There is a concept in cosmeceuticals called the Kligman Standard, developed by dermatology legend, Dr. Albert M. Kligman, the man who pioneered the use of tretinoin for acne and anti-ageing, among other things. Dr. Kligman is also called the father of cosmeceuticals, and is credited with coining the term photogaeing, to describe skin damage that results from years of exposure to UV radiation.
Cosmeceuticals encompass products that fall somewhere in between pharmaceuticals and cosmetics. While the term doesn’t have a strict legal definition, the cosmetic industry uses it to describe products with active ingredients that have the potential to affect change in the skin that is more than superficial.
Can it penetrate past the skin’s outermost layer, the stratum corneum, in a concentration high enough that allows for it to deliver its therapeutic benefits?
Does it have a known biochemical mechanism of action?
Do published, peer-reviewed, double-blind, placebo-controlled, statistically significant, clinical trials exist to support claims of its effectiveness?
I’m not one for discrediting safe, potentially beneficial ingredients based on an incomplete understanding of their mechanism of action or on scant research - finding all the answers takes time and resources. However, ingredients that uphold the Kligman Standard have their own place and niacinamide is one of the few that does. Much is known about how niacinamide works and many studies have backed up its effectiveness over the years. It is also a small molecule with a molecular weight of 122.12 g/mol that we know is readily absorbed by the skin when topically applied.
What is niacinamide?
Niacinamide is a physiologically active form of vitamin B3 or niacin, that has been used in dermatology for over four decades for many conditions including acne and rosacea, and more recently, photoaging. Since it is water-soluble, it is not stored in the body and needs to be replenished daily. It plays a central role in cellular respiration, energy production, DNA repair and our cellular response to injury, including inflammation. It is safe for use during pregnancy.
Some history: the pellagra epidemic
Pellagra, which has also often been called the disease of the four D’s, dermatitis, diarrhoea, dementia and death, was first identified among Spanish peasants in 1735. A repulsive disease, it was then given the name of mal de la rosa and while reports of what could have been pellagra in the U.S. go as far back as the 1820s, the first official case was not identified until 1907. Pellagra was especially rampant in the poor Southern states and between 1907 and 1940, around three 3 million Americans contracted the disease and 100,000 of them died.
Pellagra was initially believed to be infectious. Dr. Joseph Golderber, a brilliant clinical epidemiologist, proved however, that pellagra was in fact a dietary disease. Dr. Goldberger passed away before he was able to pin pellagra down to a deficiency in vitamin B3 and this association was discovered around a decade after his death by Conrad Elevjhem. Tryptophan, an amino acid precursor to niacin, has since been added to commercial foods to fortify them and today pellagra is almost unheard of.
This brief history, and the symptoms of patients deficient in B3, demonstrate the variety of processes that the human body needs niacin for. The prevalence of dermatitis in those deficient also demonstrates the importance of niacinamide for skin health.
Niacinamide benefits for skin and its mechanism of action
Niacinamide has recently seen its popularity surge in skin care with products like The Ordinary’s Niacinamide 10% + Zinc 1% Serum dominating the industry. Its fan base is testimony to its effectiveness. Niacinamide’s involvement in sundry cellular mechanisms allows it to affect positive change in the skin on many fronts. Here’s everything that we know niacinamide can do for your skin.
“Studies have shown that niacinamide has the potential to act as an antioxidant, can improve epidermal barrier function, decrease skin hyperpigmentation, reduce fine lines and wrinkles, decrease redness/blotchiness, decrease skin yellowness (sallowness), and improve skin elasticity. The mechanisms by which niacinamide provides this array of skin benefits is not completely understood, but the role of niacinamide as a precursor to the NADP family of coenzymes may play a significant role in all of these improvements.” Source: How Much Do We Really Know About Our Favourite Cosmeceutical Ingredients?
Niacinamide and atopic dermatitis
Given nicotinic acid’s relationship with pellagra, it makes sense to start here. Atopic dermatitis involves three things: a decrease in ceramide production in the skin, an increase in transepidermal water loss and a damaged skin barrier. A B3 deficiency can cause dermatitis and studies have shown that moisturisers formulated with niacinamide can be effective in its treatment.
Dermatitis isn’t the name given to a single condition. The term refers to a group of conditions characterised by itching, inflammation and changes in the layer of the skin called the epidermis. Atopic dermatitis is a common form of dermatitis that occurs in families with a history of asthma and hay fever. It occurs in bouts, but tends to be chronic and is characterised by an itchy, red rash.
Transepidermal water loss refers to the loss of water via evaporation, through the skin.
The primary function of the skin barrier is to keep moisture in and irritants out. When impaired however, it is unable to properly perform this function causing an immune response and inflammation.
In an experiment that incubated cells with niacinamide, niacinamide was shown to increase free fatty acids and cholesterol in the skin, both of which are essential components of the skin barrier and have reduced levels in ageing and atopic dermatitis-affected skin. Niacinamide also down-regulates aquaporin 3, a water channel in the skin that is up-regulated in dermatitis-affected skin resulting in increased transepidermal water loss.
Researchers speculate that niacinamide also improves skin barrier function by stimulating keratinocyte differentiation, something that has been observed both in cell cultures, and in human subjects. This results in a thicker stratum corneum that is better able to hold on to water.
Other studies have also demonstrated the effectiveness of niacinamide for atopic dermatitis. While in its oral form, it was only minimally effective, topical niacinamide resulted in significant improvements probably because targeted therapy was delivered to the affected area. A study that investigated the impact of the application of 2% niacinamide in 12 male patients with dry skin, twice a week for 4 weeks, showed the niacinamide was able to reduce water lost through the skin by 27% and increase free fatty acids and ceramides in the stratum corneum, the topmost layer of the skin, by 67% and 34%, respectively.
Niacinamide and skin pigmentation
Niacinamide can also be effective against pigmentation, and can even help in skin lightening - for those interested.
Most explanations of pigmentation sound like this: skin contains pigment-producing cells called melanocytes. Light and dark skin have about the same number of melanocytes, but in darker skin these produce more pigment and are more highly branched. Melanin protects us from the sun’s harmful UV rays, which is also why our skin tans. When UV hits melanocytes, pigment production is up-regulated as the skin tries to defend itself. Hyperpigmentation occurs when excessive sun exposure over time makes this process go awry, leading to uneven pigmentation with patches of lighter and darker skin.
While this explanation is correct, it is not complete - pigment production in the skin is a complex, multi-stage process. This is important to know since different pigmentation inhibitors work at different points in this process resulting in variable efficacy among compounds. This is also why anti-pigmentation ingredients tend to work better when combined as opposed to when they are used alone. However, niacinamide has been shown to be beneficial for pigmentation and works by inhibiting the transfer of melanosomes - small sacs that contain the melanin pigment produced by our melanocytes - from melanocytes to keratinocytes, the primary cell type in our epidermis.
In a study on 120 subjects with facial tanning and 18 subjects with hyperpigmentation, niacinamide resulted in a 35-68% inhibition of melanosome transfer in skin culture and was able to significantly decrease hyperpigmentation and increase skin lightness. Another double-blind, randomised control trial with 202 subjects, also yielded similar results.
Niacinamide and rosacea
Characterised by redness, pimples, and broken blood vessels, rosacea is a common chronic skin condition that usually only affects the face and eyes. It tends to begin between the ages of 30 and 60 and is more common in fair-skinned individuals and menopausal women.
People with rosacea tend to have more sensitive skin than those who don’t and flare-ups can be triggered by a variety of things from sunlight to spicy food, and even strong emotions. Triggered skin is red, blotchy, coarse and swollen. It also has a compromised skin barrier which makes it susceptible to further irritation, resulting in a vicious cycle.
Niacinamide helps those with rosacea in ways similar to how it helps those with dermatitis: by increasing free fatty acids and cholesterol in the stratum corneum and reducing transepidermal water loss, resulting in more resilient skin that is less susceptible to irritation in the face of environmental triggers.
Niacinamide also helps modulate the overactive immune response typically associated with rosacea. However, concentration matters and high concentrations, like the typical 10%, are likely to irritate the condition further. Those with rosacea should look for gentle products containing less than 5% niacinamide. Studies have shown that niacinamide is effective for those with rosacea even at concentrations as low as 2%. That said however, everyone is different, and it is still always wise to patch test a product before use, especially if your skin is sensitive or problematic.
Niacinamide and skin ageing
Energy is necessary for a cell to be able to perform all of its functions and niacinamide is essential for cellular respiration, the process by which cells convert glucose into energy. Here, niacinamide is involved in the synthesis of coenzymes nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP), which get depleted with age; using niacinamide can help correct their shortfall. NAD and NADP are also coenzymes in more than 40 other cellular biochemical reactions, and have antioxidant properties, giving niacinamide the power to have multiple skin benefits and act as a promising ingredient in the fight against skin ageing.
As we age, other changes also take place in our skin. Less collagen is produced by the fibroblasts in our dermis and ceramide levels in our stratum corneum also get depleted - this is one of the reasons why skin becomes drier with age. Niacinamide can help stimulate the production of both collagen, and ceramides. It also increases the production of the fibrous proteins, keratin, filaggrin and involucrin, within the epidermis helping to restore firmness and suppleness to the skin.
Keratin affects the structure of cells in the epidermis alongside epidermal water-binding capacity. Filaggrin is an antecedent of natural moisturising factor (NMF), i.e. the suite of substances in the skin that help it hold on to water. Involucrin is essential for the formation of cell envelopes that protect the cells in the stratum corneum.
Niacinamide also helps prevent the yellowness that often accompanies skin as it ages. This happens because glycated yellowish-brown proteins begin to accumulate in the skin as we age. Researchers speculate that since NADP and NADPH are antioxidants that can be up-regulated by the application of niacinamide, niacinamide can thus inhibit the oxidation reaction that results in the formation of glycated proteins.
Glycation is an oxidation reaction in which a sugar molecule attaches itself to a protein. This reaction is also called the Maillard reaction.
Several studies have investigated the impact of topical niacinamide on skin ageing. A double-blind, randomised control trial in which 30 Japanese women were asked to apply a formulation with 5% niacinamide for 8 weeks showed that niacinamide resulted in a significant decline in wrinkles and skin roughness. In another study 40 females aged 35-60 applied 5% niacinamide for 12 weeks also saw significant improvement in hyperpigmentation and skin texture.
Niacinamide, enlarged pores and acne
Niacinamide is also often sold as an ingredient for minimising enlarged pores. However, I wasn’t really able to find much, if anything, in the way of scientific studies that support this claim. Most evidence is anecdotal. A proposed mechanism of action however, does potentially exist. There is evidence that niacinamide helps reduce sebum production and, as I already mentioned, it also helps increase the production of collagen, keratin, filaggrin, and involucrin in the skin. Since both high sebum production and the sagging of skin with age can result in enlarged pores, niacinamide can help indirectly by fighting against both of these things. It is however, still important to note that pore size is genetically determined and there isn’t much you can do to change it.
Niacinamide’s sebostatic, anti-inflammatory and anti-pigmentation effects might potentially also be of use for people who suffer from acne, PIE and PIHP and there is some, albeit limited, evidence to support this. However, when it comes to acne, niacinamide is no substitute for first line acne treatments like salicylic acid, which is also my personal favourite. It might, however, offer additional benefit in a regimen that also contains salicylic acid.
Crème B3-B5-E and why we haven’t formulated with 10% niacinamide
We wanted to bring you the benefits of niacinamide in a format that’s easy to use and incorporate into your skincare routine, and is suitable for all skin types, including those with acne, fungal acne and sensitive skin. To this end, we’ve created Crème B3-B5-E, a lightweight moisturiser that combines 4% niacinamide with panthenol or provitamin B5 and vitamin E to provide the skin with hydration, healing and antioxidant support. We’ve formulated with 4% niacinamide since multiple studies have shown that niacinamide is effective above concentrations of 2% but a lot of consumers report experiencing irritation at the high concentrations typically available in the market. This concentration results in a product that is effective, but also better tolerated by a wider variety of people.
How can you incorporate niacinamide into your skin care routine?
Niacinamide can be used everyday, morning and night. Here are some easy skincare routine recommendations that leverage the ingredient for various different skin concerns. If you still have questions after this, as always, feel free to message us on our WhatsApp number: +92-302-222-8349. :)
Acne - Moderate
Morning: Hydrating Gentle Daily Cleanser, Crème B3-B5-E, The Ultimate Sunscreen
Night: Salicylic Acid Cleanser, Crème B3-B5-E
Severe Acne and Fungal Acne
Morning: Hydrating Gentle Daily Cleanser, Crème B3-B5-E, The Ultimate Sunscreen
Night: Hydrating Gentle Daily Cleanser, Salicylic Acid Emulsion (start by using around 3 drops 2-3 times per week and slowly build up; avoid the eye area), Crème B3-B5-E
Skin ageing and hyperpigmentation
Morning: Hydrating Gentle Daily Cleanser, Crème B3-B5-E, The Ultimate Sunscreen
Night: Hydrating Gentle Daily Cleanser, Resurfacing Face Wash (start by using it 2-3 times per week instead of the Hydrating Gentle Daily Cleanser and slowly build up if your skin allows; avoid the eye area), Crème B3-B5-E, Retin-oil Serum (start with the 0.2% and slowly build up to higher concentrations if your skin allows)
Rosacea and atopic dermatitis
Note: These conditions result in heightened skin sensitivity. Patch test each product before introducing it into your routine. Some people with rosacea might also be able to tolerate our Salicylic Acid Cleanser and Retin-oil Serums but I advise against incorporating them into your routine without conducting a patch test first. Some actives, including niacinamide, might work for you but you might not be able to tolerate using them daily. You can still benefit by using them only a few times a week.
Morning: Rinse your face with water, Crème B3-B5-E, The Ultimate Sunscreen
Night: Hydrating Gentle Daily Cleanser, Crème B3-B5-E
How long does it take to see results?
While some people might begin to notice the benefits of niacinamide within 2 weeks, for most they will take 4 weeks or more. Just like it takes time for skin damage to accumulate, it also takes time for your skin to heal from accumulated damage. As always, remember that while you don’t need a lot of products in your skincare routine to see results, every product that you use matters, including what you wash your face with and that SPF is essential for everyone looking to maintain fabulous skin long-term.
I hope this article covered everything you want to know about niacinamide. If you need help with your skin or have any other questions, feel free to reach out for a free skincare consultation or to just drop us a message on WhatsApp: +92-302-222-8349. Until next time!