15 Over-the-Counter Preparations
Summary
Keywords: nutraceuticals follicular health nutritional supplements healthy hair
Key Points
•Although there are a great number of over-the-counter preparations available for our patients, most are compounded from similar ingredients.
•The nutraceuticals and supplements described herein have been determined to be safe in that they have not been shown to be detrimental to health when taken in the amounts and dosages recommended.
•Currently, most evidence for the efficacy of ingredients in over-the-counter preparations is anecdotal; however, current objective scientific research is ongoing.
15.1 Introduction
Throughout history, men and women have sought to improve the appearance and vitality of their hair. It is no surprise then that when faced with hair loss, they have searched high and low for a pill or a potion which would return their hair to its pre-loss amount and condition. That search, to this day, is unfortunately met all too often with grand promises wrapped in slick marketing and clever sales.
As medical practitioners specializing in the medical and surgical diagnosis and treatment of hair loss disorders, patients commonly present with questions regarding any number of preparations available on the market today. And that market is huge. Sales in the global hair care market have been estimated as high as 83.1 billion dollars (USD) in 2016, and is projected to reach 100 billion by 2021.1,2 The products sold today contain a wide range of ingredients and patients look to us for guidance. Confounding the issue is the fact that many of these preparations are proprietary formulations, whose complete ingredients are known only to the manufacturers themselves.
Faced with this reality, this chapter will discuss some of the more common ingredients compounded throughout this long history of preparations, in an effort to help us educate our patients about the benefits, but most importantly the limitations of these available over-the-counter (OTC) preparations. While the list is certainly not exhaustive, it hopefully will cover the most often listed ingredients in preparations we are called upon to give our opinion about during consultation with our patients.
15.2 Background
In general, these preparations can be grossly broken down into two functional categories. There are those products which are thought to influence the growth and vitality of the hair fiber itself, typically affecting events that occur at the metabolic level of the hair follicle, and those products which are aimed at improving the cosmetic appearance of the hair fiber once it has been expressed as a result of follicular growth. Examples of the former category are usually, but not always, ingested preparations, alone or in combination with one another, while the latter category includes topical agents such as shampoos and conditioners. Finally, some of the more common commercially marketed hair care programs, or systems, which may supply both of these categorical preparations will be briefly reviewed. First let us examine preparations thought to positively influence follicular health and growth.
15.3 Preparations Affecting Follicular Health and Growth
The ingredients found in these commonly available preparations will fall into one of three general ingredient categories: herbal, supplemental, or medicinal. Herbal ingredients, also referred to as nutraceuticals or phytomedicinals, include substances directly derived from plant matter, with little or no processing other than the isolation of that main ingredient. The second category, dietary supplements, would include nutritional additives such as vitamins and minerals, for example, niacin, iron, and copper. Our third category, medicinal ingredients, which technically should be confined to those ingredients available only by prescription, is included here as well; in today’s global market, regulatory rule differences defining these categorical boundaries have become more fluid, and hence have affected the types of preparations patients can obtain “over the counter.” This is especially true of the so-called proprietary formulas, where many of the ingredients are veiled under the protection of industrial “secrets” specific to a particular manufacturer. These formulations may be ones that are protected by copyright, patent, and/or trademark. Let us first examine commonly encountered herbal ingredients.
15.4 Herbal Ingredients
A phytomedicine or phytomedicinal refers to an herbal entity that is a whole-plant preparation, as opposed to a single isolated compound. (The prefix phyto comes from the Greek word phyton, meaning “plant.”) The herbal preparation derived from the whole plant will actually contain hundreds of individual active components, which, in total, confer the plants main therapeutic activities and indications. Phytomedicinals are standardized, and their therapeutic values are backed by pharmacological and clinical studies and experience.3 Recognized and regulated in Europe as prescribed by physicians and dispensed by pharmacists, in the United States phytomedicinals are sold as OTC dietary supplements in health food stores and pharmacies. Ongoing research into phytomedicinals at the National Institutes of Health (NIH) under the National Center for Complementary and Integrative Health will no doubt increase our understanding and use of this relatively untapped resource as we explore this emerging field.4
15.5 Saw Palmetto
One of the more common ingredients patients will inquire about will be Saw palmetto, which exists in nature as a berry. The berries of Serenoa Repens, which is a palm tree species, are also known as Sabal Fructos. Saw palmetto contains fatty oils composed of phytosterols and polysaccharides. Saw palmetto has been thought to act as a 5-alpha-reductase inhibitor, and in this capacity it is proposed that it acts to reduce dihydrotestosterone (DHT) levels affecting male-pattern hair loss (MPHL). This is similar in activity to finasteride, although Saw palmetto is very weakly inhibitive by comparison.5 Typical recommended dosage is 320 mg daily.
15.6 Pygeum
Pygeum or Pygeum africanum contains beta-sitosterol, oleanolic acid, and ursolic acid, and its mechanism of action seems to be principally aimed at reduction of inflammation and swelling as seen in benign prostatic hyperplasia (BPH). In this respect, it is similar in action to Saw palmetto, but through a different biochemical pathway, which does not involve lowering of DHT levels. There are no studies available to confirm claims made that pygeum will improve hair growth and/or quality.
15.7 Stinging Nettle Root
Nettle root or Urticae radix is often used in combination with Sal Palmetto, and its sole known effect is to increase urinary flow in patients with BPH, which is also one of the effects of Saw Palmetto. Nettle is rich in protein, minerals, and vitamins, especially vitamin E.6 However, there are no definitive data to indicate that Nettle root has any effect upon hair growth or quality.
15.8 Fo Ti (Polygonum Multiflorum) (He Shou Wu)
Fo Ti or Polygonum Multiflorum, also known as He Shou Wu, was arbitrarily named “Fo Ti” on its arrival to America from China in the 1970s. It contains anthraquinones, including chrysophanol, emodin, rhein, and others. It also contains beta-sitosterol, catechins, cyanidins, and stilbene glycoside gallates, as well as the elements zinc, manganese, and calcium. Fo Ti is considered in Asia to be a “magical” herb. In mice, it has shown to have an antiaging effect at the cellular and biochemical level, increasing levels of superoxide dismutase and biogenic amines (5-hydroxytryptamine, norepinephrine, and dopamine) but decreasing the levels of monoamine oxidase-B, lipid peroxide, and malonyl dialdehyde in key organs of aging mice. It also inhibited atrophy of the thymus and adrenal glands. It was found to enhance cellular immunity, lowered LDL while raising HDL lipoprotein levels, and acted as an antioxidant in the liver.7 That research notwithstanding, however, its proposed benefits for hair growth have yet to be independently verified.
15.9 Rosemary
Rosemary leaf or Rosmarini folium is usually available as a topical essential oil, and acts as a skin irritant which increases circulation when applied to the skin. Flavonoids, phenolic acids, triterpenic acids, and monoterpene hydrocarbons are among its list of chemical components. It has been shown to have antioxidative and antimicrobial activity. It has been used with positive results in the treatment of alopecia areata.8
15.10 Horsetail
Horsetail herb or Equiseti herba/Equisetum arvense has been used as a dermatologic agent and supportive agent in wound healing,9 and has also been used as well in the treatment of dandruff as a daily topical preparation. It is a good source of silica, a necessary component for strong shiny hair,3 but the relation between ingestion and positive effects on hair growth remains to be objectively quantified.
15.11 Elderberry
Elderberry or Sambucus Nigra has been used for centuries for a number of medicinal and cosmetic indications. It contains an abundance of phytochemical nutrients, including, but not limited to, alpha-amyrin, astragalin, beta carotene, campesterol, essential fatty acids, and vitamins A, B1, B2, B3, and C. Elderberry has been shown to combat free radicals and decrease inflammation, and boost the immune system. It has been used to treat flu symptoms and sooth skin irritations. Perhaps because of its soothing effects when used for skin irritation, it is included in various hair care products, though no objective studies support claims of positive effects on hair growth. Caution should be used in using this product as the stems contain cyanide and thus can be very toxic. In general, it is contraindicated in pregnancy.3
15.12 Great Burnet
Great Burnet or Sanguisorba officinalis (or Di Yu) occurs as an egg-shaped, crimson flower which is a member of the Rosaceae or rose family and exists as a rhizomatous perennial which can survive for decades due to its extensive root system. Biochemically, the root and rhizomes contain monoterpenoids, flavonoids, saponins, ursolic acid, arabinose, vitamin C, and assorted tannins. It has been used historically in traditional Chinese medicine (TCM) for its ability to stop bleeding and “clear heat.” In western medicine, it has been utilized as both an astringent and anti-inflammatory, both internally and externally. Recently, it has been studied for its inhibitory effects on fibroblast growth factor 5 (FGF5). FGF5 is a regulator of hair growth as an important factor in promoting the irreversible transition from anagen to catagen. Inhibition of FGF5 has been observed to prolong the anagen phase and reduce hair loss.
Limited studies have shown that Sanguisorba officinalis root extract (SO extract) is an effective FGF5 inhibitor, and that SO extract enhanced the multiplication of outer root sheath cells in vitro. In vivo analyses indicated that while SO extract did not enhance the onset of growth, it significantly reduced the number of telogen-phase follicles and increased hair length.1 Subsequent studies have shown that more potent FGF5 inhibitors from various botanicals had similar effects.2 It should be further noted that in those studies, Sanguisorba officinalis root extract was the least potent of all tested. Unfortunately, that study did not reveal which botanicals were more effective, citing commercial interests. FGF5 inhibitors have been sold under the trade names Lexilis (Adnagen) and Evolis (Cellmid).
15.13 Ginkgo Biloba
Ginkgo biloba or Ginkgo Folium comes from one of the oldest trees on the planet, in existence for thousands of centuries. Ginkgo biloba fruits and leaves contain, among other things, bioflavinoids, flavoglycosides, proanthocyanidins, and a collection of unusual polycyclic structures called ginkgolides which are, chemically, polyacetones. Extracts have been used in China for over 5,000 years to treat coughs, allergies, asthma, bronchitis, and other disorders of the lungs and heart. In humans, studies have shown that Ginkgo can improve compromised cerebral circulation (improved hypoxic tolerance) as well as circulatory disturbances related to atherosclerosis. It has also been shown to improve tissue microcirculation. It has been thought that the mechanism of action is based on antioxidant and antiplatelet functions of the active ingredients. Perhaps based on its positive effect on microcirculation, Ginkgo can be found in OTC hair growth formulas, presumably on the assumption that increased microcirculation would benefit follicular health. No clinical studies to date have been conducted to objectively verify this claim.
15.14 Ligustrum
Ligustrum or Ligustrum lucidum, also called dongqingzi as its Chinese synonym, contains triterpenoids, including oleanolic acid, which is thought to be the main biologically active ingredient. Ligustrum is one of the highly valued tonics in TCM, and has been shown to exhibit numerous biologic effects in humans, including prevention of leucopenia in patients undergoing chemo- and/or radiotherapy for cancer. It is known for its anti-inflammatory and circulatory stimulating effects, as well as its ability to lower blood lipid and glucose levels in diabetic patients. It is marketed as an ingredient in topical hair care products to promote hair growth and it is being used in oral preparations for its hair darkening properties and prevention of premature graying.7 Again, despite these reported uses, no formal studies have been conducted to objectively substantiate the benefits to hair growth and maintenance.
15.15 Cade Oil
Cade oil or Juniperus oxycedrus is also known as juniper tar. Pharmacologically, it has been reported to have keratolytic and antipruritic properties, and as well has been shown to exhibit antimicrobial activities in vitro.7 Cade oil is widely used in topical preparations for the treatment of parasitic skin diseases and eczema. It has also been used to address hair loss, though again, claims of its effectiveness for that indication are anecdotal.
15.16 Neem Oil
Neem or Azadirachta indica