6)cosmeceutical vitamins 2011 - american academy … vitamin e • doses of 50 iu- 1000 iu...

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©Sharon McQuillan, MD. All rights reserved. 1 Cosmesceutical Vitamins Patrick Bitter, MD Cosmeceutical Actives: Vitamins Patrick Bitter, MD The following potential conflict of interest relationships are germane to my presentation. Speaker’s Bureau: Sciton Laser Cosmeceutical Vitamins Scientific evidence shows that certain vitamins are useful in skin care Prevention of photoaging and chronological skin aging Topical and systemic treatment of photoaging and chronological skin aging Management of acne vulgaris

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Page 1: 6)Cosmeceutical Vitamins 2011 - American Academy … vitamin E • Doses of 50 IU- 1000 IU α-tocopherol per day tolerated in humans with little to no side effects • Clinical studies

©Sharon McQuillan, MD. All rights reserved. 1

Cosmesceutical Vitamins

Patrick Bitter, MD

Cosmeceutical Actives: Vitamins Patrick Bitter, MD

The following potential conflict of interest relationships are

germane to my presentation.

Speaker’s Bureau: Sciton Laser

Cosmeceutical Vitamins

•  Scientific evidence shows that certain vitamins are useful in skin care –  Prevention of photoaging and chronological skin

aging –  Topical and systemic treatment of photoaging

and chronological skin aging –  Management of acne vulgaris

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©Sharon McQuillan, MD. All rights reserved. 2

Vitamins & Their Derivatives in Skin Care

•  Vitamin A –  normalize keratinization –  downregulate sebum production in acne –  treat photodamage, striae, and cellulite

•  Vitamin D (and analogs) –  Downregulate cutaneous immune system –  Downregulate epithelial proliferation and

promote differentiation Shapiro S, Saliou C. Role of vitamins in skin care. Nutrition

2001;17:839-844.

Vitamins and Their Derivatives in Skin Care

•  Vitamin C –  Antioxidant –  Regulates collagen synthesis (transcription and

posttranslation) –  Photoprotection (in combination with vitamin E)

•  Vitamin E –  Membrane antioxidant –  Protects against oxidative damage –  Photoprotection (in combination with vitamin C)

Vitamin A

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©Sharon McQuillan, MD. All rights reserved. 3

Vitamin A

•  Consist of natural and synthetic derivatives of Vitamin A

•  Prescription retinoids –  Retinoic acid –  Synthetic naphthalene derivatives

•  Adapalene •  Tazarotene •  Bexarotene

Vitamin A

•  Topical cosmeceutical retinoids –  Retinyl esters –  Retinol –  Retinaldehyde –  Oxoretinoids

Retinoid Metabolism in Skin

•  Retinol is oxidized into retinaldehyde

•  Retinaldehyde is oxidized into retinoic acid (biologically active form or vitamin A)

Draelos ZD, ed. 2005. Procedures in Cosmetic Dermatology: Cosmeceuticals. Philadelphia, Elsever

Saunders.

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Retinoid Penetration •  Retinoids are lipophilic molecules that penetrate

epidermis •  Penetration of retinol and retinaldehyde

investigated in vivo by measuring levels of skin enzyme cytochrome P-450-dependent RA 4-hydroxylase (CP450-RAH) with showing significant penetration and metabolism of retinol and retinaldehyde

•  Threshold concentration for adequate penetration and metabolism of retinaldehyde and retinol into retinoic acid is 0.025%

Retinoid Metabolism Study

•  Metabolism of retinol, retinaldehyde, and retinoic acid was studied using in-vitro human skin and dermal fibroblasts

•  Radiolabeled retinol and retinaldehyde applied to skin biopsies or to cultured media of fibroblasts

•  Analyses demonstrated gradient distribution of retinoids within skin and metabolism of retinol and retinaldehyde to retinoic acid

Baily J, et al. In vitro metabolism by human skin and fibroblasts of retinol, retinal, and retinoic acid. Exp Dermatol

1998;7:27-34.

Biologic Properties of Retinoids

•  Antioxidant activity via free radical quenching

•  Increased fibroblast proliferation •  Modulation of cellular differentiation and

proliferation •  Increased collagen and hyaluronate •  Decreased metalloproteinase-mediated

extracellular degradation Song O et al. Proposed mechanism of action for retinoid derivation in the treatment of skin aging. J

Cosmet Dermatol.2005;4:237-244.

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Retinoid Mechanism of Action

•  Fine lines and wrinkles •  Hyperpigmentation •  Skin roughness

Retinoids: Fine Lines & Wrinkles

•  Retinoic acid reduces fine lines and wrinkles by increasing capacity of epidermis to hold water through stimulation of glycosaminoglycan (GAG) synthesis

•  Also stimulates collagen synthesis by increasing transforming growth factor β (TGF-β) and procollagen

•  May retard or prevent further dermal matrix degradation by inhibiting enzymes that break down collagen and prevent oxidative stress

Retinoids: Hyperpigmentation

•  Retinoic acid thought to reduce pigmentation by enhancing epidermal cell turnover

•  Enhancing epidermal cell turnover decreases contact time between keratinocytes and melanocytes and promoted rapid loss of pigment via epidermopoiesis

Sorg O et al. Retinoids in cosmeceuticals. Dermatol Ther 2006;19:289-296.

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Retinoids: Skin Roughness

•  Reduces skin roughness by modulating expression of genes involved in cellular differentiation and proliferation, promoting epidermal cell turnover

•  Believed to be mediated via binding to retinoic acid receptors (RAR) and subsequent binding of these complexes to specific genes affecting gene transcription

Retinoids

•  Negative effects of topical retinoids –  Skin irritation –  Tetragenic effects

•  Retinoic acid precursors used widely in skin care industry to minimize these effects and still effectively treat photodamaged skin

Retinol •  Naturally occurring form of

Vitamin A •  Precursor to retinoic acid •  Derived by hydrolysis of

betacarotene •  Used for topical treatment

of photodamage and acne •  Activity substantially

increased when applied under occlusion

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©Sharon McQuillan, MD. All rights reserved. 7

Creidi P, Humbert P. Clinical use of topical retinaldehyde on photoaged skin. Dermatology 1999; 199(Suppl 1):49-52.

Retinaldehyde

•  Formed by oxidation of alcohol group of retinol

•  Studies show retinaldehyde can successfully treat rosacea with better patient toleration than retinoic acid

Green C et al. A clinicopathological study of the effects of topical retinyl propionate cream in skin photoaging. Clinics in Experimental Dermatology

1998; 23:162-167.

Retinyl Esters: Retinyl Propionate and Retinyl Palmitate

•  Store vitamin A in lipids

•  Retinyl propionate shown to elicit retinoid effects in treating photodamage with less irritation

•  Studies suggest retinyl palmitate has weak activity

Draelos ZD, ed. 2005. Procedures in Cosmetic Dermatology: Cosmeceuticals. Philadelphia, Elsever Saunders.

Retinyl Propionate Results

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©Sharon McQuillan, MD. All rights reserved. 8

Tretinoin

•  Trans-retinoic acid •  Used in treatment of

acne and photoaging

Kligman AM et al. Topical Tretinoin for photoaged skin. J Am Acad Dermatol 1986; 15:836-859.

Tretinoin

•  Role of tretinoin first described by Kligman –  Demonstrated significant effects on

photodamaged skin –  Reversal of epidermal atrophy, dysplasia and

atypia –  Eradication of microscopic actinic keratoses –  Uniform dispersing of melanin –  New collagen formation

Tretinoin

•  Formal clinical trials have proven tretinoin reverses photoaging at a dermal and epidermal level

•  Epidermal effects –  Epidermal thinning –  Reduction in corneocyte adhesion –  Decreased melanin production –  Increased Langerhans cell production

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Tretinoin

•  Dermal effects –  Increased collagen production –  Increased angiogenesis –  Decreased collagenase –  Decreased glycosoaminoglycans Weiss JS et al. Topical tretinoin improves photoaged skin. JAMA 1988;

259:527-532. Leyden JJ, et al. Treatment of photodamaged facial skin with topical

tretinoin. J Acad Dermatol 1990; 122:91-98.

Topical Retinol Study

•  Comparative, investigator-blinded, split-face study

•  Hydroquinone 4%/retinol 0.3% compared with tretinoin 0.05% among 41 women with mild to moderate photodamage

•  Both preparations associated with superior improvement in pigment parameters

Del Rosso JQ. Feature: topical retinoid therapy. Skin

Aging.2002;10:50-62.

Topical Retinol Study •  Randomized, double-blind, vehicle-controlled trial

in elderly patients with naturally aged skin •  Mean age=87 years •  Retinol 0.4% lotion or vehicle control applied to

patients’ forearm 3 times/week for 24 weeks •  Retinol treated skin associated with significant

improvement in fine wrinkle scores compared to baseline

•  Topical retinol associated with increase in GAG expression and procollagen I

Kafi R et al. Improvement of naturally aged skin with vitamin A (retinol). Arch Dermatol. 2007;143:606-12.

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Topical Retinoic Studies

•  0.05% retinaldehyde vs. 0.05% retinoic acid vs. vehicle in 125 patients over 18 weeks in nondouble-blind and non randomized study

•  Retinaldehyde can also produce significant clinical improvement in fine lines and deep wrinkles

Creidi P et al. Prilometric evaluation of photodamage after topical retinaldehyde and retinoic acid treatment. J Am Acad

Dermatol 1998;39:960-965.

Topical Retinoid Studies

•  0.4% retinol vs. vehicle in randomized, double-blind, vehicle-controlled, left and right arm comparison study in 36 elderly patients 3 times per week for 24 weeks

•  Clinically, retinol improved fine wrinkling with significance (p<0.001)

•  Histologically, biopsies showed retinol significantly increased GAG expression and procollagen

Sorg O et al. Retinoids in cosmeceuticals. Dermatol Ther 2006;19:289-296.

Vitamin E

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Vitamin E

•  Functions as major lipophilic antioxidant in plasma, membranes, tissues

•  Refers to eight molecules –  Four tocopherols –  Four tocotriends

•  α-tocopherol most abundant form in body

Vitamin E

•  Most important lipid-soluble antioxidant found in membranes

•  Two basic forms –  Tocopherols –  Tocotrienols

Vitamin E

•  Scavenges lipid peroxyl radicals •  Predominant physiologic antioxidants of skin

barrier •  May enhance photoprotective properties of

sunscreen •  Clinical studies show that chronic skin conditions

such as wrinkling and skin tumor incidence due to prolonged UV exposure are diminished by topical vitamin E

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Vitamin E

•  Topically applied vitamins C, E, and ferulic acid act synergistically to compound antioxidant and photoprotective properties

•  Vitamin C regenerates active form of vitamin E

•  Ferulic acid stabilizes vitamins C and E

Pinnell SR. Cutaneous photodamage, oxidative stress, an topical antioxidant protection. J Am Acad Dermatol

2003;48:1-19.

Vitamin E •  Many topical studies demonstrate benefits of

vitamin E applied before UV exposure (diminished erythema, edema, skin wrinkling, skin turnover)

Roshchupkin DI et al. Inhibition of ultraviolet light-induced erythema by antioxidants. Arch Dermatol Res 1979; 266: 91-94.

Lopez-Torres M et al. Topical application of α-tocopherol modulates the antioxidant network and diminishes ultraviolet-induced oxidative damage in murine skin. Br J Dermatol 1998; 138: 207-215.

Bissett DL et al. Protective effect of a topically applied antioxidant plus an anti-inflammatory agent against ultraviolet induced chronic skin damage in the hairless mouse. J Soc Csmet Chem 1992; 43: 85-92.

Vitamin E and Scars

•  Vitamin E used historically to minimize scar appearance

•  12 week double-blinded study comparing vitamin E to control

•  Vitamin E did not improve cosmetic outcome of post surgical scars

•  Caused contact dermatitis in 33% of treated subjects

Baumann LS, Spencer J. The effect of topical vitamin E on the cosmetic appearance of scars. Dermatol Surg

1999;5:311-315.

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Vitamin E

•  Most frequently used cosmeceutical ingredients •  Lack of published data on dose-response studies

regarding vitamin E •  Doses of 50 IU- 1000 IU α-tocopherol per day

tolerated in humans with little to no side effects •  Clinical studies suggest that orally administered

vitamin E improves facial hyperpigmentation

Funasaka Y et al. The depigmenting effect of alpha-tocopherol ferulate on human melanoma cells. Br J Dermatol

1999;141:20-29.

Vitamin C

Vitamin C

•  Water soluble, acidic, essential for life

•  Essential for hydroxylation of precollagen, lysine

•  Regenerates vitamin E and quenches free radicals

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Vitamin C (Ascorbic Acid)

•  Effective treatment for inflammatory dermatoses

•  Anti-inflammatory and antioxidant properties •  Promotion of collagen synthesis •  Inhibition of collagen degradation •  Reduction of hyperpigmentation •  Acts to regenerate vitamin E from

tocopheroxyl radical

Therapeutic Used for Vitamin C

•  Photodamage •  Photoaging •  Hyperpigmentation •  Erythema

Vitamin C

•  Normalizes histological changes of photodamage

•  Skin levels depleted after UV exposure •  Three forms of vitamin C found in

cosmeceuticals –  L-ascorbic acid –  Ascorbyl-6-palmitate –  Magnesium ascorbyl phosphate (most stable)

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Vitamin C Clinical Study

•  Topical L-ascorbic acid shown to protect skin from UVB induced erythema and sunburn cell formation

Darr D et al. 1992. Topical vitamin C protects porcine skin from ultraviolet radiation-induced damage. British Journal of Dermatology. 127:247-253.

Vitamin C Clinical Study •  3 month, double blind vehicle •  N=19 •  Split-face study 0.5 mL Cellex-C high potency

serum 10% •  Photographs, periorbital optical profilometry, and

patient self assessment •  73.9% improvement in periorbital wrinkles •  57.9% improvement in photographic assessment

over control •  Patients reported 84.2% improvement over control Traikovich SS. Arch Otalaryngol Head Neck surg 1999: 125;1091.

Beneficial Effects of Topical Vitamin C in Photodamaged & Photoaged Skin

•  Randomized, double-blind, placebo-controlled trial •  Topical vitamin C 5% cream used over 6 months vs.

placebo •  Skin treated with vitamin C cream associated with

significant improvement in physician and patient assessments

•  Significant increase in skin density •  Decrease in skin wrinkles •  Histological evidence of elastic repair

Humbert PG et al. Topical ascorbic acid on photoaged skin. Exp Dermatol.2003;12:237-244.

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Vitamin C & E Synergistic Effects Study

•  L-ascorbic acid 15% and α-tocopherol 1% used either alone or in combination vs. vehicle control

•  Individual ingredients resulted 2-fold increase antioxidant protection

•  Combination produced 4-fold increase in antioxidant protection

Lin FH et al. Ferulic acid stabilizes a solution of vitamins C & E and doubles its photoprotection of the

skin. J Invest Dermatol. 2005;125: 826-832.

Draelos ZD, ed. 2005. Procedures in Cosmetic Dermatology: Cosmeceuticals. Philadelphia, Elsever Saunders.

Vitamin C Results

Vitamin C Studies

•  Double-blind, split-face trial •  Topical solution containing 10% L-ascorbic

acid and 7% tetrahexyodeyl ascorbate compared with control

•  After 12 weeks, wrinkling and photodamage significantly reduced on cheeks, forehead, and perioral region on treated side of face.

Fitzpatric RE, Rostan EF. Double-blind, half-face study comparing topical vitamin C and vehicle for rejuvenation of

photodamage. Dermatol Surg 2002;28:231-236.

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Vitamin C Study

•  In study of postmenopausal women, vitamin C increased pro-collagen mRNA and associated enzymes to bolster collagen synthesis

Nusgens BV et al. Topically applied vitamin C enhances mRNA level of collagens I and III, their processing enzymes and tissue inhibitor or matrix metalloproteinase I in human

dermis. J Invest Dermatol 2001;116:853-9.

Vitamin B3: Niacinamide

Niacinamide

•  Precursor of cofactors niacinamide adenosine dinucleotide (NAD) and niacinamide adenosine dinucleotide phosphate (NADP)

•  Cofactors and reduced forms (NADH and NADPH) serve as reduction-oxidation coenzymes in more than 40 cellular biochemical reactions

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Niacinamide Penetration

•  Studies demonstrate significant penetration into human skin

•  Increased levels of NAD have been used as evidence of percutaneous penetration

Vitamin B3 - Niacinamide

•  Niacinamide increases epidermal turnover, improves barrier function, decreases photoaging, reduces sebum production

•  Does not irritate skin

Niacinamide: Mechanisms of Action

•  Antioxidant capacity •  Epidermal barrier function •  Erythema and blotchiness •  Skin yellowing •  Fine lines and wrinkles •  Hyperpigmentation

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Antioxidant Capacity

•  Increases antioxidant capacity of skin after topical application by increasing the reduced form NADPH, which has potential antioxidant properties

Epidermal Barrier Function & Niacinamide

•  Evidenced by reduced TEWL (transepidermal water loss) and increase in skin’s resistance to potential harmful topical agents

•  Proposed mechanisms of action –  Increased synthesis of ceramides via

upregulation of serine palmitoyl transferase, the rate limiting enzyme in sphingolipid synthesis

–  Stimulate keratinocyte differentiation by influencing keratin K1, which results in epidermal turnover

Skin Yellowing & Niacinamide

•  Yellowing of skin that occurs with aging may be result of glycation of proteins in skin (Maillard reaction)

•  Maillard reaction – spontaneous oxidative reaction between protein and sugar resulting in cross-linked proteins that are yellow-brown in color (Amadori products) and accumulate in skin matrix components

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Skin Yellowing and Niacinamide

•  NADH and NADPH are antioxidants and their levels are influenced by niacinamide, a possible effect of topical niacinamide is inhibition of oxidative processes, leading to the decrease of skin yellowing.

Niacinamide: Fine Lines & Wrinkles

•  Multiple mechanisms may be involved in ability of niacinamide to reduce appearance of fine lines and wrinkles

•  May have ability to increase dermal collagen and protein production

•  As precursor of NAD/NADP, niacinamide stimulates collagen synthesis and keratin, fillagrin, and involucrin

•  Ability to reduce GAGs

Niacinamide and Erythema, Blotchiness

•  Mechanism which improves redness/blotchiness may be related to improved skin barrier function

•  Increasing barrier function may result in less irritation when skin encounters environmental insults resulting in less redness

•  Theory has not been substantiated

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Niacinamide and Hyperpigmentation

•  Reduces melanosome transfer from melanocytes to surrounding keratinocytes

•  5% niacinamide moisturizer provided 35-68% inhibition of melanosome transfer from melanocytes to keratinocytes

Hakozaki T et al. The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome

transfer. Br J Dermatol 2002;305:26-268.

Potential Clinical Used of Niacinamide

•  Dry skin •  Acne •  Photoaging •  Blistering disorders •  Pigment disorders •  Wound healing

Niacinamide Clinical Studies

•  Randomized, double-blind studies of Japanese and white patients

•  Topical niacinamide 2% produced significant effects on sebum excretion and sebum levels in Japanese patients

•  Significant reduction in facial shine, oiliness, and overall skin appearance in white patients

Draelos ZD et al. The effect of 2% niacinamide on facial sebum production. J Cosmet Laser Ther.

2006;8:96-101.

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Niacinamide Clinical Studies

•  5% topical nicotinic acid derivative applied for 12 weeks vs. placebo in patients with photodamage

•  25% increase in skin NAD levels •  70% increase in epidermal thickness

Jacobsen EL et al. A topical lipophilic niacin derivative increases NAD,epidermal differentiation

and barrier function in photodamaged skin. Exp Dermatol. 2007;16:490-99.

Draelos ZD, ed. 2005. Procedures in Cosmetic Dermatology: Cosmeceuticals. Philadelphia, Elsever Saunders.

Niacinamide Results

Niacinamide Studies

•  3.5% niacinamide cream was compared with placebo for 4 weeks and demonstrated 14.8% reduction in skin roughness (p = 0.05)

Tano O et al. Nicotinamide increases biosynthesis of ceramides as well as other stratum corneum lipids to improve

epidermal permeability. Br J Dermatol 2000;143:524-531.

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Niacinamide Studies

•  Randomized, double-blind, split-face, placebo-controlled clinical trial

•  50 white females applied 5% niacinamide and vehicle twice daily for 12 weeks

•  Results showed significant improvement in fine lines, wrinkles, hyperpigmentation, redness, yellowing, skin elasticity (p>0.05)

Bissett Dl et al. Topical niacinamide reduces yellowing, wrinkling, red blotchiness, and hyperpigmented spots in aging

facial skin. Int J Comset Sci 2004;26:231-238.

Vitamin B5 - Panthenol

Vitamin B5 - Panthenol

•  Promotes fibroblast synthesis, epidermal re-epithelialization, increased skin lipid synthesis

•  Skin penetration enhancement

•  Used topically to treat wounds, bruises, scars, pressure and dermal ulcers, dermatoses

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Panthenol

•  Addition of panthenol to topical formulations should reduce effects of: –  Redness –  Burning –  Tingling –  Stinging –  Itching

Stozkowskaa W et al. Investigation of some topical formulations containing dexpanthenol. Acta Poloniae

Pharmaceutica 61:433-437.

Effects of Panthenol

•  Hydration: moisturizes stratum corneum, improves elasticity

•  Barrier functions: protects against irritation by improving and repairing skin barrier functions

Panthenol Studies

•  Topical pretreatment with panthenol observed to increase skin’s resistance to visible irritation upon exposure to sodium lauryl sulfate (SLS)

•  Topical panthenol can be incorporated into skin care formulations to reduce negative effects of product irritation

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Prevention of SLS-induced Erythema by Topical Panthenol (0-6 scale)

Time post SLS treatment Erythema score SLS Erythema score panthenol

2 days 4.0 2.4

3 days 3.4 1.7

4 days 2.7 1.4

Reduction in Negative Kinesthetic Effects of Formulation Containing Panthenol vs. Control

Visible/Kinesthetic Attribute Reduction by Panthenol (0-6 scale) Redness -1.4 Burning -2.4 Tingling -5.7 Stinging -4.9 Itching -4.9 Warming -5.7

Ebner F et al. Topical use of dexpanthenol in skin disorders. Am J Clin Dermatol 2002;3:427-433.

Vitamin D

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Vitamin D

•  Several vitamin D compounds and many synthetic variations

•  Active vitamin: 1,25-dihydroxyvitamin D3 •  Dehydrocholesterol (provitamin D)

cosmetically used ingredient which is converted into active vitamin D upon UV exposure

Vitamin D

•  As a result of effects of vitamin D on epidermal growth and differentiation, there has been discussion of skin barrier and photodamage mitigation activities

•  Topical vitamin D analogs used successfully in treatment of psoriasis thought to regulate cutaneous immune system and downregulate epithelial proliferation and promote differentiation

Vitamin K

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Vitamin K

•  Phylloquinone: lipid soluble vitamin K

•  Synthetic form (vitamin K3)- menadione

•  Vitamin K compounds function in blood clotting

Vitamin K Clinical Studies

•  Blinded clinical trial with split face method compared vitamin K with placebo in bruising severity

•  Another study compared vitamin K plus vitamin A with placebo in similar trial methods

•  Each study consisted of 20 subjects that demonstrated decreased bruising, frequency, and severity when applied prior to and after pulsed dye laser treatment

•  Both vitamin K products produced statistically significant results over placebo

Elias PM et al. The Permeability Barrier: Effects of physiologic and non-physiologic lipids. The Lanolin Book,

Biersdorf AG Hamburg Germany 1999; 253-259.