Cosmeceuticals

The Egyptians were the first to recognize the health properties of cosmetics. Up to the  19th century, there was no clear distinction between cosmetics and pharmaceuticals; the separation occurred when the first modern pharmaceutical industry was developed.  Cosmeceuticals rapidly expanded in the 1980s due to hydroxy acids (natural fruit acids) used as exfoliants against wrinkles. Raymond Reed, the founding member of the United States Society of Cosmetic Chemists, coined the term ‘Cosmeceutical’ in 1961. In 1971, Albert Klingman reactivated interest in cosmeceuticals by developing a formula to improve the appearance of  UV damaged and wrinkled skin, using retinoic acid. They are applied topically as cosmetics but contain ingredients that influence the skin’s biological function. Cosmeceuticals improve appearance, but they do so by delivering nutrients necessary for healthy skin. Desirable features of cosmeceutical agents are efficacy, safety, formulation stability, novelty, and patent protection, metabolism within the skin, and inexpensive manufacture. Even though some products claim to be unique botanical extracts or contain some rare ingredients with magic anti-aging properties, most of the cosmeceutical formulations use fundamental ingredients such as peptides, retinol, coenzyme Q-10, ceramides, α-lipoic acid, α-hydroxy acids, β-hydroxy acids, Aloe vera, panthenol, kinetin and vitamin A, C, E. 

Skin Cosmeceuticals 

Cosmetics and skincare products are part of everyday grooming. Protecting and preserving the skin is essential to good health. Skin, the largest organ in the body, separates and protects the internal environment from the external one. UV radiations from sunlight penetrate the skin and accelerate damage due to free radicals, which include inflammation,  wrinkling, and hyper-pigmentation. Due to prolonged exposure to UV radiation, the collagen and elastin fibers of the skin are broken down by enzymes collagenase and elastase and the texture of the skin deteriorates. Collagen and elastin are responsible for maintaining the elasticity and integrity of the skin. Cosmeceuticals being cosmetic products having medicinal or druglike benefits can affect the biological functioning of skin owing to the type of functional ingredients they contain. There are skincare products that go beyond coloring and adorning the skin. These products improve the functioning/texture of the skin by encouraging collagen growth by combating harmful effects of free radicals, thus maintaining keratin structure in good condition and making the skin healthier. Table.1 enlists the desirable attributes from each category of cosmeceutical. 

Table.1: Types and Efficacies of Cosmeceutical Products 

Type of Cosmeceutical ProductEffect/ Efficacies
ShampooPrevents dandruff and itching. 
Prevents a bad odor of hair and scalp. 
Cleans hair and scalp. 
Maintains the health of hair and scalp. 
Improves suppleness of hair and scalp. 
RinsePrevents dandruff and itching. 
Prevents a bad odor of hair and scalp. 
Replenishes and maintains moisture and oil of hair. 
Prevents split ends, breakage, or damaged hair. 
Maintains the health of hair and scalp. 
Improves suppleness of hair and scalp.
Beauty lotionTreats rough or chapped skin. 
Prevents prickly heat, chilblains, chapping, cracks, or pimples. 
Treats oily skin. 
Prevents razor burn. 
Prevents spots or freckles due to sunburn. 
Treats hot flashes due to sunburn or slowburn. 
Tightens cleans or conditions skin. 
Maintains the health of the skin or increases moisture of the skin. 
Cream, milky lotion, hand cream, and cosmetic oil Treats rough or chapped skin. 
Prevents prickly heat, chilblains, chapping, cracks, or pimples. 
Treats oily skin.  Prevents razor burn. 
Prevents spots or freckles due to sunburn. 
Treats hot flashes due to sunburn or snowburn. 
Tightens, cleans, or conditions skin. 
Maintains the health of the skin or increases moisture of the skin.  Protects skin or prevents dry skin.
Shaving preparationPrevents razor burn. 
Protects skin and makes shaving easier. 
SunscreenPrevents skin roughness due to sunburn or snowburn. 
Prevents sunburn or snowburn. 
Prevents spots or freckles due to sunburn. 
Protects skin. 
Face packTreats skin roughness or chapped skin. 
Prevents pimples. 
Treats oily skin. 
Prevents spots or freckles due to sunburn. 
Treats hot flashes due to sunburn or snowburn. 
Smoothens skin. 
Cleans skin. 
Medicated soap  (including facial cleaners) Soap with a disinfectant as the main agent 
Cleans disinfects or sanitizes skin. 
Prevents bad body odor and prevents pimples. 
Soap with antiphlogistic as the main agent 
Cleans skin and prevents pimples, razor burn, and skin roughness. 

OLAY vitamin line, which includes vitamins A, C, D, E, selenium, and lycopene, pycnogenol plus zinc and copper, is a well-established skincare line. The treatment of aging skin with a  cream containing a hormone such as estrogen results in a fresh appearance with a  rejuvenating effect. Dry emollient preparation containing monounsaturated Jojoba esters is used for cosmeceutical purposes. Novel cosmetic creams or gels with active ingredients and water-soluble barrier disruption agents such as vitamin A palmitate have been developed to improve deteriorated or aged skin. Plant extract of genus Chrysanthemum has been utilized in a cosmetic composition for stimulating skin and/or hair pigmentation. 

In general, vitamins, herbs, various oils, and botanical extracts may be used in cosmeceuticals, but the manufacturer may not claim that these products penetrate beyond the skin’s surface layers or that they have a drug-like or therapeutic effect. For cosmetic labels,  no division between active ingredients and other ingredients is required; they are all listed together. The most important botanicals about dermatologic uses, such as cosmeceuticals, include teas, soy, pomegranate, date, grape seed, pycnogenol, horse chestnut, German chamomile, curcumin, comfrey, allantoin, and aloe; only green and black tea, soy, pomegranate, and date have been studied to the extent that clinical trials. Few botanical-based cosmeceuticals have uses that are supported by evidence-based science. 

The anti-aging creams currently in the market include Rosmarinus officinalis, Vitis vinifera (grape seed extract), citronellol, Limonene, Oenothera biennis (evening primrose),  Glycyrrhiza glabra (licorice extract), Aframomum angustifolium seed extract, diosgenin (wild yam), N6 furfuryladenine (kinetin), and ergothioneine. Randomized controlled trials are still needed, although some ingredients may have a scientific basis for their use. 

Chemoprevention by oral or topical use of dietary or pharmacologic agents to inhibit or reverse the development of cancer is a possibility. Potential cosmeceutical agents in this category include green tea, grape seed extract, vitamin E, and beta-carotene.  Table.2 highlights the cosmeceutical agents obtained from botanical sources. 

Table.2: A Cross-section of Botanical based Cosmeceuticals available Commercially 

Cross-section of Botanical based Cosmeceuticals available Commercially 
Cross-section of Botanical based Cosmeceuticals available Commercially 

Some cosmeceutical agents widely used for topical application are described below. 

Retinoids 

A great amount of research has concentrated on its use as an anti-aging compound as well as its use for other cutaneous disorders. Vitamin A and its derivatives have two main functions: they act as antioxidants, and they activate specific genes and proteins. Structural changes underlying the cosmetic benefits include correction of epidermal atrophy,  deposition of new collagen, generation of new vessels, and enhancement of mitogenesis.  This enhanced mitogenesis promotes the shedding of melanin-laden keratinocytes, resulting in bleaching and subsequent depigmentation. The ability of topical tretinoin to improve the appearance of aged and photo-damaged skin by reducing wrinkles, decreasing laxity,  bleaching hyperpigmented spots, and bringing about a smoother surface has been well studied and documented. 

Hydroxy acids 

Hydroxy acids are organic carboxylic acids classified into alpha-hydroxy acids (AHAs) and beta hydroxy acids (BHAs) according to their molecular structure. Many are derived from natural sources and are often referred to as fruit acids. The different AHAs include glycolic acid, lactic acid, citric acid, mandelic acid, malic acid, and tartaric acid. AHAs have been shown to decrease the signs of aging. The skin appears smoother and more uniform. BHAs are aromatic compounds. Salicylic acid is the reference BHA; it has hemolytic properties and helps in various xerotic and ichthyotic disorders. Other BHAs include 2-hydroxy-5-octanoyl  benzoic acid, also known as β-lipo hydroxy acid, and tropic acid. Studies show that AHAs may increase sensitivity to UV radiation and that sunscreen application may be advisable when these products are used. 

Antioxidants 

In addition to the external insults like UV radiation, drugs, air pollutants, and heat and/or cold, the skin also has to cope with endogenous mitogens, most importantly Reactive  Oxygen Species (ROS) and other free radicals. These species are continuously produced during physiological cellular metabolism. To counteract the harmful effects of ROS, the skin is equipped with an antioxidant system to maintain equilibrium between the pro-oxidants, or damaging agents, and the antioxidants, or protective agents; these antioxidants intervene at different levels in the protective process. The examples of antioxidants include vitamin C,  vitamin E(α-tocopherol), panthenol, lipoic acid, niacinamide, dimethylaminoethanol,  spin traps [species that react with reactive free radicals to produce fairly stable, unreactive free radicals, thus blocking the free radicals from damaging cellular components e.g. DMPO  (5, 5-dimethyl-1-pyrroline-N-oxide), DEPMPO (5-diethoxyphosphoryl-5-methyl-1-pyrrolidine-oxide), TEMPONE-H (1-hydroxy-2, 2, 6, 6-tetramethyl-4-oxo-piperidine]. Others include melatonin (a hormone secreted by the pineal gland), catalase, glutathione, superoxide dismutase, glucopyranosides, polyphenols, cysteine, uric acid, and carnosine.  

Allantoin 

Allantoin promotes cell proliferation, aiding in the healing process. Allantoin has long been known to enhance the effectiveness and desirability of cosmetic creams and lotions by its action as a skin protectant. Allantoin has been incorporated into shampoos, lipsticks,  shaving creams, sun tanning products, bath foams, hair gels, baby powders, and various aerosol preparations. Allantoin has been called a cell proliferant, an epithelization stimulant,  and a chemical debrided. It is said to clean away necrotic tissue, hastening the growth of new healthy tissue. 

Furfuryladenine 

Furfuryladenine (Kinerase) is a natural plant growth factor that retards the aging process in plants. It is marketed as the natural evolution of anti-aging treatment with similar effects in vitro on human skin cells as that in plants, helping to slow and reverse alterations that naturally occur in the cell-aging process. 

Depigmenting agents 

Hyperpigmentation is the result of an increased amount of melanin in the epidermis, the dermis, or both. This pigmentary change can be divided into two pathophysiological processes: melanocytosis (increased number of melanocytes) and melanosis (increased amount of melanin). Hyperpigmentation, the most common and distressing condition afflicting a large subset of the population, requires cosmeceutical skin-lightening agents and corrective camouflage formulations. Combination agents with sunscreen are often the most effective treatment available. Depigmenting agents work best when melanosis or melanocytosis is restricted to the epidermis. Depigmenting agents can be divided into  several groups: 

  1. Phenolic compounds include the following: Hydroquinone, monobenzylether of hydroquinone, 4-methoxyphenyl, 4-isopropylcatechol, 4-hydroxyanisole, N-acetyl-4-  S-cysteaminylphenol. 
  2. Non-phenolic compounds include the following: Corticosteroids, tretinoin, azelaic acid, N –acetylcysteine, L-ascorbyl-2-phosphate. 
  3. Kojic acid combination formulae include Kligman’s formula, Pathak’s formula,  Westerhof’s formula. 

Sunscreens 

Regular use of effective sunscreen is the most important step to maintain healthy,  youthful-looking skin. Primarily, the ultraviolet light from the sun causes most of the visible effects of ‘aging’ skin. Traditional chemical sunscreens act primarily by binding to skin protein and absorbing ultraviolet B (UVB) photons (280-320 nm) and most are based on para-aminobenzoic acid (or its derivatives), cinnamates, various salicylates, and benzophenones,  dibenzoyl methane, anthralin derivatives, octocrylene, and homosalate. Avobenzone  (Parsol-1789) is a benzophenone with excellent ultraviolet A (UVA) protection. Physical agents, or sunblocks, act as barriers, which reflect or scatter radiation. Direct physical blockers include metal-containing compounds such as iron, zinc, titanium, and bismuth. Zinc oxide and titanium dioxide are highly reflective white powders, but submicron zinc oxide or titanium dioxide powder particles transmit visible light while retaining their UV blocking properties, thus rendering the sunblock invisible on the skin. Some commercially available sunscreens are benzophenone-8, Neo Heliopan MA and BB, Parsol MCX and HS, Escalol 557,  587, and 597. A patent reports a sunscreen composition comprising of activated platelet factor as an ingredient in a cosmeceutical acceptable carrier. Such a composition in the form of shaving cream or foam, aftershave lotion, moisturizing cream, suntan lotion,  lipstick, would assist in restoring the skin to its natural condition when the skin is damaged by cuts, abrasions, sun, wind, and the like. 

Moisturizers 

Moisturizers function to smooth out the age lines, help brighten, and tone the delicate skin. Moisturizers usually incorporate emollients to smoothen the skin surface by working their way into the non-living outer layers of the skin, filling spaces between the layers and lubricating, and humectants to help skin cells to absorb and retain moisture in these layers.  Healthy Remedies Balancing Lotion® has been created for menopausal women containing ingredients, which diminish the appearance of fine lines, and wrinkles, uplift the neck area, and moisturize the dry, sagging skin. Some of those ingredients include black cohosh, soy extract, and vitamins A and E. Augmenting the skin’s natural moisture balance is a nourishing complex containing hyaluronic acid and a revival complex containing green tea leaf extract,  and glutathione. 

Bleaching agents 

Bleaching agents are used for bleaching/fading the various marks and act to block the formation of the skin pigment melanin. Hydroquinone is the most commonly used agent for  ‘bleaching’ brown marks, liver spots, and melasma. It has been developed as a synthetic detergent bar for skin bleaching. The bar is composed of a synthetic anionic detergent,  hydroquinone, a stabilizer for hydroquinone, water, a buffer that maintains the pH between  4 and 7, and excipients such as waxes, paraffin, dextrin, and starch. Similarly, a skin bleaching preparation comprising hydroquinone, tertiary butyl hydroquinone, and optionally an additional stabilizer and buffer to maintain the pH between about 3.5 and 7.5 has also been developed. Because of the maintenance of low pH and the presence of a stabilizer,  hydroquinone is not oxidized and thus the product is characterized by extended shelf life. 

Hair Cosmeceuticals 

Haircare, color, and style play an important role in an individual’s physical appearance and self-perception. Among the earliest forms of hair cosmetic procedures in ancient Egypt were hair setting by the use of mud and hair coloring with henna. In ancient Greece and Rome,  countless ointments and tonics were used for the beautification of the hair, as well as remedies for the treatment of scalp diseases. While shampoos have primarily been products aimed at cleaning the hair and scalp, current formulations are adapted to the variations associated with hair quality, hair care habits, and specific problems such as treatment of oily hairs, dandruff, and androgenic alopecia related to the superficial condition of the scalp.  Cosmetics for the treatment of hair are applied topically to the scalp and hair. While they can never be used for therapeutic purposes, they must be harmless to the skin and scalp, to the hair, and the mucous membranes and should not have any toxic effect, general or local, in normal conditions of their use. A hair care cosmetic composition comprising iodopropynyl butyl carbamate and/or a solution of zinc pyrithione in N-acyl ethylenediamine triacetate has been patented, which includes an appropriate carrier and a non-allergenic dry extract of yarrow (Achillea millefolium L.), obtained by oxidation of a water-alcohol solution extract of flower tops of yarrow. The extract containing less than 0.5% by weight of polyphenolic derivatives, is used for the treatment of hair, in particular oily hair, based on an extract of yarrow.  A patent describes a method for treatment for androgenic alopecia wherein Liquor Carbonic  Detergents are topically applied. It is generally accepted that genetic hair loss arises from the activation of an inherited predisposition to circulating androgenic hormones. 

Typically, a hair cosmeceutical product includes – conditioning agents, special care ingredients, and hair growth stimulants. Conditioning agents are intended to impart softness and gloss, reduce flyaways, and enhance the disentangling facility. Several ingredients may be used, mostly fatty ingredients, hydrolyzed proteins, quaternized cationic derivatives,  cationic polymers, and silicones. Accordingly, current antidandruff ingredients are virtually all-effective antifungal agents – zinc pyrithione, ciclopirox, and ketoconazole. Hair growth stimulants cannot be expected to have any impact on hair growth due to short contact time and water dilution. A minoxidil-related compound (2, 4-diamino-pyrimidine-3-oxide) is a  cosmetic agent with the claim of acting as a topical hair growth stimulant. Its target of action has been proposed to be the prevention of inflammation and perifollicular fibrosis. Some degree of efficacy of 2, 4-diamino-pyrimidine-3-oxide has been claimed in the prevention of seasonal alopecia. In the United States recent approval of two new products, Propecia and  Rogaine Extra Strength (Minoxidil) 5%, indicated in men to promote scalp hair growth, have added a new dimension to treatment options offered by physicians in treating androgenetic alopecia. 

Other Cosmeceuticals 

The skin beneath the eye lacks subcutaneous fat and has virtually no oil glands. This delicate skin needs protection and plenty of moisture to replenish and repair, which helps to reduce the signs of premature aging. As the skin ages, it becomes thinner, drier, and rougher.  Over-exposure to the elements and environmental pollution aggravates this condition.  Many topical skin-soothing products intervene in this process, but products for this area need to be particularly gentle and specially formulated with ingredients that work from the inside out by interacting with the cells under the skin’s surface – without irritating the eyes.  Numerous cosmeceutical eye creams nourish the skin with natural emollients and beneficial nutrients. The other functional ingredients include butcher’s broom,  chamomile, and vitamin E, antioxidants – vitamins A, C, and E, green tea and Tiare flower,  Ginkgo biloba, and also cucumber, calendula, and α-bisabolol, an active constituent of chamomile, to calm irritated skin. A key ingredient in the eye lifting moisture cream – that treats puffiness, irritation, and also protects against future skin damage is yeast which helps to plump up the wrinkles. The eye wrinkle cream helps to forestall the signs of aging and generally contains wheat germ and corn oil, squalene, and carrot extract. Eye firming fluid has again, algae extract from seaweed that helps the skin to maintain elasticity. Lawlor had developed dental care compositions, which are useful for providing a substantive composition on the surfaces of the oral cavity, which can provide prophylactic, therapeutic, and cosmetic benefits. 

The rationale to Create a Cosmeceutical Category 

The absence of a proper regulatory framework and dilemma over the understanding of the term cosmeceuticals has become an undue advantage of the cosmetic manufacturer. Manufacturing,  labeling, sale, and advertisement of such products need a proper regulatory framework to safeguard the interest of consumers and control the regulatory market. The current legal definitions of drugs and cosmetics are archaic and unworkable. At present, the dividing line between the two is not sharp and the transition towards acceptability of cosmeceuticals is relatively slow as far as the regulatory framework is concerned. 

The regulatory framework shall help to 

  1. support the use of pharmaceuticals by health care professionals. 
  2. ensure and provide factual information to the public regarding pharmaceuticals. 
  3. protect the consumers from unproven claims and unsafe products. 
  4. drive the growth and export of pharmaceuticals. 

By the addition of a small number of cosmeceutical agents to the cosmetic formulations which do not require medical regulations would improve the production of cosmeceuticals that could help to improve skin, nail, and body mass growth. New challenges will also be presented to government regulatory agencies as more chemicals with true biological activity are invented and tested. In conclusion, cosmeceuticals are not only for external beautification but also for improvement of the internal beauty through health-related functions. 

The convergence of cosmetics and foods, so-called nutricosmetics, refers to oral supplementation of nutrients, marketed mainly for anti-aging effects, i.e. reducing wrinkles by fighting free radicals generated by solar radiation. Nutricosmetics include antioxidants such as carotenoids (beta-carotene, lycopene, lutein, zeaxanthin, and astaxanthin) and polyphenols (anthocyanidins, catechins, flavonoids, tannins, and procyanidins).

Make sure you also check our other amazing Article on : Definition of Cosmetics as per Indian Regulations
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