradually and gently lighten dark spots without irritating the skin. Check out our Testimonials to read what some of our clients have said about it on http://goo.gl/GMCNE

    Wishing you the blessings of good health and timeless beauty,
    Sharon Gnatt Epel
    CEO/Founder La Isha Natural Anti-Aging SkinCare

    Posted on October 1, 2011 at 11:11 am

  • Marta says:

    Hi Sharon, apologies for the tardy response. I'd love to give it a try.

    Posted on October 4, 2011 at 9:29 am

  • JustD says:

    My mom has large deeply pigmented spots on her cheeks, which we had a dermatologist look at and it was very similar to the mask, which I suspect it was because my Mom wasn't given to HRT and it finally caught up with her in her late 60s. Despite some topical medication she was given, which I doubt she used, it didn't change, but incredulously, aside from that she has beautiful skin still. I don't get it, anyway I'd like to have a go at trying your La Isha’s Natural Age Spot Eraser. Thanks for the post Sharon! Checking out your website and testimonials.

    Posted on October 4, 2011 at 10:46 am

  • JustD says:

    After reading your About Us info and purusing many of your very interesting products, I purchased the sampler pkt. to give it a try and see how your products work for me. Thanks for the free ship on this order, very gracious.

    Posted on October 4, 2011 at 11:21 am

  • Donna says:

    I have 2 large dark spots (one on each cheek)
    that I have been working on for months. I will give the applecider vinegar a try.
    Anyone have any luck with this or anything else?

    Posted on November 13, 2011 at 6:24 pm

  • Ana says:

    Hi Marta,
    Did you try the apple cider vinegar? Curious to find out!
    I dabbed a little on a spot on my cheek and my skin turned bright red ... so not planning to try it again soon until I find out how I'm supposed to do it!

    Posted on January 30, 2012 at 3:22 pm

  • Carolyn says:

    are there any reports back/further instructions on the acv? TIA, as it were : )

    Posted on March 24, 2012 at 4:16 pm

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