Skin Brightening Ingredients!!




Skin Care Products:

“Always tap. Don’t rub.”


1. Hydroquinone (HQ)

What is HQ and how does it work?
HQis a phenolic compound.  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.

A prescription strength retinoid (0.5% tretinoin) steroid (0.01% fluocinolone acetonide) and Hydroquinone

A skin-lightening ingredient that works by inhibiting the activity of tyrosinase, by acting as a melanocyte cytotoxic inhibitor, and by increasing the cytotoxicity of melanocytes.

Hydroquinone (Wikipedia)

<p><b>Hydroquinone</b>, also <b>benzene-1,4-diol</b> or <b>quinol</b>, is an <a href=”; title=”Aromatic” class=”mw-redirect”>aromatic</a> <a href=”; title=”Organic compound”>organic compound</a> that is a type of <a href=”; title=”Phenols”>phenol</a>, a derivative of <a href=”; title=”Benzene”>benzene</a>, having the <a href=”; title=”Chemical formula”>chemical formula</a> C<sub>6</sub>H<sub>4</sub>(OH)<sub>2</sub>. Its <a href=”; title=”Chemical structure”>chemical structure</a>, shown in the table at right, features two <a href=”; title=”Hydroxyl group” class=”mw-redirect”>hydroxyl groups</a> <a href=”; title=”Covalent bond”>bonded</a> to a <a href=”; title=”Benzene ring” class=”mw-redirect”>benzene ring</a> in a <a href=”; title=”Arene substitution patterns” class=”mw-redirect”><i>para</i></a> position. It is a white granular <a href=”; title=”Solid”>solid</a>. Substituted derivatives of this parent compound are also referred to as hydroquinones. The name “hydroquinone” was coined by <a href=”; title=”Friedrich W&ouml;hler”>Friedrich W&ouml;hler</a> in 1843.</p>

<!– mw container end –>”>hydroquinone (4%) has been shown to be effective in treating melasma and general darkening of the skin over the course of eight weeks. According to Dr. Audrey Kunin, M.D., a Kansas-City based dermatologist, should not be used for longer than eight weeks, as the steroid component may cause the skin to become thinner ( (and hence more photosensitive and prone to sun-induced signs of aging, etc.).

What hydroquinone is used for: Since 1982, hydroquinone has been FDA-approved for the treatment of freckles, melasma, and general brown patching. Today, hydroquinone is the most commonly used bleaching agent in the United States.

How hydroquinone works: Hydroquinone works in two distinct ways: 1.) inhibiting tyrosinase, the rate-limiting enzyme of melanin (i.e., pigment) production, and 2.) increasing the cytotoxicity of melanocytes, the melanin producing-cells.

Risks: Unfortunately, hydroquinone has been banned in some countries, including France and South Africa, for concerns about increased cancer risk and ochronosis (darkening of the skin) with its use. Yet I have yet to encounter an American dermatologist who believes hydroquinone in skin care products increases cancer risk. Dr. Susan C. Taylor, M.D., a Philadelphia-based dermatologist, states, ”The maximum levels of hydroquinone currently allowed (2 percent for over the counter, 4 percent for prescription) aren’t dangerous. At worst, it might cause redness or irritation, but only if your skin is sensitive or allergic to the medication.” (Elle, October 2007). Dr. Jacob Levitt, M.D. also reviewed the existing studies on hydroquinone and concluded “topical applications of hydroquinone in standard product concentrations are not carcinogenic to humans” (Journal of the American Academy of Dermatology, 2006), and Dr. David J. Goldberg, a clinical professor of dermatology at the Mount Sinai School of Medicine, agrees, “Over 100 scientific articles confirm it is a safe topical for humans; no independent studies prove the opposite.” (Elle, October 2007).

As for ochronosis, a paradoxical darkening of the skin that is caused by a build-up of phenylalanine or tyrosine, that may be a small, though legitimate, concern for those with darker skin tones (American Journal of Clinical Dermatology, 2001). Dr. Jacob Levitt reviewed 10,000 cases of hydroquinone use over the course of 50 years, and found just 22 cases of ochronosis amongst them, yet all involved patients of color (Journal of the American Academy of Dermatology, 2006). The reasons for ochronosis occurrence in patients with darker skin are not clear. However, increased risk of ochronosis have been linked to using hydroquinone with resorcinol (an agent often used to treat postinflammatory inflammation) and to excess sun exposure while using hydroquinone. As such, always use hydroquinone without resorcinol and with a sunscreen.


2. Licorice Root

Also suppress tyrosinase (melanin production catalyst) production. The substance has anti-inflammatory components hence can lessen sunburn effects

3. 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.

What azelaic acid is used for: Same as hydroquinone – freckles, melasma, and general brown patching. Sometimes azelaic acid is used in place of kojic acid in hydroquinone four-week alternating periods. Azelaic acid works as an acne treatment, and, to a lesser extent, a rosacea treatment.

How azelaic acid works: Take a guess – yep, you got it, azelaic acid also inhibits tyrosinase. According to a double-blind study in the International Journal of Dermatology, over the course of six months, a 20% azelaic acid cream yielded good or excellent results in 65% of patients.

In fact, according to the same study, 20% azelaic acid had “no significant treatment differences” observed when compared to 4% hydroquinone (the prescription level) with regard to overall rating, reduction in lesion size, and pigmentary intensity.

Risks: Side effects, such as allergic sensitization or exogenous ochronosis (associated with hydroquinone) were not observed with 20% azelaic acid

4. 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.

has a similar chemical composition to hydroquinone, but without the potentially irritating side effects.

5. 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

Vitamin C

Holds the number 10 spot among the best whitening ingredients. Vitamin C is a recognized anti-oxidant that decreases skin-aging process. Vitamin C can cut down melanin production in the skin a minimum of 10%. Additionally, Vitamin C contains magnesium phosphate, which is common in most whitening products. Moreover, vitamin C has the power to defend skin from the UV lights.

Vitamin C inhibits the enzyme tyrosinase, which helps produce melanin. By inhibiting tyrosinase, Vitamin C basically helps prevent melanin production so that the dark spots and hyperpigmentation stop dead in their tracks. Vitamin C as been found to lighten the areas affected by hyperpigmentation but leave unaffected areas alone so it knows to focus on those troubled spots.

Vitamin C, or ascorbic acid, is probably one of the best known skin brighteners. It’s a potent antioxidant that’s amazing for dull, congested complexions as it increases cell turnover to boost brightness and overall radiance, and has a lightening effect on all kinds of pigmentation.

What vitamin C is used for: Sunspots, skin dullness, UV-induced erythema and sunburn, increase skin firmness (mild effect), decrease wrinkle depth (mild effect).

How vitamin C works: Vitamin C inhibits tyrosinase, an enzyme in melanin production (Cosmetic Dermatology, Burgess, 2008).

Risks: Risks associated with topical vitamin C use are rare and few side effects have been reported. Probably the biggest risk is not storing vitamin C properly. While most of the ingredients listed on this page are sensitive to light and heat, vitamin C in particular becomes far less ineffective when exposed to air, light, and heat. Another risk of using vitamin C is not selecting the right form of vitamin C. Different forms include L-ascorbic acid, ascorbyl glucoside, magnesium ascorbyl palmitate, and ascorbyl glucosamine. My favorites are L-ascorbic acid (high concentrations are available) and ascorbyl glucoside (found to be absorbed well into the skin).

I choose azelaic acid over ascorbyl glucosamine for hyperpigmentation, as 20% azelaic acid has been shown to be more effective than 5% ascorbyl glucosamine in treating solar lengitines (Dermatology, 2002). For more on the different forms of vitamin C, please see my Spotlight On: Vitamin C post.

6. 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.

Vitamin B3

Vitamin B3 comes to number 9. It generally called niacin amide due to its antioxidant and anti-inflammatory abilities. It restrains melanin production. It gives you utterly lighter skin.

A vitamin B derivative, niacinamide has been known to have positive effects on lightening hyperpigmentation marks on skin by suppressing the transfer of melanin to the outer layer of the skin. It’s different in that while some ingredients inhibit the production of melanin, niacinamide prevents melanintransfer so that color-inducing pigment can’t get to the epidermis, the outermost layer of the skin.

 “No, it works deeper in the skin. It takes a while of using it every day to see results. Like months. I’m not sure of the exact mechanism, but it somehow interferes with the skin creating pigmentation. So as your skin creates new layers, that’s where you see the results.”

7. 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.

Licorice can help reduce the appearance of dark spots and hyperpigmentation because it contains something called “glabridin” which inhibits the enzyme that causes skin to darken. Glabridin helps decrease the production of melanin and will help even out those dark spots.


8. 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.

Vitamin A

Vitamin A is in the eighth spot. Oftentimes it called as retinol. It boosts skin reproduction process and improves vision too. It can give healthy and restored skin along with whiter skin.


A form of vitamin A, retinols work at the cellular level to increase cell turnover, stimulate collagen and elastin production, and fade hyperpigmentation. As already written about, retinols can be very strong so use with caution and under the supervision of your doctor so that you can ease these products into your skin care routine.

These ingredients target discoloration while treating the whole complexion for dullness and uneven skin tone.

9. Undecylenoyl phenylalanine

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).”


10.Mulberry Extract

It’s been shown that the derivatives of the mulberry plant’s root bark inhibit tyrosinase similar to Vitamin C. As mentioned above, tyrosinase helps produce the pigment-causing melanin so inhibiting tyrosinase means inhibiting those annoying dark colored spots.

11. Fruit Extracts

When melanin build up has occurred one way to tackle it is to increase exfoliation so that you can continuously reveal new, fresh skin. Fruit extracts help with very gently exfoliation. Fruit extracts help soften and exfoliate skin which in turns helps to  fade dark spots and remove dead skin cells.

12. Glycolic acid

What glycolic acid is used for: mottled pigmentation, skin dullness, fine lines, surface roughness, freckles, lentigines, and to treat actinic and seborrehic keratosis

How glycolic acid works: As the most commonly used alpha hydroxy acid, glycolic acid advance desquamation and exfoliation of the top layer of the skin. As a result, glycolic acid quickens the rate of cell turnover, decreases small wrinkles and increase fibroblast proliferation of collagen. It does not specifically inhibit melanin production, like hydroquinone or kojic acid.

Risks: A lot of people experience irritation after at-home glycolic acid peels, for two main reasons. First,glycolic acid sensitizes the skin, such that the skin is more likely to be irritated by other ingredients used in conjunction with glycolic acid (Skin Therapy Letter, 1998). Second, glycolic acid has been associated with skin burns and ulcerations, so it is important to speak with a dermatologist first to see which strength is appropriate for you (International Journal of Cosmetic Science, 2007).


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