The Cosmetic World: A New Substrate for Pharmaceuticals

Kamal Dua

Cosmeceuticals are now-a-days available as OTC products and are easily accessible to the users which are quite ignorant and deprived of relevant information about the incorporated pharmaceutical ingredients. These ingredients play vital and significant role in exerting their effects to the user, which are not apparent and prominent by nature but may prove crucial or hazardous during and after their use.

The present article encompasses and establishes a vital relationship between cosmetics and pharmaceutical ingredients with an emphasis on its regulatory aspects, which are essentially required for the safe and beneficial utilization of cosmeceuticals.

Introduction:

Cosmeceuticals, "performance cosmetics", "functional cosmetics","dermoceuticals", "active cosmetics".... these are the buzz words in twenty first century personal care. The revolution they triggered is apparent from the fact that cosmetics are no longer visualized as products that cover up or camouflage imperfections in personal appearance. Today's healthful cosmetics offer protective, healing and rejuvenative attributes as well.

Cosmeceuticals: What they are?

A cosmeceutical is an ingredient with medicinal properties that manifests beneficial topical actions and provides protection against degenerative skin conditions. The word "Cosmeceutical" was popularized by Albert M. Kligman, a professor at the University of Pennsylvania Medical School in the late 1970s. It encompasses cosmetic actives with therapeutic, disease fighting, or healing properties, serving as a bridge between personal care products and pharmaceuticals.

Originally appearing in global markets in the 1990's as an off shoot of the nutraceuticals revolution, cosmeceuticals are now recognized as a rapidly growing segment in health and personal care in countries like India , U.S. , Japan and some European countries. The global business of cosmeceuticals amounts to greater than $50 billion ¹ .

They are applied topically as cosmetics, but contain ingredients that influence the skin’s biological function ¹ . The Food, Drug, and Cosmetic Act defines cosmetics by their intended use, as ‘articles intended to be rubbed, poured, sprinkled, or sprayed on, introduced into, or otherwise applied to the human body for cleansing, beautifying, promoting attractiveness, or altering the appearance.’ Among the products included in this definition are skin moisturizers, perfumes, lipsticks, fingernail polishes, eye, and facial makeup preparations, shampoos, permanent waves, hair colors, toothpastes, and deodorants, as well as any material intended for use as a component of a cosmetic product ² . These cosmeceuticals, serving as a bridge between personal care products and pharmaceuticals, have been developed specifically for their medicinal and cosmetic benefits.

Cosmeceutically active ingredients are constantly being developed by big and small corporations engaged in pharmaceuticals, biotechnology, natural products, and cosmetics, while advances in the field and knowledge of skin biology and pharmacology have facilitated the cosmetic industry’s development of novel active compounds more rapidly. Some commonly used pharmaceutical ingredients in cosmetics are listed in Table-1. Desirable features of cosmeceutical agents are efficacy, safety, formulation stability, novelty, and patent protection, metabolism within skin and inexpensive manufacture ³ .

Present article is an attempt to highlight the salient features of various types of cosmeceuticals (Fig-1) along with a brief discussion on the regulatory aspects controlling the usage and manufacturing of cosmeceuticals.

Skin Aging: Role of Pharmaceutical Ingredients asNutricosmetics ⁴ :

A radiant appearance is only a reflection of optimal health and well-being. This forms the underlying principle of current trends in the personal care industry. Cosmetic products no longer seek to cover up signs of aging. The root causes of skin, hair and nail damage are addressed externally by using cosmeceuticals and internally with nutraceutical supplements.Vitamin and mineral deficiences, poor antioxidant status, impaired digestion and compromised immune functions are all reflected in a sallow complexion, lifeless hair and brittle or discolored nails. Oral intake of antioxidants such as carotenoids, selenium, proanthocyanidins (found in grape seed extract, apples and other plant sources) and vitamin E is reported to reduce the risk of DNA damages by ultraviolet radiation that lead to skin aging and skin cancers. A recent study reports that curcumin, the antioxidant pigment from turmeric is useful in the oral treatment of melanoma. In other studies, orally administerd phytonutrients such as soy isoflavones and green tea polyphenols were found to offer protection against photoaging through inhibiting the action of enzymes that degrade connective tissues.

Skin Aging and Cosmeceuticals ^{5, 6, 7} :

The skin actively participates in the body's homeostasis through its abundant microcirculatory and sensory functions. Its appendages participate in the excretion of sweat and metabolic by-products, and by possibly participating in the regulation of melatonin - a hormone that regulates circadian rhythms in the body. Healthy looking skin therefore reflects overall health and warrants optimal well-being. Natural antioxidants that quench free radicals are an essential component of antiaging formulations. They potentially offer protection against damage to the tissues against the detrimental effects of environmental and other agents. Biochemical reactions that accelerate the progression of skin aging have their roots in inflammatory processes, as inflammation generates micro-scars that mature into blemishes or wrinkles. Various types of inflammatory mediators such as leukotrienes and prostaglandins, cytokines and growth factors may influence melanin synthesis by affecting the proliferation and functioning of melanocytes. Protein kinase C, the enzyme, that phosphorylates proteins, may also influence the growth and differentiation of melanocytes. Cytokines such as endothelins (also known as vasoconstrictive peptides) are also reported to accelerate melanogenesis. Natural anti-inflammatory agents are therefore included in anti-aging formulations, and serve to soothe, heal and protect skin tone and integrity. A wide range of natural actives are available for use in anti-aging topical formulations. It is important however that the ingredients selected are amenable to formulation, and do not damage the appearance, texture and general acceptability of conventional cosmetic compositions. These requirements often pose challenges; necessitating careful application -oriented research to facilitate the development of innovative extracts from traditionally used botanicals.

Pharmaceutical Ingredients Vs. Skin Care Cosmetics ⁴

Cosmetics and skin care products are the part of everyday grooming. Protecting and preserving the skin is essential to good health. Our skin, the largest organ in the body, separates, and protects the internal environment from the external one. Environmental elements, air pollution, exposure to solar radiation as well as normal aging process cause cumulative damage to building blocks of skin – DNA, collagen, and cell membranes. Use of cosmetics or beauty products will not cause the skin to change or heal; these products are just meant to cover and beautify. Cosmeceuticals being cosmetic products having medicinal or drug-like benefits are able to affect the biological functioning of skin owing to type of functional ingredients they contain. There are skin-care products that go beyond coloring and adorning the skin.

Botanicals: Inclusion in Cosmetics ⁵ -

Botanical extracts that support the health, texture and integrity of skin and hair, are widely used in cosmetic formulations. Plant materials, from which these extracts are prepared, have a long history of traditional "cosmeceutical" use, although the term itself is of recent origin. In most cases, these cosmetic applications are adequately supported by efficacy data from scientific literature, as well as documented safety. Among the more popular functional natural ingredients, several antioxidants used in cosmetics, are scientifically proven to offer additional benefits in supporting skin texture, appearance and tone.

Formulation challenges :

However, while in traditional cultures, plant materials were used in crushed or dried and powdered form, their incorporation into contemporary cosmetic formulations presents unique challenges. Highly colored or gritty plant extracts need to be blended seamlessly into "milky" or clear creams, lotions and gels. This is where a judicious blend of art and science comes in handy. The goodness of herbs and botanicals is extracted out and the actives are tailored for use in conventional formulations with their biological activity remaining intact. One example is the curcuminoids-rich turmeric extract well known for its antioxidant properties, antimicrobial effects, and beneficial effects on inflammation. Turmeric has been traditionally used by South Asian women in skin care since ancient times. However, its yellow color may be unattractive to contemporary formulators. An innovative patented colorless (white to very light tan) derivative,

Tetrahydrocurcuminoids, addresses this drawback, and offers effective protection against sun damage. Its antioxidant action is of a comprehensive “bioprotectant” nature, efficiently preventing the formation of free radicals, while quenching pre-formed ones as well, thereby protecting the skin cells from damage by UV radiation and the resultant inflammation and injury. This in turn has far reaching beneficial effects on overall health and well being, rendering a healthy glow to the skin. Additionally the composition efficiently lightens skin tone ⁶ .

Hair Cosmeceuticals:

A hair cosmeceutical product includes – conditioning agents, special care ingredients, and hair growth stimulants. Conditioning agents are intended to impart softness and gloss, to reduce flyaway and to enhance disentangling facility. A number of ingredients may be used, mostly fatty ingredients, hydrolyzed proteins, quaternized cationic derivatives, cationic polymers, and silicons ⁸ . Special care ingredients are aimed at modifying specific problems relating to the superficial scalp. These shampoos are formulated around one or more specific ingredients selected for their clinical effectiveness in these conditions. Accordingly, current antidandruff ingredients are virtually all-effective antifungal agents – zinc pyrithione, octopirox, and ketoconazole ⁹ . Hair growth stimulants cannot be expected to have any impact on hair growth due to shortcontact time and water dilution. A minoxidil-related compound (2,4-diamino-pyrimidine-3-oxide) is a cosmetic agent with claim of acting as a topical hair growth stimulant ¹⁰ . Its target of action has been proposed to be the prevention of inflammation and perifollicular fibrosis ¹¹ . Some degree of efficacy of 2,4-diamino-pyrimidine-3-oxide has been claimed in the prevention of seasonal alopecia ¹² . Recent approval in the United States 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 ¹³ .

Other cosmeceuticals ⁴

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 to 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. There are numerous cosmeceutical eye creams that 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 forestall the signs of aging and generally contains wheat germ and corn oil, squalene and carrot extract. Eye firming fluid has aosain, an algae extract from seaweed that helps the skin to maintain elasticity.

Regulatory aspects:

The claims made about drugs are subject to high scrutiny by the Food and Drug Administration (FDA) review and approval process, but cosmetics are not subject to mandatory FDA review. Much confusion exist regarding the status of ‘cosmeceuticals.’ Although there is no legal class called cosmeceuticals, this term has found application and recognition to designate the products at the borderline between cosmetics and pharmaceuticals ¹⁴ . Cosmeceuticals are not subject to FDA review and the Federal Food, Drug and Cosmetic Act do not recognize the term itself. It is also often difficult for consumers to determine whether ‘claims’ about the actions or efficacies of cosmeceuticals are in fact valid unless the product has been approved by the FDA or quivalent agency. Some experts are calling for increased regulation of cosmeceuticals that would require only proof of safety, which is not mandatory for cosmetics. Some countries have the classes of products that fall between the two categories of cosmetics and drugs: for example, Japan has ‘Quasi-drugs’; Thailand has ‘controlled cosmetics’ and Hong Kong has ‘cosmetic-type drugs ⁸ .’ The regulations of cosmeceuticals have not been harmonized between the USA , uropean, Asian and other countries.

Conclusion:

The concept of cosmeceuticals is spreading its wings rapidly all over the world and cosmetics are no longer only restricted to beauty care products.  Pharmaceuticals are making rooms into the cosmetic world at a great pace and resulting in the genesis of  “ Cosmeceuticals ” which not only contain the cosmetic ingredients but also contain certain pharmaceutically active ingredients. These ingredients play vital and significant role in exerting their effects to the user, which are not apparent and prominent by nature but may prove crucial or hazardous during and after their use. Every cosmetic product should be supplemented with the leaflets and inserts bearing the detailed information about the nature and effects of its ingredients particularly those of pharmaceutical significance.

The need of the hour is to identify, formulate and implicate the strict regulatory controls with respect to cosmeceuticals as the same are easily available as over the counter (OTC) products and easily accessible to the users. Though it may be not be a matter of much importance from users’ point of view, yet it should be a matter of great concern for the people engaged in the manufacturing and R&D activities of cosmetic products.

In nutshell, it can be said that the present scenario offers ample opportunities for pharmaceutical arena to exploit the cosmetic world but one should not forget that the ultimate target is a living human being who has got all rights to get information concerned with his safety and health. 

References:

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5. Muhammed Majeed and Lakshmi Prakash, Cosmeceuticals: A Revolution in the making , Sabinsa Corporation, USA .

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8. Trüeb RM. The value of hair cosmetics and pharmaceuticals. Dermatology 2001; 202:275-82.

9. Shapiro J, Maddin S. Medicated Shampoos. Clin Dermatol 1996; 14:123-8.

10. Mahé YF, Buan B, Bernard BA. A Minoxidil-related compound lacking a C6 substitution still exhibits strong anti-lysyl hydroxylase activity in vitro . Skin Pharmacol 1996; 9:177-83.

11. Jaworsky C, Kligman AM, Murphy GF. Characterization of inflammatory infiltrates in male pattern alopecia: implications for pathogenesis. Br J Dermatol 1992; 127:239-46.

12. Courtois M, Loussouarn G, Hourseau C, Grollier JF. Periodicity in the growth and shedding of hair. Br J Dermatol 1996; 134:47-54.

13. Sawaya ME. Novel agents for the treatment of alopecia. Semin Cutan Med Surg 1998; 17:276-83.

14. Hammes C. Cosmeceuticals: The cosmetic- drug borderline. In: Hori W, editor.Drug discovery approaches for developing cosmeceuticals: advanced skin care and cosmetic products. Southborough: IBC Library Series; 1997.

Table-1: List of Pharmaceutical Ingredients commonly Incorporated in Cosmetics

About Authors:

Kamal Dua *

Workign as a Lecturer, Department of Pharmaceutics, DJCOP,Niwari Road Modinagar and having more than three years of professional experience

Dr.U.V.Singh Sara
Workign as a Director and Head, Department of Pharmaceutics, DJCOP,Niwari Road Modinagar and having more than thirteen years of professional experience

Vijay Kumar Sharma

Workign as a Asst.Professor, Department of Pharmaceutical Chemistry, DJCOP,Niwari Road Modinagar and having more than ten years of professional experience.

Prasad Tandale

Narsee MonjeeInstitute of Management & Higher Studies, Mumbai-400 056.