PAR-2 Blockers To Lighten Skin and Even Skin Tone

diagram showing the composition of the epidermal melanin unit

Protease-activated receptor 2  (PAR-2) is a receptor that can be blocked to lighten skin color. Treating uneven skin tone is challenging because skin lightening ingredients take 8-16 weeks to work. There is no way to lighten skin fast, but there are tips to make skin lightening treatments work better. Adding PAR-2 blockers to your skin-lightening regimen is one way to lighten skin faster. 

What Skincare Products Lighten Skin?

To lighten skin, you should use a combination of various types of skincare products that work together to enhance each other’s efficacy. The cleansers, moisturizers, melasma creams, melasma serums and other dermatologist-recommended treatments for dark spots on the face will work best when your skincare routine is customized with the following considerations:

  • What is the Baumann Skin Type?

  • Lifestyle habits

  • Sunscreen preferences

  • Which fatty acids are in the moisturizer?

  • Use of penetration enhancers such as hyaluronic acid

  • The skincare routine order

  • Use of exfoliators

  • Choice of antioxidants

  • Choice of anti-inflammatory ingredients

  • Choice of safe skin lightening products

There are several categories of skin-lightening ingredients that should be used in skincare routines to lighten skin. To learn more about these skin lightening ingredients and how to lighten dark skin, read this educational material about the various categories of skin lightening skincare products. For now- let's focus our attention of PAR-2 blockers and how they are used in skincare routines to lighten skin color and even skin tone.


Where is Skin Pigment Made?

Skin pigment, known as melanin, is made in the melanocyte cell and packaged in melanosomes for delivery to skin cells. One melanocyte provides melanin to 35 or more skin cells in the epidermis. Melanocytes move around in the epidermis and dermis, but for this discussion, we are going to visualize melanocytes located in the bottom of the epidermis of the skin forming an Epidermal Melanin Unit.  Each melanocyte looks like an octopus and has long arms that extend between skin cells in the epidermis called keratinocytes.


The skin pigment melanin, packaged in melanosomes, travels up the arms of the melanocytes and into the 36 + attached keratinocytes.  This causes the skin color to darken.


What is PAR-2 and Why is it Important in Skin Lightening Products?

At the connection points between the melanocyte and the keratinocytes, there is a receptor that functions like a locked doorway.  This doorway is called the PAR-2 receptor. In order for melanosomes filled with melanin to travel from the melanocyte into the keratinocyte, the PAR-2 doorway must be open. Skin lightening ingredients that block the PAR-2 receptor prevent this movement of the melanosomes, preventing skin pigmentation.1

How To Block The PAR-2 Receptor To Lighten Skin?


Skincare ingredients can be used to block the PAR-2 receptor.  These function as locks on the PAR-2 doorway which prevent movement of melanin into skin cells.  Using a PAR-2 blocking skincare ingredient will prevent skin pigmentation.  PAR-2 blockers do not lighten dark skin fast but prevent further pigmentation so it can take over 30 days to see a difference in skin color with skin lighteners. PAR-2 blocking ingredients should be used in combination with tyrosinase inhibitors which prevent the production of melanin, and exfoliants which help desquamate away old skin cells so they can be replaced with newer less pigmented skin cells.  Of course, sun protection must be used to prevent the formation of new melanin.


What Skincare Ingredients Are PAR-2 Blockers?

The most commonly used PAR-2 blocking cosmeceutical ingredient is niacinamide.  Niacinamide has many important functions such as decreasing inflammation, increasing cell energy to help cellular repair processes, and blocking PAR-2.  Combining niacinamide in a skin lightening skincare routine with tyrosinase inhibitors, the best moisturizer to enhance the function of the tyrosinase inhibitors, a tinted sunscreen and exfoliants such as hydroxyacid cleansers and retinoids is the best way to remove dark spots on the skin.  Other PAR-2 blockers such as activated soy found in Aveeno products are used to lighten skin. New PAR-2 blockers are being developed to be used in skin lightening products.  Stay tuned on social media @SkinTypeSolutions to learn when new PAR-2 blockers come on the market.


1Seiberg, M., Paine, C., Sharlow, E., Eisinger, M., Shapiro, S. S., Andrade-Gordon, P., & Costanzo, M. (2000). Inhibition of melanosome transfer results in skin lightening1. Journal of Investigative Dermatology115(2), 162-167.

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