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Whitening Ingredients from a Len of science

Keywords: Skin-whitening strategy, Melanin, Pigmentation, Anti-pigmentation, Skin, Cosmetic, Ingredient

The skin-whitening beauty trend is an enormous and lucrative market that has been estimated to reach $24 billion in 2027 [1]. In fact, the business in Asia alone would account for more than 50% of the global market at $12.3 billion [2]. Hence, the market is constantly striving to search for better, safer, and more efficacious ingredients and strategies to tackle "melanogenesis".

With this blog, YOU can grasp the science behind anti-pigmentation and skin-whitening strategies, along with some familiar ingredients (and products too!) that are now on the market. But before that, we are going to take a short view of the melanogenesis process.

Strategy 1: Inhibition of Melanogenic enzymes

First, let’s have an insight into the so-called melanogenesis, a biological process in your body that produces melanins accounting for your skin’s shade and color. There are two major types of melanin in our skin, which was well explained in one of our previous blogs.

In our melanocytes, Tyrosine under the catalysis effect of tyrosinase (“-ase” suffix means enzyme!) will eventually form the highly reactive Dopaquinone. Here, Dopaquinone will undergo a spontaneous transformation to either Eumelanin or Pheomelanin, with the help of enzymes tyrosinase, tyrosinase-related protein 1 (TRP-1), and tyrosinase-related protein 2 (TRP-2). By targeting these enzymes, we can reduce the production of melanin, hence the skin-whitening and anti-spot effect.

(The diagram below is for chemistry and science addicts!)

Figure 1: Enzymatic synthesis of melanin schematic [3,4]

This strategy covers the "true inhibitors" of tyrosinase, such as Hydroquinone, Alpha arbutin, Azelaic acid, and 4-butyl resorcinol, which directly inactivate the enzymes. Hydroquinone is incredibly effective, but it comes with many side effects. The newer ingredient, 4-butyl resorcinol, has been reported to have strong anti-tyrosinase properties with less undesirable effects [5], and it could even be found in non-prescription cosmetics!

The Ordinary Azelaic Acid Suspension 10%, for example, can help you reduce the blemish, even out the dark spots, and improve rosacea with the incredible power of Azelaic acid!

Strategy 2: Inhibition of Melanosome transport

Next, once formed, melanins will be stored inside vesicles called melanosomes, and they are transported from melanocytes into keratinocytes, our skin’s building blocks. The melanocyte has specific structures along dendrites to facilitate the transport of melanosomes. Tackling this process will reduce the number of melanosomes moving upward to the surface, which is one efficacious strategy.

Figure 2: Melanosome transport

Nicotinic acid (A.K.A. Niacinamide - Vitamin B3) has been long reported to have this ability [6]. Niacinamide is the most famous ingredient for this strategy, and it also shows anti-inflammatory function, anti-aging, and ceramide-stimulating properties. All the goodies!

One famous niacinamide product that could be mentioned is La Roche Posay Pure Niacinamide 10.

Strategy 3: Antioxidants & UV Filters

The role of Reactive Oxygen Species (ROS) has been known to worsen skin integrity, pigmentation, evenness, and also wrinkles! By supplying further sources of anti-oxidants and UV filters to diminish the effect of UV lights, your skin can see a drastic improvement in pigmentation, texture, and aging signs. This is the strategy used by UV filters, Vitamin C, Vitamin E, and Coenzyme Q10.

ISDIN Eryfotona Actinica Mineral Sunscreen 50+ is ready to protect your skin with SPF, DNA Repairsome®, and vitamin E for battling against photodamage!

Strategy 4: Acceleration of epidermal turnover and desquamation

For healthy adults, our skin desquamates every 28 days. With exfoliating agents, the skin turnover is sped up, removing the uppermost skin layer containing melanins.

Alpha-hydroxy acid (AHA), Beta-hydroxy acid (BHA), and Polyhydroxy acid (PHA) can speed up the process (we also have a blog mentioning these acids). AHA and BHA work as surface exfoliators to help remove dead skin cells and reveal younger skin layers beneath, but AHA has also been reported to also directly inhibit tyrosinase activity besides its primary effect [7].

Lotion P50 from Biologique Recherche is a predominant icon for this strategy, an indispensable cornerstone for every exfoliating product.

So which ingredients and products to choose?

It is a great question, but there is no simple answer to this. Melanogenesis is a complex biological process; besides the above-mentioned strategies, there are also ingredients that target the MITF transcription factor’s pathways, α-MSH pathway, PKC-β pathway, and so on.

However, if you want to see fast and reliable results, it is advisable to incorporate multiple strategies when it comes to anti-pigmentation and skin whitening. Currently, there are many products that make use of this approach, like Shiseido Haku Melanofocus, Neostrata Illuminating serum, and NIOD RE: Repigment, just to name a few.

Let's get out there, experience a little, learn more about the science, and you can have some fun while figuring out the best products for your skin's condition!


[1] Nikkei Asia (July 1st, 2020). Retrieved on November 27th, 2022, from

[2] Bloomberg (September 22nd, 2021) Retrieved on November 28th, 2022, from

[3] Gillbro, J. M., & Olsson, M. J. (2011). The melanogenesis and mechanisms of skin-lightening agents--existing and new approaches. International journal of cosmetic science, 33(3), 210–221.

[4] D'Mello, S. A., Finlay, G. J., Baguley, B. C., & Askarian-Amiri, M. E. (2016). Signaling Pathways in Melanogenesis. International journal of molecular sciences, 17(7), 1144.

[5] Kolbe, L., Mann, T., Gerwat, W., Batzer, J., Ahlheit, S., Scherner, C., Wenck, H., & Stäb, F. (2013). 4-n-butylresorcinol, a highly effective tyrosinase inhibitor for the topical treatment of hyperpigmentation. Journal of the European Academy of Dermatology and Venereology: JEADV, 27 Suppl 1, 19–23.

[6] Hakozaki, T., Minwalla, L., Zhuang, J., Chhoa, M., Matsubara, A., Miyamoto, K., Greatens, A., Hillebrand, G. G., Bissett, D. L., & Boissy, R. E. (2002). The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer. The British journal of dermatology, 147(1), 20–31.

[7] Usuki, A., Ohashi, A., Sato, H., Ochiai, Y., Ichihashi, M., & Funasaka, Y. (2003). The inhibitory effect of glycolic acid and lactic acid on melanin synthesis in melanoma cells. Experimental dermatology, 12 Suppl 2, 43–50.

* Figures were made with BioRender and Chemdraw


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