Cosmeceutical Vitamins: Vitamin B

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Chapter 9 Cosmeceutical Vitamins: Vitamin B

Donald L. Bissett, John E. Oblong

INTRODUCTION

The nutritional value of B vitamins has long been known, and in recent years the utility of topical vitamin B3 (niacinamide) and provitamin B5 (panthenol) is being increasingly recognized. There are several reports of topical niacinamide and panthenol providing therapeutic dermatologic effects. More recently, both of these B vitamins have been utilized in topical cosmetic products to provide beneficial effects for a wide array of more common skin problems such as those associated with aging. In those applications, these B vitamins have been found to be well tolerated by the skin and can thus be used broadly across skin types.

The likely mechanisms involved in these effects have not been completely elucidated. However, since both of these B vitamins are precursors to important cofactors in metabolism, a general mechanism involving this precursor function can be invoked.

This chapter overviews the topical effects and mechanisms of these B vitamins. Since there is a considerable literature on both materials, this review can by necessity only briefly describe the array of published work.

NIACINAMIDE

• Material

Vitamin B3 encompasses a family of structurally similar compounds. The focus here is on niacinamide, also known as nicotinamide and in older literature as vitamin PP (for pellagra preventing). Niacinamide is a water-soluble, stable, low molecular weight substance that readily pene-trates the stratum corneum.

• Topical therapeutic effects

Niacinamide has been used topically in prevention of photodamage, reduction in acne, improvement in bullous pemphigoid, and treatment of rosacea and atopy. The specific mechanisms for these effects have not been defined, although there are considerable effects of niacinamide that may contribute. Additionally, niacinamide is a precursor to NAD(P) and their reduced forms NAD(P)H, cofactors which are important in many cellular metabolic enzyme reactions, so it has potential to impact many tissue functions. Also, since the reduced forms of these cofactors are potent antioxidants, a redox regulation mechanism is a strong possibility.

• Topical cosmeceutical effects

Topical niacinamide is extremely well tolerated by the skin. That mildness and the broad use potential noted above have triggered several recent controlled cosmeceutical clinical studies, which have revealed many beneficial effects of chronic topical niacinamide in aging skin.

BARRIER AND IRRITATION

Topical niacinamide reduced transepidermal water loss (TEWL), indicating improved barrier function. The treated skin was found to be significantly more resistant to damage by barrier-destructive agents such as the surfactant sodium lauryl sulfate (SLS) and trans-retinoic acid. This translates into less irritation and facial red blotchiness (Fig. 9.1).

image

Fig. 9.1 Red blotchiness improvement by topical 5% niacinamide in Caucasian facial skin: (A) baseline; (B) 8 weeks

The mechanism for barrier improvement is likely due to niacinamide-induced increases in skin barrier layer lipids such as ceramides and barrier layer proteins such as keratin, involucrin, and filaggrin. Increases in these primary structural components would be expected to have a significant effect on building the barrier.

HYPERPIGMENTED SPOTS

Chronic topical niacinamide also reduces the appearance of hyperpigmented spots in both Caucasian and Asian facial skin. The mechanism for this was found to involve inhibition of melanosome transfer from the melanocytes to the keratinocytes. With transfer inhibited, the melanocytes stop producing melanin. As anticipated, the melanin reduction effect is reversible with cessation of niacinamide treatment both in culture and clinically.

YELLOWING (SALLOWNESS)

With topical niacinamide, yellowing was significantly prevented (Figs 9.2 and 9.3). The mechanism for this may involve antioxidancy via NAD(P)H, specifically prevention of protein glycation (Maillard reaction), the end products of which are cross-linked yellow-brown proteins (Amedori products) that accumulate in skin. Niacinamide has been reported to have antiglycation properties.

image

Fig. 9.2 Anti-yellowing effect in Chinese facial skin by topical 3.5% niacinamide: (A) baseline; (B) 4 weeks

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Fig. 9.3 Topical 5% niacinamide prevents skin yellowing (‘b’ value analysis from images)

TEXTURE AND SEBUM

A factor in poor texture of older skin is enlarged pore size. Topical niacinamide has been observed to significantly improve texture with chronic usage. Niacinamide reduces sebum production which may lead to reduction in pore size and thus smoother texture.

WRINKLES

A small but significant wrinkle reduction activity is observed after chronic topical niacinamide treatment (Fig. 9.4). There are two mechanisms which have been explored regarding this wrinkle reduction: an increase in dermal collagen production and a decrease in excess upper dermal glycosaminoglycan (GAG) production. While a low level of GAG is required for normal structure and function of the dermal matrix, excess levels are associated with poor visible appearance of skin.

image

Fig. 9.4 Topical 5% niacinamide reduces facial skin wrinkles (total wrinkle line length reduction from quantitative computer image analysis)

PANTHENOL

• Material

Panthenol or provitamin B5 is also known as pantothenol and pantothenyl alcohol. The D optical isomer of panthenol is termed dexpanthenol. Panthenol is a water-soluble, stable, low molecular weight cosmeceutical that readily penetrates the stratum corneum.

• Topical therapeutic effects

Panthenol has been used topically to treat wounds, bruises, scars, pressure and dermal ulcers, thermal burns, postoperative incisions/distention, and dermatoses. The specific mechanisms for these effects are not known. However, dexpanthenol is a precursor to pantothenic acid (vitamin B5). Pantothenic acid is a component of coenzyme A which functions in acyl group transfer during fatty acid biosynthesis and gluconeogenesis. By increasing skin lipid synthesis, an improved barrier would occur, resulting in improved wound healing. In addition, panthenol promotes fibroblast proliferation and epidermal re-epithelialization, effects that promote wound healing. Additionally, panthenol has found utility for skin penetration enhancement.

• Topical cosmeceutical effects

Topical panthenol is extremely well tolerated by the skin, leading to wide topical use of this material and many reported skin benefits. Among those are hydration and the associated improvement in roughness, scaling, and epidermal elasticity; protection against skin irritation and SLS-induced damage; skin soothing; and anti-inflammatory and antipruritic effects.

HYDRATION

Panthenol’s hydration effect likely derives from its hygroscopic properties. Panthenol is an effective moisturizer of stratum corneum and is even more effective when combined with glycerol. In addition, it improves the dryness, roughness, scaling, pruritus, and erythema associated with a wide variety of skin problems such as atopic dermatitis, ichthyosis, psoriasis, and contact dermatitis. It also reduces the cutaneous side effects associated with retinoid therapy. This hydration effect has further led to its use in hair care, promoting improved elasticity, softening, and easier combing.

BARRIER AND IRRITATION

Panthenol protects against irritation via improvement in skin barrier function. Topical pre-treatment with panthenol was observed to increase skin’s resistance to visible irritation upon subsequent exposure to the surfactant SLS (Table 9.1). Since panthenol is the precursor to pantothenic acid, which is a cofactor in barrier layer lipid biosynthesis, this could account for the noted barrier effect.

Table 9.1 Prevention of SLS-induced erythema by topical panthenol

  Erythema score (0–6 scale) for skin treated with:
Time point post SLS treatment SLS Panthenol then SLS
2 days 4.0 2.4
3 days 3.4 1.7
4 days 2.7 1.4

Some consumers are sensitive to specific components (e.g. certain preservatives, fragrances, sunscreen actives, etc.) in cosmetic formulations, leading to induction of negative kinesthetic irritation effects such as burn, sting, itch, and tingling. Topical panthenol incorporated into such formulations can reduce those negative effects (Table 9.2). The mechanism for this may be related to the reported soothing or anti-inflammatory effect of panthenol.

Table 9.2 Reduction in negative kinesthetic effects of formulation containing panthenol

Visible or kinesthetic attribute Reduction in attribute by panthenol (0–6 scale)
Redness − 1.4
Burning − 2.4
Tingling − 5.7
Stinging − 4.9
Itching − 4.9
Warming − 5.7

DISCUSSION

Topical vitamin B3 and provitamin B5 provide a variety of beneficial effects to skin, such as barrier enhancement, moisturization, and aging skin appearance improvement. While there is opportunity to better understand their specific mechanisms, there is currently a solid foundation of mechanistic learning to point the way for future experimentation. In topical use, these water-soluble agents are nonirritating to facial skin, easily formulated, chemically stable, and compatible with other formulation components. They are thus ideal for use in cosmetic products and can be used in combination to increase the overall skin benefits achieved.

FURTHER READING

Biro K, Thaci D, Ochsendorf FR, Kaufmann R, Boehncke WH. Efficacy of dexpanthenol in skin protection against irritation: a double-blind, placebo-controlled study. Contact Dermatitis. 2003;49:80–84.

Bissett DL, Oblong JE, Saud A, Berge CA, Trejo AV, Biedermann KA. Topical niacinamide provides skin aging appearance benefits while enhancing barrier function. Journal of Clinical Dermatology. 2003;32:S9-S18.

Bissett DL, Miyamoto K, Sun P, Li J, Berge CA. Topical niacinamide reduces yellowing, wrinkling, red blotchiness, and hyperpigmented spots in aging facial skin. International Journal of Cosmetic Science. 2004;26:231–238.

CIR. Final report of the safety assessment of niacinamide and niacin. International Journal of Toxicology. 2005;24S:1–31.

Draelos ZD. Niacinamide-containing facial moisturizer improves skin barrier and benefits subjects with rosacea. Cutis. 2005;76:135–141.

Draelos ZD, Ertel KD, Berge CA. Facilitating facial retinization through barrier improvement. Cutis. 2006;78:275–281.

Draelos ZD, Matsubara A, Smiles K. The effect of 2% niacinamide on facial sebum production. Journal of Cosmetic and Laser Therapy. 2006;8:96–101.

Ebner F, Heller A, Rippke F, Tausch I. Topical use of dexpanthenol in skin disorders. American Journal of Clinical Dermatology. 2002;3:427–433.

Fivenson DP. The mechanisms of action of nicotinamide and zinc in inflammatory skin diseases. Cutis. 2006;77S:5–10.

Gehring W. Nicotinic acid/niacinamide and the skin. Journal of Cosmetic Dermatology. 2004;3:88–93.

Gloor M, Senger B, Gehring W. Do dexpanthenol/glycerin combinations achieve better skin hydration than either component alone? Aktuelle Dermatologie. 2002;28:402–405.

Greatens A, Hakozaki T, Koshoffer A, et al. Effective inhibition of melanosome transfer to keratinocytes by lectins and niacinamide is reversible. Experimental Dermatology. 2005;14:498–508.

Hakozaki T, Minwalla L, Zhuang J, et al. The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer. British Journal of Dermatology. 2002;147:22–33.

Kang HT, Lee HI, Hwang ES. Nicotinamide extends replicative lifespan of human cells. Aging Cell. 2006;5:423–436.

Matts PJ, Oblong JE, Bissett DL. A review of the range of effects of niacinamide in human skin. International Federation of the Societies of Cosmetic Chemists Magazine. 2002;5:285–289.

Niren NM. Pharmacologic doses of nicotinamide in the treatment of inflammatory skin conditions: a review. Cutis. 2006;77S:11–16.

Proksch E, Nissen HP. Dexpanthenol enhances skin barrier repair and reduces inflammation after sodium lauryl sulphate-induced irritation. Journal of Dermatological Treatment. 2002;13:173–178.

Reber F, Geffarth R, Kasper M, et al. Graded sensitiveness of the various retinal neuron populations on the glyoxal-mediated formation of advanced glycation end products and ways of protection. Graefes Archive for Clinical and Experimental Ophthalmology. 2003;241:213–225.

Romiti R, Romiti N. Dexpanthenol cream significantly improves mucocutaneous side effects associated with isotretinoin therapy. Pediatric Dermatology. 2002;19:368.

Sauberlich HE. Pantothenic acid. In: Goodhart RS, Shils ME, editors. Modern nutrition in health and disease. Philadelphia: Lea & Febiger; 1980:209–216.

Shindo Y, Witt E, Han D, Epstein W, Packer L. Enzymic and non-enzymic antioxidants in epidermis and dermis of human skin. Journal of Investigative Dermatology. 1994;102:122–124.

Soma Y, Kashima M, Imaizumi A, Takahama H, Kawakami T, Mizoguchi M. Moisturizing effects of topical nicotinamide on atopic dry skin. International Journal of Dermatology. 2005;44:197–202.

Stozkowskaa W, Piekos R. Investigation of some topical formulations containing dexpanthenol. Acta Poloniae Pharmaceutica. 2004;61:433–437.

Thornalley PJ. Glycation in diabetic neuropathy: characteristics, consequences, causes, and therapeutic options. International Review of Neurobiology. 2002;50:37–57.

Wozniacka A, Sysa-Jedrzejowska A, Adamus J, Gebicki J. Topical application of NADH for the treatment of rosacea and contact dermatitis. Clinical and Experimental Dermatology. 2003;28:61–63.

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