Topics in Dermatology Vermont Association of Naturopathic Physicians January 22, 2011

• David Rochefort, RPh • Northern New England Compounding Pharmacy, Littleton, NH 03561 • (800) 964-0004 www.nnecp.com

1

Objectives • Discuss alternative treatments of common dermatological conditions • Discuss cosmetic formulations and natural options • Discuss formulation considerations and dosage forms

Why Compound? • Ingredient unavailable commercially – Demand – Stability – Combination

• Desired to add or eliminate ingredients – Preservatives – Pharmacological + Cosmetic

• New dosage form

2

UV Damage • Excessive sun exposure is responsible for most of the skin damage associated with aging. This damage accumulates slowly over time and starts at an early age. • Most common requests for repair – Discoloration – Wrinkles/fine lines – Chronic dryness

Formulas to treat UV Damage • • • • • • • • •

Eye Serums / Under Eye Creams Anti-Wrinkle Facial Creams/ “Super Creams” Alpha Hydroxy / Polyhydroxy Acid Products Skin Lighteners After Peel Products Exfolliants Lip Care Men’s Products, After Shave Lotions Cosmetic Color Products

3

Targets in Skin Anti-Aging General Objectives • Repair and protect epidermal barrier – Example -- replenish with lipids, ceramides, barriers

• Protect against oxidation - Antioxidants • Optimize cellular defense – Example -- Vitamin C, Retinoids

• • • •

Increase Cellular proliferation – AHA’s Enhance fibroblast activity – Biopeptides Protection from UV- Sunscreens Protect from smoke, environmental toxins – Antioxidants

Ingredient

Conc

Stability Issues

Examples

Ascorbic Acid

1 to 20+%

oxidation is a problem, will turn brown quickly

Vitamin C serum, or Cream.

1 to 20+%

This is an ester of ascorbic acid Some skin care people claim this is mildly COMEDOGENIC, thus promoting comedones (clogged pores)

Ascorbyl Palmitate 10% in light facial cream. Reduces redness and blemishes from sun damage. Can be added to retinoids for acne

1 to 20+% (5 to 10% common )

This is an another ester of vitamin C that is WATER SOLUBLE and very stable in H20 solutions. It prefers a slightly neutral to neutral pH, so may present an issue with acidic ingredients. has skin lightening properties, and has been studied in acne. There is an enzyme that cleaves the molecule in the skin and converts to ascorbic acid.

Vitamin C Acne Cream

Ascorbyl Palmitate

Sodium-LAscorbyl-2Phosphate

4

Vitamin E Acetate (1iu/mg)

Tocotrienols 50% solution (30-3794)

Idebenone

0.5 to 5%

oily, resides in oil phase of emulsion. Decent antioxidant

0.1 to 2%

is a true full spectrum palm tocotrienol complex with the highest ratio of alpha-, beta-, gamma, and delta-tocotrienols. Contains natural occuring mixture of tocotrienols and tocopherol extracted and concentrated from virgin crude palm oil/ palm fruits (Elaeis guineensis). It also contains of other phytonutrients such as plant squalene, phytosterols, coenzyme Q10 and mixed carotenoids that are naturally extracted together with tocotrienols from palm fruits, making it a natural and wholesome tocotrienol complex. Oily solution, very good antioxidant

0.5 to 2%

Synthetic derivative of CoQ10 with greater stability compared to CoQ10 in aqueous systems, as well as increased antioxidant properties.

Vitamin E Cream

Eye Cream; Lip Cream-works on fine lines

0.5 to 5%

Great antioxidant with lipo and hydrophilicity. Has a smell to it, which limits its use a bit. Use of vitamin E and A with it helps diminish the smell.

Retinol Molecular Film Fluid 0.1%

0.1 to 3%

Molecular dispersion of pure vitamin A (retinol), which is designed to keep the retinol more stable in the formulation as well as assist in permeation. Even though this liquid has 0.1% retinol, it gets into the skin very well. If using this or any other vit a derivative, be sure the patient is using sunscreen. Goes into creams very easily.

Vitamin A palmitate (1,7M IU/gm)

0.05 to 0.3%

used for vitamin A content. vitamin E needed to help stabilize.

Coenzyme Q10

0.1 to 2%

protect from light, other antioxidants need to be present in formula to help stabilize, yellow in color

0.1 to 1%

Multiple actions against skin aging… antioxidant, free radical scavenger, chelating agent, anti-glycating agent, anti-crosslinking agent Protects the skin with two lines of defense against reactive oxygen species (ROS) and reactive carbonyl species (RCS)Exists in muscle tissues and brain and protects against oxidative stress

Lipoic acid (30-2781)

L-Carnosine

Fine lines and wrinkles lips and eyes

Eye and lip creams

5

Glycine Soya Protein

Bacopa Monnieri liquid extract

Peucedanum Ostrithium Liquid Extract (Masterwort)

3 to 7%

Good moisturizer with protection against UV damage, also has some antioxidant effect. A solution that is easy to incorporate into creams

3 to 5%

Ayurvedic medicine, soothes and protects the skin; inactivates free radicals and reduces UVA induced lipid peroxidation in vitro. It has the ability to reduce cutaneous sensitivity

1 to 3%

used for wound healing and anti-inflammatory. reepithelialization, stretch marks, after-sun, wound healing. Antioxidant, mildly astringent, moisturizing. Invitro tests have been intriguing

N-Acetylcysteine 1 to 10% (30-1601)

Ingredient

Glycosaminogl ycans Solution Acetyl Hexapeptide-3 Solution

Repairs acute damage

Smells too bad to use

concentration

notes

formula examples

1 to 5%

Decreases action of MMPs that breakdown collagen and elastin. successful in dark circles, rosacea as well

Adrenal stress eye cream

5 to 10%

BOTOX like action, inhibits acetylcholine at the neuro junctions, just in a more mild fashion.

Anti aging cream or aftershave

Palmitoyl 1 to 10% Pentapeptide (5% typical) 3

stimulates fibroblasts to make more collagen.

Yeast Extract Solution

0.5 to 2%

stimulates fibroblasts to make more collagen

Wrinkle creams

Acetyl Dipeptide-1 Cetyl Ester Solution

3%

This is an endorphin like peptide that reduces cutaneous sensitivities

Excellent acute treatments

6

1 to 3%

All natural, physical exfoliant designed for body use, due to the size of the microspheres. Can be used in cleansers and creams/gels

Exfoliant, Grape Seed Face

1 to 3%

All natural, physical exfoliant designed for face or body use, due to the size of the microspheres. Can be used in cleansers and creams/gels

Chamomile Flower Fluid Extract

1 to 5%

calming, soothing, anti-inflammatory. Great for acne, post peel, post meso, post sun

Marigold Extract

1 to 5%

Soothing and antiseptic in nature, used in ancient times for wound healing and to reduce scars

Ferulic Acid

0.1 to 10%

natural cinnamic acid derivative that is a tremendous antioxidant. Is also considered a natural UV filter (UVB 236 - 322 nm)

EGCg (>90%) (30-3876)

0.1 to 2%

predominate green tea catechin, excellent antioxidant with antibacterial, antifungal and antiviral properties. Potential for keloids.

DMAE Complex 38% W/V

up to 15%

proprietary solution of DMAE Glycolate, pH'd to around 5. Toning, low to no smell.

L-Carnitine

up to 10%

Actually increases skin cell turnover much like AHA's but without irritation or sun sensitivity. pH is neutral as well. Most common % is around 5.

Arnica Flower Tincture

up to 5%

promotes healing and increases circulation. Some have used it in after sun products as well.

Witch Hazel Extract

up to 10%

astringent and disinfectant. Used in toners

Pineapple Liquid Extract

up to 20%

natural toner with antioxidant benefits

Bioflavinoids Citrus 13% Powder

0.1 to 1%

antioxidant

Exfoliant, Apricot-Body

7

Wrinkles • Part of aging • Skin damage from breakdown of elastin and collagen • Matrix metalloproteinases (MMP), the enzymes that break down collagen and elastin, the skin's key structural proteins. MMP become overactive as we age and contribute to wrinkles and sagging skin. • Transretinoic Acid (Tretinoin) is a Vitamin A derivative that indirectly inhibit MMPs • Squalane has been called ‘facelift in bottle’

Tretinoin • Commercially available as Renova or Retin-A • Can be compounded with other components • Increases sun sensitivity, skin-irritation, dryness, peeling. Associated with dose • Effective for wrinkles, acne, and other conditions

8

Acne ƒ Niacinamide 4% Gel provides potent anti-inflammatory activity ƒ No risk of inducing bacterial resistance* ƒ Equal in efficacy to 1% Clindamycin ƒ Seems to work best on active lesions • International Journal of Dermatology. 34:434-437

ƒ Azelaic acid 5% ƒ Lipoic acid 0.5% ƒ Tretinoin topical 0.05% - 0.1% cream; gel; etc ƒ Tea Tree Oil 5% Gel

Eczema • Eczema is a form of dermatitis. The term eczema is broadly applied to a range of persistent skin conditions. These include dryness and recurring skin rashes which are characterized by one or more of these symptoms: – – – – – –

redness, -Flaking skin edema (swelling) -bleeding itching and dryness -oozing Crusting -blistering Cracking Areas of temporary skin discoloration may appear and are sometimes due to healed lesions, scarring is rare. In contrast to psoriasis, eczema is often likely to be found on the flexor aspect of joints.

• Traditional treatments include steroids, antibacterial ointments, and antihistamines

9

Eczema--Treatments • Cyanocobalamin 0.07% Cream – Vitamin B12 inhibits production of inflammatory cytokines and can trap nitric oxide. – Apply the vitamin B12 cream two times per day for eight weeks. – Only a few mild adverse reactions – British Journal of Dermatology (2004;150:977–83).

Eczema--Treatments • Vitamin E 400iu/gm Cream – 60% reported "great improvement" or near remission of their eczema, while only 2% of those taking a placebo reported similar improvement. – Blood levels of immunoglobulin E (IgE), a measure of immune-system stimulation, also decreased in those taking vitamin E, no change in placebo group – Moisturizers such as squalane, allantoin, and essential oils can be formulated with this – Adjunct to dietary modifications ie. Allergy elimination – International Journal of Dermatology (2002;41:146–50).

10

Eczema--Treatments • Extreme Moisturizing Cream: – Urea – Allantoin – Squalane – Avocado Oil – Coconut Oil – Glycerin • In a thick cream base used in conjunction with dietary and immune modification

Psoriasis • Psoriasis a chronic, non-contagious autoimmune disease which affects the skin and joints. It commonly causes red scaly psoriatic In contrast to eczema, psoriasis is more likely to be found on the extensor aspect of the joint. • The disorder is a chronic recurring condition which varies in severity from minor localized patches to complete body coverage. Fingernails and toenails are frequently affected (psoriatic nail dystrophy) and can be seen as an isolated finding. Psoriasis can also cause inflammation of the joints, which is known as psoriatic arthritis.

11

Psoriasis • Typical treatment includes corticosteroids, coal tar, immunosuppressants • Many adverse side effects • Raptiva taken off market 4/9/09 due to progressive multifocal leukoencephalopathy – Rare brain disorder

Psoriasis • Zinc Pyrithione 0.25% Solution – Apply twice daily for 3 weeks • Reduction in scale, erythema, and pruritus. No significant side effects during and after the treatment period. • Exact mechanism of action of the zinc pyrithione is unknown it may be speculated that the possible antiproliferative mechanism of action of zinc pyrithione may involve the regulation of DNA transcription factors containing "zinc finger" binding domains. It is also well recognized that many enzymes require the binding of metal ions for activation. It is also well known that a deficiency of zinc produces psoriasiform lesions. Perhaps the vehicle or the activated form of zinc pyrithione permits a physiologic level of zinc to be reached in the target cells, either epidermal and/or lymphocytic. Dermatology Online Journal: 3(1) : 3

12

Psoriasis • • • •

Cyanocobalamin 0.7%/Avocado Oil 5% cream Avocado source for Omega-3 FA Compared to Vitamin D Analogue (4-week max) Vitamin B(12)/Avocado preparation suitable for use in long-term therapy • Tolerability of the vitamin B(12) cream containing avocado oil as significantly better in comparison with that of calcipotriol. – Dermatology. 2001;203(2):141-7

Warts • • • • •

Viral component-HSV 2-deoxy (d) glucose 0.19% Cream Active component of Alaskan Red Algae Applied twice daily for 8 weeks Zinc can also be added for it’s anti-viral activity – Antiviral Res. 1986 May;6(3):137-49

13

Summary • How and why things can be compounded • Utilized what you need for what you’re treating • Questions • For a copy of the handouts email: [email protected]

14