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What’s the best skin lightening ingredient? Episode 35

Do skin bleaching products really work? Are the ingredients safe? This week Randy and I explain everything you need to know about skin lightening.    

Show notes

Beauty Science News: 7 ways to spot a real expert

As you know we like to promote skeptical thinking, especially when it comes to beauty products. I found an interesting article from Forbes that gives 7 ways to tell you’re dealing with a real expert and not someone who’s just faking it.

  1. Real experts focus on their field, not themselves.
  2. Real experts have no trouble saying: “I don’t know.”
  3. Real experts demonstrate intellectual honesty.
  4. Real experts show intellectual curiosity.
  5. Real experts know when and how to share.
  6. Real experts know when and how to improvise.
  7. Real experts cannot help but teach.

Question of the week: What’s the best skin lightening ingredient?

Hannah from Australia asks…What’s in skin whitening products (or dark spot correctors or age imperfection correctors, or a million other confusing names.) What is it that’s bleaching away dark spots and is it good for you?

To understand skin lightening you first have to understand skin darkening. So let’s talk about what causes hyperpigmentation.

Causes of hyperpigmentation

Hyperpigmentation means your skin produces too much melanin. Melanin is the pigment that colors your skin, hair and the iris of your eyes. It comes from the Greek term meaning “dark.” Melanocytes are cells that actually create the pigment particles.  Melanosomes are little vesicles, or capsules, that hold the melanin and carry them to various parts of the skin.

There are 2 basic causes of HP. Not surprisingly, both involve melanocytes which are the pigment producing cells in your skin.

1. If the melanocytes increase the amount of melanin they produce, this is called  Melantotic HP (melan-tot-ic)

2. If the melanocytes make the same amount of pigment but the NUMBER of melanocytes are increased, this is called Melanocytic HP (melano-cy-tic). Both conditions lead to increased melanin.

HP is further classified by WHERE this excess pigment is: If its in the outer layer it’s called Epidermal HP In the middle it’s called Dermal HP. There are many different types of HP…here are some of the most common.

Freckles

Everyone is familiar with freckles but I bet you didn’t know that they are technically called  (ephelides) e-fel-i-deeze.  These are melantotic which means your skin has a normal number of melanocytes but they produce more pigment. And the more you are exposed to the sun, the more freckles you’ll get and the darker they’ll become. Also, freckles are kind of the cute version of skin HP.

Age spots

Age spots are formally known as Solar Lentigines (len-tij-in-eeze ) and they are  small brown patches on the skin. As the name implies, they are caused by sun exposure.  These used to be called “liver spots” because they were associated with liver problems that occur as you age. Lentigines are melanocytic which means they are caused by the creation of MORE melanocytes.  While these are triggered by sunlight, once they’re formed they pretty much stay stable in their color even if you get more sun exposure.

Post inflammatory HP (PIH)

This is skin darkening that occurs as a result of skin injury or trauma. As part of the healing process the melanocytes kick into high gear and produce more pigment. These spots may become darker if exposed to sunlight. Two examples: dark marks from acne. Have a zit which is infected, the trauma causes the “scar.” Do you know another area of the body that’s prone to PIH? Armpits! Shaving your pits causes some micro trauma which triggers melanin production. A lot of people complain about dark armpits. Even rubbing of clothing agains armpits can cause this.

Melasma

It causes brown to gray-brown patches on the face. Most people get it on their cheeks, bridge of their nose, forehead, chin, and above their upper lip. It’s caused by sun exposure but may be triggered by hormones so you can get it due to pregnancy or taking a contraceptive pill. In fact, it’s so common that it’s called “the mask of pregnancy.”

Other conditions

Acral melanosis usually located on the acral areas of the fingers and toes. It is mostly seen in newborns or during the first years of life. Not very common. Tinea versicolor – typically occurs on the chest and it is caused by yeast growing out of control. It is one of the most common skin diseases in tropical and subtropical areas of the world.

How to treat HP

For each of these conditions, treatment depends on WHERE the pigment is. For Dermal HP – there’s not much you can do. Not much helps with this except for certain lasers. You basically have to cover it up. Epidermal HP – The good news is that most common types, like freckles and age spots, are epidermal so you have several treatment options.

  • Topical treatments – creams and lotions
  • Abrasive methods – chemical peels (combined with topical)
  • Surgical methods (Dermabrasion, Cryosurgery, Lasers)

Since Hannah asked about creams and lotions, we’ll limit out discussion to the pros and cons of skin lightening creams and lotions.

Hydroquinone

What is HQ and how does it work?
HQ , like many skin lightening ingredients, is a phenolic compound. That means it contains a 6 carbon ring with an OH group attached. This structure allows it to inhibit melanin synthesis by acting as a substrate for tyrosinase. Tyrosine, an amino acid, is acted upon by the enzyme tyrosine to form melanin. These phenolic compounds “interrupts” this reaction by giving the tyrosine something else to attach to. That way the tyrosine never makes melanin particles.

Nothing works better than HQ – it’s considered the gold standard for skin lightening. Here’s a quote from Dr. Rendon, associate clinical professor, University of Miami who says “other products haven’t proven that they really are as good as they say they are. In the few studies that actually compare them to hydroquinone, they never beat it.” Now, that doesn’t mean it works instantly – it can take several months of usage to reach maximum lightening efficacy.

What are the concerns about HQ?
There are some concerns about HQ, as you probably have heard. The reaction that’s responsible for it working so well also causes damage to the melanosomes and melanocytes which is one of the reasons HQ raises safety concerns. And animal and cell culture studies have shown that HQ can cause DNA damage which has raised concerns about cancer. Another concern:  In some people HQ causes a condition called Ochronosis (Oak-row-know-sis) which is a permanent bluish-black discoloration of the skin. This is rare and some dermatologists say it only occurs after prolonged use of high concentration hydroquinone.

So is HQ safe or not?
These studies that raised cancer concerns were based on oral or injected application and there have been no clinical studies or cases of skin cancer or any kind of internal malignancy related to topical HQ use. Therefore, the International Agency for Research on Cancer  (IARC) considers hydroquinone as “not classifiable” as to its carcinogenicity in humans. As far as the Ochronosis is concerned, this is one of reasons that regulatory bodies in other countries have banned HQ for over the counter use. It has has to be prescribed by a doctor which helps prevent the kind of long term abuse that can lead to that permanent discoloration. In the US The Food and Drug Administration (FDA) has even proposed banning over-the counter skin bleaching agents containing hydroquinone but as of right now it’s still available.

(Very important point – it’s a myth that’s it’s “banned” in other countries, it’s really just restricted to prescription use. Europe and Asia currently allow hydroquinone at 2-5% concentration by prescription. The drug is valued worldwide but is regulated to protect against misuse and bad formulations.)

There are quite a few other ingredients which have skin lightening properties but based on everything we could find, nothing works as well as HQ and some of the ingredients that work pretty well have their own issues. While it’s generally recognized that HQ is the gold standard, there are not a lot of studies directly comparing all these other agents to each other. So it’s difficult to rank them. But we’ll give you a quick run down.

Mequinol

This is a derivative of HQ which According to Dr. Draelos, this outperforms OTC alternatives and is a prescription alternative to hydroquinone. Of course, as you’ll see with almost all these agents it has side effects as well which include erythema, burning, pruritus, desquamation, skin irritation.

Azelaic acid

It’s a dicarboxylic acid which occurs natural in wheat, rye, and barley. inhibits DNA synthesis in melanocytes and has a modest antityrosinase effect. According to some sources, it works better than 2% hydroquinone and about as good as 4%. The interesting thing is that its apparently safe to use during pregnancy. Side effects of itching, mild redness, scaling, and burning but overall this is a good contender. It’s also prescription. Kojic acid This is a fungal metabolite and also a famous cop show from the 70s. It works by inhibiting the production of free tyrosinase. Could not find any data directly comparing it to other agents but one source considers it to be be the most effective skin-lightening agent behind hydroquinone. We do know that it can cause greater irritation, it is highly sensitizing and may be mutagenic. For this reason, it is banned in Japan, just like over-the-counter (OTC) hydroquinone.

Alpha arbutin

Arbutin is chemically related to hydroquinone and was originally obtained from the bearberry plant. Like HA it decreases melanin biosynthesis through the inhibition of tyrosinase activity.  It also inhibits melanosome maturation and is less cytotoxic to melanocytes than hydroquinone. However, several studies have shown that arbutin is less effective than kojic acid for hyperpigmentation. Deoxyarbutin is a synthesized topical derivative. Studies have shown that it has an enhanced sustained improvement, general skin lightening and a safety profile comparable to hydroquinone.

Vitamin C

A study compared 5% ascorbic acid and 4% hydroquinone in 16 female patients with melasma and found 62.5% and 93% improvement respectively

Niacinamide

It works by interfering with the interaction between keratinocytes and melanocytes, thereby inhibiting melanogenesis. We’ve talked about this in our anti-aging show and it does work but not much data comparing it to other options.

Licorice extract

Licorice extract improves hyperpigmentation by dispersing the melanin, inhibition of melanin biosynthesis and inhibition of cyclooxygenase activity thereby decreasing free radical production. Glabridin, a polyphenolic flavonoid is the main component of licorice extract. Studies have shown that glabridin prevents Ultraviolet B (UVB) induced pigmentation and exerts anti-inflammatory effects by inhibiting superoxide anion and cyclooxygenase activity. However, more studies are needed to prove its de-pigmenting action.

Retinoids

Works three ways: dispersion of keratinocyte pigment granules, interference with pigment transfer, and acceleration of epidermal turnover Something like 68% improvement (although you can’t really compare numbers across studies.) Side effects: erythema, peeling, and possible post inflammatory hyper pigmentation. Can help with Melasma which is in the dermis. Works very slowly. Takes 24 weeks or more at 0.1% Need a prescription. One paper we found listed something links an additional 16 other ingredients that have some data but not enough to fully validate them.

Undecylenoyl phenylalanine (Update 3/20015)

We just became aware of another ingredient Undecylenoyl phenylalanine. We don’t know much about this yet but here’s a quote from the Cosmetic Cop that provides a couple of helpful references:

“Although this ingredient’s research pales in comparison to what’s known about hydroquinone and many forms of vitamin C, it is a promising ingredient that is worth considering in products meant to lighten brown spots and help even out skin tone (Sources: Journal of Cosmetic Dermatology, September 2011, pages 189–196 and December 2009, pages 260–266; and Clinical Experiments in Dermatology, July 2010, pages 476–476).”

Skin lightening vs brightening vs “imperfection correctors”

True skin lightening products are drugs and have to be labeled with very specific language. If you are selling an HQ product it has to bel labeled as a “skin lightener” or a “skin bleach.” If you are selling a cosmetic that uses any of the other ingredients we talked about you CAN’T call it a skin lightener or a bleach which is why you see products called “brighteners” imperfection correctors” and so forth. These are marketing terms that are NOT regulated by law which explains why they are so confusing. Our recommendation is not to pay too much attention to the name but rather look for the active ingredients.

The Beauty Brains bottom line

Check with your doctor but based on the evidence we’ve seen, for treatment of isolated areas of hyper-pigmentation (a couple of dark spots here and there), short term use of hydroquinone followed by the use of sun protection is most effective. Under those use conditions they’re don’t appear to be any serious health issues. We do not recommend it for long term use over larger areas of your body (e.g, trying to lighten overall skin tone).

References

http://www.jcasonline.com/article.asp?issn=0974-2077;year=2013;volume=6;issue=1;spage=4;epage=11;aulast=Sarkar

http://palaeo.gly.bris.ac.uk/melanosomes/melanin.html

http://www.fda.gov/downloads/Drugs/DevelopmentApprovalProcess/DevelopmentResources/Over-the-CounterOTCDrugs/StatusofOTCRulemakings/ucm094385.pdf

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{ 22 comments… add one }

  • Eileen June 17, 2014, 11:43 am

    Wonderful post. Comprehensive without getting mired in too much technical detail. In short, consumer friendly 🙂 I’m particularly glad that you debunked the myth that hydroquinone is banned in other countries. That is the first thing the fear-mongers say when talking about the “evils” of hydroquinone. True, it is a powerful skin lightener, but banning something and moving it into the prescription only category is hardly the same thing. Used properly and under a dermatologist’s supervision, hydroquinone is safe and effective. It is, indeed, the gold standard for skin lightening.

    Back in the 60’s I developed melasma as a result of the ridiculously strong birth control pills of that era. A dermatologist treated it with hydroquinone applied morning and night and sunscreen applied every single day no matter what. Interestingly, when I got the script for hydroquinone filled, I also had to order the sunscreen; not because it was by prescription, but because it was so rare that most people didn’t even know it existed. Hydroquinone to lighten and sunscreen to protect did a beautiful job of evening my skin tone. I do think that moving hydroquinone into the prescription category makes sense, though. It is powerful and there will always be those people who mis-use it.

    • admin June 17, 2014, 6:46 pm

      Eileen: I always REALLY enjoy your well thought out comments. Thanks for being part of our community!

    • Jes May 28, 2016, 5:15 pm

      Do you remember the nMe of the sunscreen?

  • Tree June 17, 2014, 12:25 pm

    What about products that promise to make your skin lighter, not fight hyperpigmentation? They are very popular in Asia, are they essentially using the same ingredients as for hyperpigmentation? Or are they completely different? I’ve heard it’s not politically correct to discuss this in the US, but I guess you can make an exception for us foreigners 🙂
    One brand sells whitening creams with tomato, I wonder if that has any real effect or it is just a marketing story.
    Btw, it will be cool if there is an option to subscribe for future comments.

    • admin June 17, 2014, 6:46 pm

      They use the same technology.

    • Eileen June 17, 2014, 7:24 pm

      Hi Tree,

      Tomato is an acidic fruit and lightens the appearance of the skin via the gradual exfoliation of the surface. Some homemade skin lightening remedies call for tomato alone, but more often it is combined with lemon juice. (You can Google it). It was a pretty common combination in the 1800’s. It only acts on the surface, is very gradual, and does not offer a permanent solution.

  • Ruth Marie June 17, 2014, 3:05 pm

    My first show. Goodness! you Silly boys made me giggle. Dig it MAN !! groovy 🙂 ruth

  • Christina June 17, 2014, 9:58 pm

    Hyperpigmentation is easily one of the most sought out growing categories.

    There are many over the counter forms of Hydroquinone still available at a 2%. I swear by Hydroquinone for clients with a 3 months on then 3 months off routine. During the 3 months off I suggest a Licorice/Mulberry based treatment to sustain their progress while giving their system a break.

    Informative as always Beauty Brains! Not to mention the crickets sound effect took it to a whole new level. Do I see a Beauty Brains soothing sounds CD in the future?

    • Randy Schueller June 17, 2014, 10:39 pm

      I’m working on a “babbling brook” sound effect for those episodes where Perry gets a little too verbose.

  • Christina June 18, 2014, 12:33 am

    ..and of course audio books on tape of Perry reading in different character voices. Hopefully the authors will supply masculine female characters since we discovered this podcast that Perry does not yet have the vocal range to emulate a female voice. :op

    Nothing but love Perry! Nothing but love.

  • Chante Chanel June 18, 2014, 1:45 pm

    I like that you included the distinction between skin lightening and skin brightening. It makes sense and is very understandable and clear. Thank you!

  • Emily @ Tips on Healthy Living June 19, 2014, 12:40 am

    Honestly, one of the most clear and concise articles about lightening dark spots on skin that I’ve ever read. Thank you!

  • Leigh June 25, 2014, 9:04 am

    Hi there! I am a new listener and have been getting caught up with previous episodes.

    I just purchased a product with 4% Hydroquinone. The directions are to use twice a day.

    But, based on your advice, I am wondering if this would be too often? I was also going to use on my whole face, but maybe that is not so great.

    Also, does a person need to keep using Hydroquinone to keep the age spots faded; or once they are faded they will remain so as long as you use sunscreen?

    Thanks for the help! and the always interesting information

    • Randy Schueller June 25, 2014, 12:22 pm

      You could always check with your doctor about using 4% HQ, Leigh. And once the age spots have faded sunscreen should be enough to keep them at bay. Keep your fingers crossed!

      • Leigh June 25, 2014, 4:25 pm

        Thank you for the reply!

  • Sara January 15, 2015, 3:30 pm

    I like that you included the distinction between skin lightening and skin brightening. It makes sense and is very understandable and clear.

  • Grace July 21, 2015, 3:57 am

    Hi, Beauty Brains! I’m quite interested in this topic and wondered if I could ask a few questions:

    1) I saw in a research paper comments about the effects of fatty acids on the biochemical pathways associated with skin pigmentation. It seemed to be suggested that things like stearic and palmitic acids could negatively impact the skin lightening process while linoleic acid, oleic acid, and a few others have the capacity to lighten skin significantly. If I’m trying to keep my skin light as a fairly pale person, should I consider that notion? A lot of lotions and moisturizers seem to have stearic acid in them, but since reading that, I have also discovered that palmitic and stearic acids are found in combination with oleic and lineoleic acids as part of plant oils that are otherwise quite useful, or at least seem to be. I don’t know if there being that combined aspect of fatty acid varieties mitigates the potential negative effects of palmitic and stearic acid, and the complicated references to these ubiquitous acids has been very confusing reading indeed.

    2) What about commonly found Asian skin lightening substances like (topical) glutathione or papain? Also, there seems to be a lot of information about the potential harm of taking licorice as a supplement. Are topical applications of licorice likely to be exempt from that?

    3) Why are so many of ingredients used for this purpose irritating? Also, acidic skin lightening products designed to be washed off seem a bit less irritating than, say, creams — but is it only because they aren’t really doing anything in that relatively short timeframe?

    Thanks for reading, and for the reading material!

    • Randy Schueller July 21, 2015, 8:19 am

      Hi Grace!

      1. Lots of substances can “impact the biochemical pathways” but that doesn’t mean they have that effect when applied topically. As we noted in the show, we could only find a few ingredients that have been proven to lighten skin and the fatty acids you mentioned weren’t included. (I’d love to take a look at the study you cited if you can provide a link.)

      2. Kind of the same answer as #1: I’d stick with the ingredients that have been proven to work.

      3. Wash off products are less likely to irritate but they’re also much less effective at delivering active ingredients compared to leave on products.

      • Grace July 23, 2015, 6:49 am

        Hi! Thanks for answering. I really appreciate that. The fatty acid information is mentioned in a couple of research papers I’ve seen, with the most easy to locate being Ebanks, J.P., Randall Wickett, R., and Boissy, R. E. 2009, “Mechanisms Regulating Skin Pigmentation: The Rise and Fall of Complexion Coloration”, International Journal of Molecular Sciences, Vol. 10, No. 9, pp. 4066-4087.

        The section on linoleic acid includes the following information:

        “6.3. Linoleic Acid

        Unsaturated fatty acids including oleic acid (C18:1), linoleic acid (C18:2) or α-linolenic acid (C18:3) suppresses melanogenesis and tyrosinase activity, while saturated fatty acids such as palmitic acid (C16:0) or stearic acid (C18:0) increases it [113]. Linoleic acid reduces the activity of tyrosinase in melanocytes, while mRNA levels remain unchanged [51]. No evidence of change in TYRP-1 and TYRP-2 protein levels suggest that fatty acids selectively target tyrosinase. This may influence the enzyme’s degradation via a physiologic proteasome-dependent mechanism, altering the tyrosinase protein content in hyperactive melanocytes [10,114]. Linoleic acid also influences skin pigmentation by stimulating epidermal turnover and increased desquamation of melanin pigment from the epidermis [51]. Studies completed to assess the skin lightening capabilities of unsaturated fatty acids, linoleic acid or α-linoleic acid, on UV induced hyperpigmentation of brown guinea pig skin, showed an efficient lightening effect [115]. It is thought that the unsaturated bonds of these molecules can be easily peroxidized, which in combination with an increase in epidermal turnover, correlate with an inhibitory effect on melanogenesis in vivo[51,115].”

        (The relevant references cited in-text in this extract are:

        10) Briganti, S; Camera, E; Picardo, M. Chemical and instrumental approaches to treat hyperpigmentation. Pigment Cell Res 2003, 16, 101–110.

        51) Badreshia-Bansal, S; Draelos, Z. Insight into skin lightening cosmeceuticals for women of color.J. Drugs Dermatol 2007, 6, 32–39. 

        113) Ando, H; Funasaka, Y; Oka, M; Ohashi, A; Furumura, M; Matsunaga, J; Matsunaga, N; Hearing, V; Ichihashi, M. Possible involvement of proteolytic degradation of tyrosinase in the regulatory effect of fatty acids on melanogenesis. J. Lipid Res 1999, 40, 1312–1316. 

        114) Halaban, R; Cheng, E; Zhang, Y; Moellmann, G; Hanlon, D; Michalak, M; Setaluri, V; Hebert, D. Aberrant retention of tyrosinase in the endoplasmic reticulum mediates accelerated degradation of the enzyme and contributes to the dedifferentiated phenotype of amelanotic melanoma cells. Proc. Natl. Acad. Sci. USA 1997, 94, 6210–6215.

        115) Ando, H; Ryu, A; Hashimoto, A; Oka, M; Ichihashi, M. Linoleic acid and α-linolenic acid lightens ultraviolet-induced hyperpigmentation of the skin. Arch. Dermatol. Res 1998, 290, 375–381.)

        • Randy Schueller July 23, 2015, 8:32 am

          Very interesting, Grace! I had not heard this before and I’m surprised by that fatty acids would have this effect. Linoleic acid does penetrate skin so it seems plausible it could interact with melanocytes (which seems to be confirmed by the guinea pig study cited above.) The other fatty acids mentioned don’t penetrate skin much (at least as far as I know.)

          The missing piece of information here is how the lightening effect of linoleic acid compares to something like hydroquinone. My guess is that it’s much less effective or else we’d already be seeing skin lightening products based on linoleic acid.

  • DC April 16, 2016, 12:35 pm

    Hey guys!

    Thanks for the great podcast! It was super enlightening. I’ve heard so many dubious skin lightening “miracle” ingredients talked about like they’re the second coming, so it’s nice to hear some advice that’s actually grounded in data and science.

    After listening to your podcast, I started doing some research on hydroquinone, and I found this interesting product that seems too good to be true! I wonder what you think of it. It’s a 1% hydroquinone serum that’s sold on Etsy (!) and it also includes kojic acid, alpha arbutin, vitamin c and hyaluronic acid among others. It costs about $15 for 1.5 ounces.

    The listing is here in case you want to take a look: http://etsy.me/1qxcBfp

    I recognise at least 3 ingredients in there that you spoke favourably about, so my heart is all aflutter! Could this formulation be the freckle-banishing unicorn serum of my dreams? Or will all those skin lightening ingredients bleach my face into oblivion?

    Any advice or insight is appreciated! Thank you! (And, of course, I understand that your advice is just advice and should not be taken as a doctor’s order or anything like that!)

    • Randy Schueller April 17, 2016, 10:05 am

      I haven’t seen any evidence that combining these active ingredients gives you any boost in performance. The good news is it’s relatively cheap and it’s unlikely to do any additional harm to your skin so give it a try!

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