One of the most popular articles I have written for UL Prospector® in the last eight years featured the use of niacinamide as a cosmetic active. Since then, its popularity has substantially grown to the point that it is commonly found in many premium skincare treatment products. The reasons for its popularity are simple; it’s effective, safe, stable, easy to use and is reasonably priced. Niacinamides’ skincare benefits have been extensively documented in numerous peer-reviewed scientific publications, and it is probably one of the most dermatologist-recommended cosmetic active. It has been used in dermatology for more than 45 years to treat a diverse range of conditions, including acne, rosacea, atopic dermatitis, psoriasis, seborrheic dermatitis, hyperpigmentation, autoimmune bullous dermatoses, and the treatment/prevention of photoaging and photo immunosuppression.
Niacin is a water-soluble B vitamin that is made and used by your body to turn food into energy. It helps keep your nervous system, digestive system, and skin healthy. Niacinamide is a biologically active form of niacin or vitamin B3 found widely in many plants and animals. Tryptophan is converted to Niacin in the body, and approximately 2/3 of your body’s niacinamide is tryptophan derived.
Skin Benefits
An unusual property of niacinamide is its ability to act as a synergizer to improve the performance of many different types of skin actives.
- Improves skin barrier function
- Topical niacinamide increases free fatty acid and ceramide levels in the skin (1).
- Niacinamide increases barrier layer proteins such as involucrin, filaggrin and keratin. Filaggrin is critical in the formation of natural skin moisturizing factors (2).
- Niacinamide reduces skin irritation induced by sodium lauryl sulfate and dimethyl sulfoxide (3).
- Moisturizes skin
- 2% topical niacinamide shown to be more effective than petrolatum for reducing skin water loss and increasing its hydration levels (4).
- Two niacinamide/glycerin moisturizers demonstrated an excellent improvement in dry skin compared to no treatment and several other commercial moisturizers (5).
- Niacinamide improves the appearance of aged skin.
- A 12-week clinical study using a 5% niacinamide cream demonstrated a 21% improvement in fine lines along with a 14% skin tone clarity and 15% radiance improvement (6).
- A 4% niacinamide cream showed a marked to moderate improvement in fine lines in 64% of the subjects with a significant difference as compared with the control site (P < 0.001). (7).
- Niacinamide lightens skin
- A 5% niacinamide provided significant improvements versus control for reducing fine lines/wrinkles, hyperpigmentation spots, texture and red blotchiness. In addition, skin yellowing (sallowness) versus control was significantly improved (8).
- Good to excellent skin lightening activity was observed using a 4% niacinamide cream in 44% of patients, compared to 55% using a 4% hydroquinone cream (9).
- A 5% niacinamide/2% n acetyl glucosamine and SPF 15 formulation regimen was significantly more effective than the vehicle control formulation regimen in reducing the detectable area of facial spots and the appearance of pigmentation (10).
- Niacinamide has antiacne efficacy
- 4% niacinamide improved overall acne in 80% of volunteers after 8 weeks versus 68% of volunteers after eight weeks using 1% clindamycin (11, 12).
- Niacinamide reduces sebum and enlarged skin pores
- Using a 2% niacinamide cream for four weeks significantly decreased sebum and enlarged pores in Caucasian women vs. baseline, and vs. the vehicle control moisturizer (13).
- Niacinamide has antioxidant activity
- Niacinamide has better antioxidant activity against singlet oxygen (the most destructive type of free radical) than ascorbic acid or Tocopherol (14).
- Niacinamide increases the antioxidant capacity of skin after topical application by increasing the reduced forms of NADPH, which have potent antioxidant properties (15).
- Niacinamide can improve the microbiome and increase the production of antimicrobial peptides in skin (16, 17, 19).
- Niacinamide inhibits skin irritation
- Niacinamide reduces substance P Induced edema (18).
Commercially Available Vitamin B3 Derivatives
- Niacinamide (water-soluble)
- Inositol Nicotinate (water-soluble)
- Niacinamide Dinucleotide (water-soluble)
- Nicotinamide Riboside (water-soluble)
- Tocopheryl Nicotinate (oil-soluble)
- Menthyl Nicotinate (oil-soluble)
- Myristyl Nicotinate (oil-soluble)
Formulation Tips
- Only ~11% of niacinamide applied topically penetrates. Phospholipids like Lysofix Liquid (Glycerin and Glycine Soja (Soybean) Extract-Kemin), Soy Lecithin and Hydrogenated Lecithin can be useful to improve Niacinamide bioavailability (20, 21).
- Avoid using fatty acids in formulations. Niacinamide and the carboxylic acid/salts can form mixed crystals or a complex together.
- Niacinamide may be useful to reduce retinol-induced skin irritation.
References
- Tanno O, Ota Y, Kitamura N, et al. Nicotinamide increases biosynthesis of Ceramides as well as other stratum corneum lipids to improve the epidermal permeability barrier. Br J Dermatol. 2000;143:524-531.
- Bissett DL (2002) Topical Niacinamide and barrier enhancement. Cutis 70S:8–12.
- Bissett DL (2002) Topical Niacinamide and barrier enhancement. Cutis 70S:8–12.
- International Journal of Dermatology, March 2005, pages 197-202.
- Christman JC, et. al. Two randomized, controlled, comparative studies of the stratum corneum integrity benefits of two cosmetic Niacinamide/glycerin body moisturizers vs. conventional body moisturizers. J Drugs Dermatol. (2012).
- Bissett DL, Oblong JE, Saud A, et al. Topical Niacinamide provides skin aging appearance benefits while enhancing barrier function. In: Elsner P, Maibach HI. (Eds,) Cosmeceuticals and Active Cosmetics, 2nd edn. New York: Taylor and Francis Group, 2005,421-440.
- Kawada A, Konishi N, Oiso N, Kawara S, Date A., Evaluation of anti-wrinkle effects of a novel cosmetic containing niacinamide. Int J Cosmet Sci. 2004 Oct;26(5):231-8.
- Bissett DL, et. al. Topical niacinamide reduces yellowing, wrinkling, red blotchiness, and hyperpigmented spots in aging facial skin. Int J Cosmet Sci. (2004).
- Moncada B. A Double-Blind, Randomized Clinical Trial of Niacinamide 4% versus Hydroquinone 4% in the Treatment of Melasma. Dermatol Res Pract. 2011:379173.
- Kimball AB, et. al. Reduction in the appearance of facial hyperpigmentation after use of moisturizers with a combination of topical niacinamide and N-acetyl glucosamine: results of a randomized, double-blind, vehicle-controlled trial. Br J Dermatol. (2010).
- Shalita AR, Smith JG, Parish LC, Sofman MS, Chalker DK, Topical nicotinamide compared with clindamycin gel in the treatment of inflammatory acne vulgaris. Int J Dermatol. 1995 Jun;34(6):434-7.
- Griffiths CEM. Nicotinamide 4% gel for the treatment of inflammatory acne vulgaris. J Dermatol Treat. 1996;6(Suppl 1):8–10.
- Bissett DL, Topical niacinamide and barrier enhancement. Cutis 70S:8–12 (2002).
- Yasuhiro Nishida, Eiji Yamashita and Wataru Miki, Quenching Activities of Common Hydrophilic and Lipophilic Antioxidants against Singlet Oxygen Using Chemiluminescence Detection System. Carotenoid Science, Vol.II, 2007, 16-20.
- Wozniacka A, Sysa-Jedrzejowska A, Adamus J, Gebicki J. Topical application of NADH for the treatment of rosacea and contact dermatitis. Clin Exp Dermatol. 2003;28:61–63.
- EP2742942, Unilever, 6/18/14.
- Niacinamide leave-on formulation provides long-lasting protection against bacteria in-vivo, Ms, Mruthyunjaya1, Shilpa Vora1, Jyoti, AAD 2018 Poster.
- L’Oréal US 8858968, 10/14/14.
- Response of the skin microbiome to emollient treatment in patients with atopic dermatitis-L’Oreal (AAD Poster 2016).
- Franz TJ. Percutaneous absorption: on the relevance of in vitro data. J Invest Dermatol. (1975). Feldmann RJ, Maibach HI. Absorption of some organic compounds through the skin in man. J Invest Dermatol. (1970).
- In vitro Percutaneous Absorption of Niacinamide and Phytosterols and in vivo Evaluation of their Effect on Skin Barrier Recover, Alessia Offerta1, Francesco Bonina1, Franco Gasparri2, Andrea Zanardi2, Lucia Micicchè1 and Carmelo Puglia, Current Drug Delivery, 2016, 13, 111-120.
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Dear George, what an interesting article and thank you for summarizing in such a detailed and scientific way all niacinamide’s benefits.
I’m currently working with niacinamide, but I was wondering if there is a natural derived niacinamide since all the ones that I know of are synthetic.
Thank you
Nice & useful information! Thanks!!!
Dear Carolina:
There is no natural sourced Niacinamide available.
Thanks for reading!
George
Another great article by you. Very informative. Good Job!
Thanks.
Dear George,
Could the niacinamid be introduced in water phase A in a hot process formulation (65-70°c), or should it be rather added in the cool down phase?
I read that niacinamid was quite thermoresistant, but also that its conversion to niacin was increased if heated and in low pH conditions.. what do you think about that? It is safe to use it in a formulation with 4.5-5 pH range?
Thank you very much for your answer..
Sinverely
Catherine
Hi, Catherine. Per George Deckner, what you’ve mentioned in your comment should be ok. Thank you!