INTRODUCTION

The explosive growth of the cosmeceutical industry has resulted in the introduction of many new ‘active’ ingredients. Most are derived from nature for unique marketing stories and to reduce the risk of federal oversight. About 100 different ingredients derived from plant sources are being incorporated into cosmeceutical and skin care products. It behooves all physicians and skincare providers recommending cosmeceuticals to have a working knowledge of botanicals so the best recommendations can be made to patients and clients.

Botanicals used for medicinals, flavorings, or fragrances are known as herbs. These are the historic foundation of pharmacologic medicine. An understanding of the significant science underlying the function of the botanical base is usually lacking. Specific issues include:

The methods of topical application of botanicals include: (1) water-based cream and lotion; (2) oil- and wax-based ointment; (3) powder and paste; (4) poultice of freshly cut herb; (5) fomentation or compress of warmed moistened herb; and (6) juice, tea, tincture, elixir, decoction, and infusion.

In the United States, botanical remedies are considered dietary supplements of food additives by federal regulators so there are no standards for potency of the components and efficacy of the products. In 2003, the Food and Drug Administration removed Ma huang (Ephedra sinica) from the market due to 155 deaths. Thirteen additional herbs including St John’s wort, gingko, ginseng, birthwort, arnica, cayenne, comfrey, henna, kava kava, mistletoe, rue, senna and yohimbine have induced fatalities. Severe mucocutaneous reactions induced by herbal formulations include anaphylaxis angioedema/urticaria, exfoliative erythroderma, linear IgA bullous dermatosis, lupus erythematosus, malignancies, pemphigus, Stevens–Johnson syndrome, Sweet’s syndrome, ulcerative stomatitis, and vasculitis.

The German Commission E regulates botanical products based on usage, clinical efficacy, and the quality of this evidence. It developed standardization of botanical products and now is the standard throughout the developed world. The US equivalent—PhytoPharm U.S. Institute of Phytopharmaceuticals—also evaluates clinical evidence and adverse reactions to identify ‘reasonable uses’ for hundreds of herbs. This information is very important with botanicals because the time of harvest, growing conditions, processing of the herb and ingredient mixes can substantially alter solubility, stability, pharmacokinetics, pharmacologic activity, and toxicity of the finished product.

These multiple variables indicate the need for certain efficacy and safety data. Quality healthcare demands evidence-based decisions. Only finished products tested in controlled double-blind clinical trials compared to placebo or a positive control of a prescription product and conducted by independent researchers using a statistically significant number of panelists is acceptable evidence based effectiveness.

A basic safety study of contact irritation and sensitization with a topical application of 50 or more patients should be a routine safety study for herbal products because these are far the most common adverse reactions. These studies also demonstrate to patients, clients, and media that healthcare providers of skin treatments and products put quality of care ahead of profits made from products based on dubious science and poor, if any, credible data.

Herbs with mucocutaneous therapeutic indications as determined by Commission E and PhytoPharm are listed in Table 12.1. The first group of herbs discussed below consists of most of the top 12 largest selling herbs in the US based on dollar volume. Of all the herbs listed with mucocutaneous applications, only 27 have been supported by reliable double-blind or open label clinical trials as listed in Table 12.2. The second group consists of most of the 21 herbs formulated into products tested in blinded clinical trials for treatment of photoaging as listed in Table 12.3.

Table 12.2 Herbs with clinical trials for treatment of mucocutaneous diseases/conditions

Table 12.3 Herbs with clinical trials for photoaging therapy

LARGEST SELLING HERBS

• Echinacea (Fig 12.1)

Echinacea angustifolia was originally used by the Sioux Native Americans not only for the treatment of snake bites and war wounds because of its antiseptic and analgesic properties, but also for insect bites, gonorrhea, measles, abscesses, and ulcers. The other two species are E. purpurea and E. pallida.

Fig. 12.1 Topical and oral Echinacea is an antioxidant. Echinacea is rich in caffeic and ferulic acids

E. purpurea contains the immunostimulating polysaccharides and glycoproteins, flavonoids, caffeic and ferulic acid derivatives, volatile oils, alkamides, polyenes, and pyrrolizidine alkaloids. E. pallida and E. angustifolia contain the same actives except glycoproteins and pyrrolizidine alkaloids.

All three Echinacea species stimulate immunity, protect type III collagen, and have antioxidant activity, thus photoaging therapy is promising (Tables 12.1, 12.2). They are also cytotoxic to multiple bacteria and viruses.

E. purpurea is approved by the German Commission E for the treatment of stomatitis, wounds, and burns, and to treat and prevent infection. Research has further documented effectiveness in treating psoriasis and herpes simplex.

Echinacea species have a nearly 10% rate of anaphylactic reactions with topical sensitization in atopic patients.

• Saw palmetto (Fig. 12.2)

The major components of saw palmetto (Serenoa repens) include sterols, glucosides, flavonoids, free fatty acids, and polysaccharides. This herb has documented anti-androgenic, anti-estrogenic, anti-inflammatory, and anti-exudative effects. It is a remedy for dermatitis, mucositis, and alopecia in folk medicine (Tables 12.1, 12.2).

Fig. 12.2 Saw palmetto is used orally for patients with androgenic alopecia; it possesses antiandrogen and antiestrogen effects

When used with two other herbs in an open clinical trial of 20 panelists, a significant reduction in sebum production occurred with topical application.

• Ginseng (Fig. 12.3)

There are three species of ginseng. The most potent is Siberian ginseng (Eleutherococcus senticosus). But Panax ginseng is used in more products and Panax quinquefolius is the American indigenous variety. The main active components are steroidal saponins known as ginsenosides, polysaccharides, and polyenes. Lignans, coumarins, steroids, and caffeic acids are only present in Eleutherococcus senticosus.

Fig. 12.3 Ginseng contains ginsenosides and is a topical cosmeceutical antioxidant

Ginseng species have potential as treatments for photoaging. In vitro, Panax ginseng stimulated fibroblast type I collagen synthesis. Ginsenosides in vivo inhibited cyclooxygenase-2, nuclear factor kappa B, activating protein-1, and melanogenesis. Hyaluronan and epidermal growth factor synthesis were stimulated as was matrix metalloproteinase I. Thus a product containing any ginsengs must have a clinical trial with the marketed formulation to prove efficacy for photoaging.

Hair growth was stimulated with topical ginseng in an open clinical trial.

Ginseng enhances immunity and is cytotoxic to tumors when applied topically in mice. This herb has antioxidant and antiviral activity.

Cases of vaginal bleeding from a topical face cream are a very rarely reported adverse reaction, as is death (Tables 12.1, 12.2).

• St John’s wort (Fig. 12.4)

St John’s wort (Hypericum perforatum) is a clinically proven wound healing agent due to its antistaphylococcal anti-inflammatory and T-lymphocyte stimulation activity. In folk medicine, St John’s wort was also used to treat dermatitis.

Fig. 12.4 St John’s wort contains the anti-inflammatory quercetin. It is used to enhance wound healing

This herb’s actives include flavonoids, and oligomeric procyanidins (OPCs), xanthones, acylphloroglucinols, volatile oils, caffeic acid derivatives, and anthracenes including hypericin. The major adverse reactions include death, photosensitivity and radiation recall dermatitis (Tables 12.1, 12.2).

• Lavender (Fig. 12.5)

Lavandula angustifolia aromatic essential oil contains 70% linalool and linoyl acetate in the volatile phase and 13% tannins. Hydroxycoumarin and caffeic acid are non volatile actives. This herb has anti-inflammatory, anti-mutagenic, and antimicrobial, and mast cells inhibition activities. It is cytotoxic to fibroblasts if the concentration exceeds 0.25%.

Fig. 12.5 Lavender contains a high concentration of linalool

Lavender oil is therapeutic for insect bites, burns, wounds, lacerations, acne, psoriasis, herpes, and fungal infections. A double-blinded clinical trial treating alopecia areata with a mixture of five other botanical oils produced a significant improvement in hair regrowth after 7 months (Tables 12.1, 12.2). In a 40-panelist open clinical trial using lavender in an aromatherapy bath, anger/frustration levels were significantly reduced.

One 4-year-old and three young teenage boys were treated with 100% lavender oil or lavender/tea tree oil shampoo, respectively. All four boys developed reversible gynecomastia after about a year of using these products daily. Lavender concentration exceeding 15% produces estrogenic effects due to the potency of its phytoestrogens. Tea tree oil over an 8% concentration damages stratum corneum barrier integrity. Thus, due to the surface to volume ratio effects, children and anyone with a compromised barrier such as an atopic must be cautious using products with lavender concentrations exceeding 5% for prolonged periods.

HERBS IN PHOTOAGING CLINICAL TRIALS

There is a paucity of human clinical trials using topically applied herbal formulations to treat photoaging. Twenty herbal ingredients have been used in these studies (Table 12.3). Only seven were solitary actives in double-blind trials including green tea, soy (total), date palm, licorice, oat, tamarind and coffeeberry.

SUMMARY

Numerous plant-sourced ingredients are being added into cosmeceutical formulations as ‘active’ ingredients. Unfortunately, they have multiple variables that affect formulation integrity and clinical activity and safety. Only 20 herbs have been used in topical formulations treating photoaging in human clinical trials. When treatment of all skin diseases and conditions is administered topically or orally, another 27 herbs have been evaluated in human clinical trials.

This chapter has discussed some of those cosmeceutical herbs that treat skin diseases including photoaging. Botanical ingredients are incorporated into moisturizers, cleansers, toners, cosmetics, and hair care products to add increased consumer interest and benefits.