Cosmeceuticals

March 19, 2024

Prelude

Albert Kligman coined the word "cosmeceuticals" in 1984 to describe products with both medicinal and cosmetic effects. One of the most promising, yet difficult, therapeutic alternatives that doctors may provide their patients is cosmetics. They represent the area of the skin care market with the highest growth, and some topical Treatments with cosmetics for issues like wrinkles, hyperpigmentation, and photoaging have Pharmaceuticals and cosmetics together are referred to as cosmeceuticals. Cosmetics with physiologically active components that claim to have therapeutic or drug-like effects are known as cosmeceuticals. In addition to being used to nourish and enhance the appearance of the skin, cosmetics have also been shown to be successful in treating a range of dermatological issues. Cosmeceuticals enhance attractiveness by supplying the nutrients required for skin health.

Products classified as "cosmeceuticals" fall between cosmetics and pharmaceuticals and are designed to improve the health and appearance of skin. Cosmeceuticals, which make up a growing portion of the skin care market, are made of many different types of ingredients. It is critical that doctors recognize these agents and comprehend their advantages, restrictions, and potential drawbacks given the increased interest that patients are showing in these medications and the compelling claims made by the producers.

Cosmeceuticals are cosmetic products that claim to have medicinal or drug-like properties and contain physiologically active components. A component having therapeutic qualities, cosmeceuticals exhibit positive topical effects and offer defense against age-related skin disorders. Albert M. Kligman popularized the term "cosmeceuticals" in the late 1970s. It bridges the gap between pharmaceuticals and personal care products by incorporating cosmetic actives with therapeutic, illness-fighting, or healing qualities. Cosmeceuticals are applied topically, just like cosmetics, but they contain substances that affect the skin's biological function.

Cosmeceuticals enhance attractiveness by supplying the nutrients required for skin health. Typically, cosmetics promise to reduce wrinkles and enhance skin tone, texture, and shine. Within the natural personal care business, the fastest-growing segment is called cosmetics. Customers are constantly concerned about looking young, and as the median age of the world's population rises, this market is expanding too. The Food and Drug Administration (FDA) of the United States states that products may be either drugs or cosmetics, or a combination of the two, although the phrase "cosmeceuticals" is meaningless in legal terms.

Therefore, the Federal Food, Drug, and Cosmetic Act does not accept the term "cosmeceuticals." While safety testing is required for cosmetics and skincare products, it is not required to assess whether or not beneficial substances genuinely meet manufacturer claims. In general, vitamins, herbs, different oils, and botanical extracts can be included in cosmetics, but the producer is not allowed to state that these items have therapeutic or drug-like properties or that they penetrate the skin's outer layers.

"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" is how the Food, Drug, and Cosmetic Act defines cosmetics. Products covered by this category include moisturizers for the skin. Cosmetic products such as deodorants, shampoos, permanent waves, lipsticks, nail polishes, eye and facial makeup preparations, and any material meant to be used as an ingredient in a cosmetic product. These Cosmeceuticals, which act as a link between medications and personal care products, were created especially for their therapeutic and cosmetic properties.

When it comes to the history of cosmetics, the Egyptians are credited with using them for the first time around 4000 BC. The Hebrews, Babylonians, and Sumerians of antiquity all used makeup. In other instances, from the second to the nineteenth centuries, the European cosmetic known as Ceruse was in use. Large and small companies involved in biotechnology, pharmaceuticals, natural products, and cosmetics are always developing new active ingredients for cosmetics; at the same time, the cosmetic industry is developing novel active compounds at a faster pace thanks to advancements in the field of skin biology and pharmacology. Effectiveness, safety, formulation stability, patent protection, novelty, skin metabolism, and low manufacturing costs are desirable qualities of cosmetic agents.

While cosmeceuticals are already well-recognized tools in dermatological procedures for treating photo aging, their broader use to wound healing is still unexplored. The complicated process of wound healing can lead to a variety of undesirable outcomes, including keloids, dehiscence, hypertrophic scars, and ulcers.[8] Large and small companies involved in pharmaceuticals, biotechnology, natural products, and cosmetics are continuously developing cosmeceutically active ingredients, and advances in the field and knowledge of skin cream containing a hormone like estrogen result in a fresh appearance with a rejuvenating effect.

The global cosmetics market size was valued at USD 262.21 billion in 2022 and is expected to expand at a compound annual growth rate (CAGR) of 4.2% from 2023 to 2030.

A patent was granted to Kuno and Matsumoto for an external skin agent that included an extract made from olive plants as a skin-beautifying ingredient, namely as an anti-aging and/or skin-whitening ingredient.

SKIN CARE COSMECEUTICALS

Products for skin care and makeup are a part of daily grooming. For optimal health, the skin must be preserved and protected. The largest organ in the body, our skin serves to protect and divide the inside and external environments. The fundamental components of skin, including DNA, collagen, and cell membranes, are cumulatively harmed by environmental factors, air pollution, sun exposure, and the aging process. The purpose of cosmetics and beauty products is to cover up and enhance the appearance of the skin, not to alter or heal it.

Because they contain certain functional chemicals, cosmetic products with medicinal or drug-like properties, known as "cosmeceuticals," have the ability to influence the biological functioning of skin. Skincare products are available that do more than just color and embellish the skin. By preventing the damaging effects of free radicals and promoting collagen formation, these products enhance the appearance and functionality of the skin while also preserving the integrity of the keratin structure. The well-known OLAY vitamin range contains zinc, copper, pycnogenol, vitamins A, C, D, E, and selenium in addition to lycopene.

When aged skin is treated with a lotion that contains a hormone like estrogen, the skin looks younger and more refreshed.An external skin care product containing an extract made from olive plants was patented by Kuno and Matsumoto as a skin-beautifying ingredient, namely as an anti-aging and/or skin-whitening ingredient.  For cosmetic purposes, a dry emollient formulation comprising monounsaturated Jojoba esters was utilized. Martin used a genus Chrysanthemum plant extract in a cosmetic formula to promote skin and/or hair pigmentation. To repair the deteriorating or aging skin, new cosmetic creams or gels containing active chemicals and water-soluble barrier disruption agents as vitamin A palmitate have been developed.

Sunscreen Agents

Skin cancer and early wrinkles can be avoided by using sunscreen products and reducing sun exposure. Sunscreen ingredients are applied to stop sunburns. Sunscreen agents come in two varieties: chemical and physical. Whereas physical sunscreen agents reflect, scatter, absorb, or block the sun's rays, chemical sunscreen agents shield the skin from UV and visible light radiation. Sunscreen ingredients can frequently consist of many ingredients.

Examples of ingredients included in products are those that offer protection against UVA (ultraviolet A) sun rays and UVB (ultraviolet B) sun rays, which are more likely to result in sunburns than UVA rays. Protection against UVA and UVB radiation should ideally be included in the covering. When comparing sunscreen-protected skin to unprotected skin, the sun protection factor (SPF) listed on the label of these products indicates the lowest quantity of UVB sunlight required to cause redness. Higher SPF sunscreen lotions offer increased solar protection.

The U.S. Department of Health has suggested the following sunscreen ingredients: • Digalloyl trioleate; Benzyl salicylate and Benzyl cinnamate (2% each); Cycloform (isobutyl p-amino benzoate); Propylene glycol p-amino benzoate; Monoglyceryl p-amino benzoate);

In addition to this, chemical sunscreens that are mostly based on anthraline derivatives, cinnamates, different salicylates and benzophenones, dibenzoylmethanes, octocrylene, homosalate, and para-aminobenzoic acid are commonly used as sunblocking agents. Metal-containing substances, such as bismuth, iron, zinc, and titanium, are direct physical blockers. Submicron titanium dioxide and zinc oxide powder particles transmit visible light while keeping their UV-blocking characteristics, making the sunblock invisible on the skin. Both zinc oxide and titanium dioxide are highly reflecting white powders. Benzophenone-8, NeoHeliopan MA and BB, Parsol MCX and HS, Escalol 557, 587, and 597 are other commercially marketed sunscreens.

Moisturizing Agents

The stratum corneum, the skin's principal barrier, has the dual function of keeping the inside and outside of the body. This barrier is abundant in ceramides, free fatty acids, and cholesterol. To keep the skin's suppleness, numerous greasy preparations have been employed (Mineral oil, Lanolin, cyclomethicone, etc.). Dehydration results from the stratum corneum's water rapidly evaporating.

Skin hydration can be prevented by utilizing moisturizers that give the skin elasticity. The essential components of the moisturizing formulations are humectants. Moreover, humectants aid in keeping formulations from drying out. A thin layer of humectants is created on the skin when moisturizers are applied, helping the skin look nicer and retain moisture. Formulations containing bio-imimetic lipids aid in the restoration of injured skin to its normal state. Applying water to the skin for an extended length of time can result in the excretion of cytokines. This could also result in the induction of inflammation, vasodilatation, and edema. 

Moisturizers can even change the physiology of the skin by moisturizing the stratum corneum. Moisturizers that include ceramides are highly sought-after because they have the same lipid composition as human skin. Ceramides19–27 are the names of the nine distinct ceramide types found in the stratum corneum.They make up forty to fifty percent of the lipids in this topmost layer.

These ingredients have been shown to be effective in treating eczema and can also be used to treat dry skin. It has been discovered that ceramide formulations including fluocinolide decrease eczema5. In addition to these, vitamins A and E, soy extract, and black cohosh aid in enhancing the skin's natural moisture balance. Another promising moisturizing agent is a complex blend of hyaluronic acid and arevival complex, which contains green tea leaf extract and glutathione.

Skin Lightening Agents

Hyperpigmentation, which results from an excess of melanin in either the dermis or the epidermis, is the darkening of the skin's color intensity. Melanocytosis (an increase in the number of melanocytes) and melanosis (an increase in the amount of melanin) are two pathophysiologic processes that could be causing this shift. The finest results from skinlightening products come from melanocytosis or melanosis that is limited to the epidermis.

Those with Fitzpatrick skin types III and darker may also seek therapy for pigmentary changes that occur around the eyes, in the intertriginous areas, after dermatitis, or with acne and trauma. Patients with Fitzpatrick skin types IIII have advantages over type IV, such as type I-III benefiting from local pigment lightening for the treatment of hormonally induced melasma and postinflammatory hyper pigmentation caused by acne and trauma.

The conventional dermatological treatment for skin whitening is hydroquinone; however, due to concerns about its toxicity, other agents such retinoid, mequinol, azelaic acid, arbutin, kojic acid, aleosin, licorice extract, ascorbic acid, soy proteins, and N-acetyl glucosamine are being used instead.

Boswellic acids

The source of it is Boswellia serrata. The primary purpose is to inhibit lipoxygenase, one of the enzymes that causes inflammation, and skin damage.

Tetrahydrocurcuminoids

It is made of carnosic acid, cosmarinic acid, ursolic acid, and white (colorless) curcuminoids of turmeric (Curcuma longa) extracted from rosemary. The other chemicals that are utilized to facilitate tissue damage and restore the healthy status of skin are antioxidants like rosemarimusofficinalis.

Retinoid

Its application for various cutaneous problems and as an antiaging chemical have been the focus of a significant amount of research. Two primary roles of vitamin A and its derivatives are as antioxidants and as activators of particular genes and proteins. Underlying the cosmetic improvements are structural modifications such as the enhancement of mitogenesis, the deposition of new collagen, the formation of new capillaries, and the repair of epidermal atrophy. Melanin-containing keratinocytes shed more readily as a result of this increased mitogenesis, which causes bleaching and eventual depigmentation. Topical tretinoin has been shown in numerous studies and studies to enhance the appearance of aged and photodamaged skin by smoothing down the surface, minimizing wrinkles, lowering laxity, and bleaching hyperpigmented areas.

Hydroxy acids

Acids categorized based on their molecular structure into betahydroxy acids (BHAs) and alpha hydroxy acids (AHAs). Many are called fruit acids and are obtained from natural sources. Glycolic acid, lactic acid, citric acid, mandelic acid, malic acid, and tartaric acid are among the several AHAs. It has been demonstrated that AHAs reduce aging indicators. The skin seems more homogeneous and smoother.Aromatic chemicals are BHAs. The standard BHA is salicylic acid, which has dermolytic qualities and aids in a number of xerotic and ichthyotic conditions.

Antioxidants

Apart from external stressors such as ultraviolet radiation, medications, air pollutants, heat, and/or cold, the skin also needs to adapt to internal mitogens, primarily reactive oxygen species (ROS) and other free radicals. During physiological cellular metabolism, these species are continuously generated. The skin has an antioxidant system in place to combat the destructive effects of reactive oxygen species (ROS). This system works to keep a balance between pro-oxidants, or damaging agents, and antioxidants, or protective agents, with the antioxidants interfering at different stages of the protective process.Below is a list of a few antioxidants.

 Vitamin C

The hydroxylation of proline, lysine, and collagen requires vitamin C. Vitamin C helps to repair and restore the abnormalities brought on by photodamage.Some of the effects of photoaging on skin can be mitigated by using vitamin C to induce collagen repair. However, due to its high acidity and susceptibility to heat and light degradation, vitamin C poses some issues when used in a multipurpose skin care formulation. A synthetic collagen fraction that was just introduced provides increased efficacy, stability, and compatibility.

Vitamin E

The main lipophilic antioxidant in plasma, membranes, and tissues is vitamin E (alpha-tocopherol).Thirty naturally occurring compounds (four tocopherols and four tocotrienols) that are all known to have vitamin E activity are collectively referred to as vitamin E. Its primary function is thought to be scavenging lipid peroxyl radicals to stop the chain from propagating in lipid peroxidation, hence preventing the breakdown of the cell membrane.It has been demonstrated that topical application of vitamin E prior to UV irradiation reduces the development of DNA adducts, sunburned cells, erythema, edema, and immunological suppression from sunshine.

Panthenol

Diphenol Water-soluble humectants like panthenol, the alcohol analog of vitamin B-5, are frequently found in a variety of commercial skin care products, lipsticks, lotions, and hair preparations. When there is oxygen and light present, it is stable; but, when acids, bases, and high temperatures are present, it becomes unstable. In the skin, pantenol is transformed into topantothenic acid, a crucial oncoenzyme component. a necessary component of healthy cellular metabolism.

Lipoic acid

One special defense against free radicals is lipoic acid. It dissolves in water and fat. Dihydrofolic acid, another antioxidant, is produced when lipoic acid has passed through the cell membrane. In addition, alpha lipoic acid recycles other important antioxidants including vitamin C.

Niacinamide

Niacinamide is inexpensive to produce and stable in the presence of acid, oxygen, and high temperatures. The majority of its recognized impacts stem from heightened epidermal turnover and exfoliation. It has been discovered that topical kinetin and niacinamide have a synergistic antiaging cutaneous effect on individuals in the People's Republic of China.

Dimethylaminoethanol

Ethylene dimethylamine Dimethylaminoethanol (DMAE)-containing topical formulations have been hailed for its capacity to increase skin firmness and elevate drooping skin. DMAE may reduce the cross-linking of proteins that happens with aging, most likely by scavenging free radicals. Spinal cordsSpecies known as "free radical spin traps" react with reactive free radicals to create relatively stable, non-reactive free radicals, preventing the free radicals from causing damage to cell components. TEMPONE-H (1-hydroxy-2,2,6,6tetramethyl-4-oxo-piperidine) · DEPMPO (5-diethoxyphosphoryl-5methyl-1-pyrroline-N-oxide) · DMPO (5,5-dimethyl-1-pyrroline-N oxide).

Melatonin

The pineal gland secretes the hormone melatonin.Melatonin's protective effects have been attributed to its capacity to scavenge free radicals and enhance the activities of antioxidant enzymes. It has been demonstrated to reduce erythema brought on by UV exposure.

Catalase

The enzyme catalase, which is found in practically every human cell, catalyzes the conversion of hydrogen peroxide to oxygen and water. Excessive concentrations of this enzyme in the skin can provide antioxidative properties.

Glutathione

The tripeptide glutathione is made up of glycine, cysteine, and glutamic acid. Every living tissue in an animal contains it. Glutathione is an essential antioxidant, and UV radiation causes a substantial drop in its levels.

Superoxide dismutase

The enzyme superoxide dismutase (SOD) breaks down superoxide, a highly reactive oxygen species. Since SOD is a big molecule, it has trouble getting deeply into the skin. Theoretically, SOD functions as a potent antioxidant and reduces UV erythema and damage once it reaches the lower epidermis and dermis.

Polyphenols

Antioxidants include polyphenolic chemicals, sometimes referred to as epicatechins, such as flavonols, thioflavins, catechins, and thearubigins. When these substances were evaluated on UV-stressed human keratinocyte cells, they demonstrated strong antioxidant capabilities.

Cysteine

According to a number of recent studies, cysteine derivatives can offer protection against the harmful effects of UV radiation. N-acetylcysteine (NAC) in particular has been demonstrated to be a useful defense against UV-B-induced immunosuppression.

Allantoin

Allantoin facilitates the growth of new cells, which helps the body repair. Because of its skin-protecting properties, allantoin has long been known to improve the desirability and efficacy of cosmetic creams and lotions.Shampoos, lipsticks, shaving creams, suntanning lotions, bath foams, hairgels, baby powders, and a variety of aerosol preparations have all contained allantoin.Allantoin has been referred to as a chemical debrider, an epithelization activator, and a cell proliferant. It is supposed to remove necrotic tissue and speed up the formation of new, healthy tissue.

Furfuryladenine

Furfuryladenine, also known as Kinerase, is a naturally occurring plant growth factor that slows down plant aging. Untreated leaves become brown, but cutleaves immersed in a solution containing furfuryladenineremain green. It is advertised as the organic advancement of antiaging therapy, working to halt and reverse changes that naturally transpire during the aging process of cells in human skin cells, much like it does in plants.

Uric acid

Uric acid was formerly mostly thought of as the byproduct of purine metabolism. Uric acid has gained more attention as a significant biological antioxidant in recent years.

Carnosine

A physiological dipeptide called carnosine (beta-alanyl-L-histidine) has the ability to revitalize aged human fibroblasts. It has been demonstrated that carnosine has antioxidant, free radical-scavenging, and metal ionscavenging properties.

Depigmenting Agent

Melanin accumulation in the dermis, epidermis, or both can lead to hyperpigmentation.Melanocytosis (an increase in the number of melanocytes) and melanosis (an increase in the amount of melanin) are the two pathophysiologic processes that account for this pigmentary shift. When melanosis or melanocytosis is limited to the epidermis, depigmenting treatments function well. Depigmenting agents fall into a number of categories.

Hair Cosmeceuticals

Unlike all other land mammals, humans have direct control over the appearance of their hair, which is one of their physical characteristics. The length, color, and style of hair can all be changed to suit one's desired appearance. Hair color, style, and maintenance have a big impact on how people feel about their bodies and how they look. Henna hair coloring and clay hair setting were two of the first hair beautification techniques used in ancient Egypt. Numerous ointments and tonics were prescribed in ancient Greece and Rome for the treatment of scalp ailments as well as for hair beauty.

The first person to distinguish between medical treatments meant to cure illnesses and cosmetics meant to enhance appearance was Henry de Mondeville. However, the distinction between pharmaceuticals and cosmetics has grown increasingly difficult in the modern day due to the emergence of "cosmeceuticals," or cosmetics containing physiologically active chemicals. The most common type of cosmetic hair care is shampooing. Although the original purpose of shampoos was to clean the hair and scalp, modern formulations are tailored to address variations in hair quality, hair care habits, and particular issues like treating oily hair, dandruff, and androgenic alopecia, which is related to the superficial condition of the scalp.

Topical application of hair and scalp cosmetics is used to treat hair. They cannot be used therapeutically, but they must be safe for the skin, hair, and mucous membranes. They also shouldn't have any harmful effects, either local or general, when being used as directed. A shampoo mixture created by Mausner37 cleans the hair and scalp without endangering the delicate biological balance of the scalp and hair. A hair-care cosmetic composition that contains zinc pyrithione in N-acyl ethylenediamine triacetate solution and/or iodopropynyl butyl carbamate has been patented. It also includes a suitable carrier and a non-allergic dry extract of yarrow (Achillea millefolium L.), which is made by oxidizing a water-alcohol solution produced by oxidizing an extract of yarrow flower tips in a water-alcohol solution. The extract, which is based on yarrow extract and contains less than 0.5% by weight of polyphenolic derivatives, is used to cure hair, especially oily hair.34 Buck36 has patented a procedure that involves using liquor carbonic detergent topically to treat androgenic alopecia.

Stimulants for hair development, conditioning agents, and components for particular care are all included in hair cosmeceuticals. The goals of conditioning compounds are to improve disentangling ability, minimize flyaway, and impart softness and gloss. Many components can be employed, but the most common ones are hydrolyzed proteins, cationic polymers, quaternized cationic derivatives, and silicons.  Ingredients in special care products are designed to address certain issues with the superficial scalp. These shampoos are made up of one or more key components that have been chosen for their therapeutic efficacy in treating these ailments. As a result, the majority of the active components in antidandruff products now are antifungal drugs: zinc pyrithione, octopirox, and ketoconazole.

Because of the brief contact duration and water dilution, hair growth boosters are not predicted to have any effect on hair growth. 2,4-Diamino-pyrimidine-3oxide is a cosmetic chemical that bears the potential to function as a topical stimulant for hair growth, similar to minoxidil. It has been suggested that it works by preventing perifollicular fibrosis and inflammation.It has been suggested that 2, 4-diamino-pyrimidine-3-oxide is somewhat effective at preventing seasonal alopecia. The United States has approved Propecia and Rogaine Extra Strength (Minoxidil) 5%, two new drugs suggested for men to encourage scalp hair growth. These approvals have expanded the range of treatments available to doctors treating androgenetic alopecia.

Other Cosmeceuticals

There is almost no subcutaneous fat and very few oil glands in the skin under the eyes. In order to renew and heal itself and lessen the appearance of premature aging, this fragile skin needs protection as well as an abundance of moisture. The skin gets rougher, dryer, and thinner as we age. This illness is made worse by prolonged exposure to the outdoors and contamination from the environment. Numerous topical skin-soothing solutions interfere with this process; however, products intended for this area must be extra gentle and specifically made with substances that interact with the cells beneath the skin's surface to operate from the inside out without causing irritation to the eyes.

Many cosmeceutical eye creams provide the skin with healthy nutrients and natural emollients. The other useful components are a-bisabolol, an active component of chamomile that soothes sensitive skin, cucumber, calendula, butcher's broom, chamomile, and vitamin E. Antioxidants include green tea, tiare flower, and Ginkgo biloba. Yeast is a major component of the eye lifting moisture cream, which helps to fill out wrinkles and relieves puffiness and irritation while shielding the skin from further damage.

Squalene, carrot extract, wheat germ and corn oil, and other ingredients are typically found in eye wrinkle creams, which help prevent the appearance of aging. Aosain, an algal extract from seaweed found in eye firming fluid, aids in the preservation of the skin's elasticity. Lawlor created dental care compositions that are helpful for applying a thick layer to the surfaces of the oral cavity, offering therapeutic, preventive, and cosmetic benefits.

Regulatory Aspects

The Food and Drug Administration (FDA) reviews and approves claims made about medications under strict scrutiny, although FDA clearance is not required for cosmetics. There's a lot of misunderstanding about the status of "cosmeceuticals." Despite the lack of a formal legal class, the term "cosmeceuticals" has gained legitimacy and application in order to refer to products that fall within the categories of cosmetics and pharmaceuticals. The FDA does not approve cosmeticals, and the term itself is not recognized by the Federal Food, Drug, and Cosmetic Act.

Consumers frequently find it challenging to verify the veracity of "claims" made regarding the functions or efficacies of cosmetics unless the product has received FDA or other government approval. Increased regulation of cosmetics, which would merely need to provide proof of safety—something that is not required for cosmetics—is being advocated by certain specialists. Certain nations have product classes that lie in between the drug and cosmetic categories: Japan has "quasi-drugs," Thailand has "controlled cosmetics," and Hong Kong has "cosmetic-type drugs"44.The laws governing cosmetics in the United States, Europe, Asia, and other nations are not uniform.

Future prospects

A tiny amount of cosmeceutical agents might be added to cosmetic formulations that don't need to follow medical standards. This would increase the production of cosmeceuticals, which could aid in improving the growth of body mass, nails, and skin. 

Government regulatory bodies will face further difficulties when more compounds with real biological activity are developed and examined. In summary, cosmetics enhance internal beauty by improving health-related functions in addition to their external beauty.

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