Cosmeceuticals

Lecture 41
P J Mahajan

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Introduction, Definition and
difference from cosmetics
 Cosmeceuticals are cosmetic products with biologically active
ingredients purporting to have medical or drug‐like benefits.
 A cosmeceutical ingredient have medicinal properties that
manifests beneficial topical actions and provides protection
against degenerative skin conditions.
 The word "Cosmeceuticals" was popularized by Albert M. Kligman
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.
 Cosmeceutical ingredient formulations are effective than regular
skin care products. For example, vitamin C is a known
antioxidant, and when added to a lotion or cream, it is
considered a cosmeceutical. Same goes for products with
ingredients like retinol or peptides.

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 According to the United States Food and Drug
Administration (FDA), the Food, Drugs, and Cosmetics
Act; a product can be a drug, a cosmetic, or a
combination of both, but the term “Cosmeceuticals”
has no meaning under the law”. So the term
Cosmeceuticals is not recognized by the Federal
Food, Drug, and Cosmetic Act.

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 All cosmeceuticals claim to contain functional
ingredients with either therapeutic, disease-fighting or
healing properties.
 It provides external aesthetic benefits; the additional
medicinal properties of cosmeceuticals are based on
molecular structure, biological function relationships,
and modes of action related to healing, anti-aging,
free radical rampage reduction, dead epidermal cell
exfoliation, and so on.
 In cosmeceuticals the importantance to know the
interaction between skin and cosmeceuticals which
could even be influenced by environmental fact.

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 Cosmeceuticals improve the appearance, but they do so by
delivering nutrients necessary for healthy skin and treats
medically on impaired skin cells.

 Desirable features of Cosmeceuticals agents are efficacy,

safety, formulation stability, technology transfer, creulty free
standards, computer aided designing’s, novelty, and patent
protection, regulatory bodies, metabolism within skin and
inexpensive manufacture.
 Cosmeceuticals contains naturally derived ingredients and
synthetics too, but all contains functional ingredients with their
therapeutic, disesase-flighting and healing properties.

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 Cosmetics vs Cosmeceuticals

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 Cosmetics vs Cosmeceuticals

 Cosmetics are '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.‘

 Cosmeceuticals are cosmetic products with

biologically active ingredients purporting to have
medical or drug‐like benefits.

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 Cosmetics and skin care products are the part of
everyday grooming they protect and preserve the skin
and maintain good health. Use of cosmetics or beauty
products will not cause the skin to change or heal; these
products are just meant to cover and beautify.
 But a cosmeceutical product will have active ingredients
which acts much lively to protect, heal and prevent
damage to the skin. Cosmeceuticals are aimed at
modifying specific problems relating to the deeper or
superficial surfaces

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 Cosmetics normally do not have active ingredients.
Cosmetics products are “self-diagnose” and choose a skin
care product that is easily available from a drug or
department store.
 Cosmeceuticals To be classed as a cosmeceuticals, active
ingredients must be at the scientifically proven levels of
concentrations that have a positive effect on the skin.

 Cosmetic products are widely accessible, available from

supermarkets, department stores and salons.
 Cosmeceuticals are only available from Medi Spas,
Paramedical skin clinics, Dermatologists, Cosmetic and
prescribed by a skin professional. By having a profession skin
diagnosis your will be prescribed the correct skincare that
will lead to amazing results.

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 Cosmetics cannot penetrate the epidermis to access the
deeper layers of the skin. So, while cosmetics may refresh your
complexion for a few hours, they cannot create structural
changes or deliver long-term results. A Cosmetic will
effectively maintain your skin by providing somewhat
temporary results.
 Cosmeceuticals when applied to the skin the active
ingredients are able to reach the deeper dermal layers of skin
to allow them to work on the skin and be able to make
noticeable changes in the skin. These changes can include
reducing acne severity, re-hydrating the skin, diminishing the
appearance of aging and sun damage, and promoting a
healthy, radiant complexion.

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History of Cosmeceuticals

 The term “cosmeceutical” was created in the 1990’s

and is used by the cosmetic professionals to refer to a
product that combines medicinal or pharmaceutical
properties with cosmetic.
 Many dermatologists believe the term
“cosmeceutical” was first coined by Albert M.
Kligman, MD, PhD, a dermatologist also known for
discovering the benefits to our skin of retinoids.
 The US Food and Drug Administration does not
recognize the term.

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 History of Cosmeceuticals

 Additionally, the FDA states that: "Food, Drug and Cosmetic

Act defines drugs as those products that cure, treat,
mitigate or prevent disease or that affect the structure or
function of the human body. While drugs are subject to an
intensive review and approval process by FDA, cosmetics
are not approved by FDA prior to sale. If a product has
drug properties, it must be approved as a drug."

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 History of Cosmeceuticals

 A cosmeceutical is legally not a drug, though the ingredients are

believed to be bio-active.
 In recent years, more cosmeceuticals are being evaluated for
efficacy and tolerance in scientific studies.
 When studies are not available on a cosmeceutical, we may
measure its value based on peer reviews, and previously studied
ingredients.
 Cosmeceuticals may fall closer to a drug or pharmaceutical or
closer to a cosmetic depending on their ingredients.
 A Roman physician named Galen invented the first cold cream,
an emulsion of olive oil and beeswax.
 He advised using it for “keeping the skin healthy and well-
groomed.”

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 Retinoids
 Vitamin A is the first vitamin approved by the Food and Drug
Administration as an anti-wrinkle agent that changes appearance
of the skin surface and has anti-aging effects.
 Vitamin A is in a group of fat-soluble substances and belongs to
the category of retinoids.
 Apart from retinol, that group includes structurally related
substances with the biological properties of retinol.
 Vitamin A and its derivatives are among the most effective
substances slowing the aging process.
 Retinoids regulate the cell apoptosis, differentiation and
proliferation and regulate epithelial cell growth.
 Anti-wrinkle properties of retinoids promote keratinocytes
proliferation, strengthen the protective function of the epidermis,
restrain transepidermal water loss, protect collagen against
degradation and inhibit metalloproteinases activity.
 Retinoid activity is related to high affinity for nuclear receptors:
RAR – retinoid acid receptors and RXR – retinoid X receptors.

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 Retinoids

 Source
• A vitamin A derivative

 Function:
• Antiaging compound
• Antioxidants
• Correction of epidermal atrophy,
• Deposition of new collagen,
• Generation of new vessels,
• Enhancement of mitogenesis, which 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 hyper pigmented spots
• Vitamin A and its derivatives have 2 main functions: they act as antioxidants, and they activate specific
genes and proteins.

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 Use:
 Anti-wrinkle treatments, improvement of texture,
dyspigmentation, dryness, and fine lines
 Retinoids are used in the treatment of many diverse
diseases and are effective in the treatment of a number
of dermatological conditions such as inflammatory skin
disorders, skin cancers, disorders of increased cell
turnover (e.g. psoriasis), photoaging, and skin wrinkles.
 Common skin conditions treated by retinoids
include acne and psoriasis.
 Isotretinoin is not only considered the only known possible
cure of acne in some patients,

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 Based on the molecular structure and properties, retinoids
can be divided into three generations: –
 First generation – natural retinoids, monoaromatic
compounds obtained by modifying polar groups at the
end and side chain of the polyene vitamin that do not
act selectively – retinol (vitamin A) and its metabolites –
retinal, tretinoin, isotretinoin,
 Second generation – monoaromatic retinoids, synthetic
compounds in which the cyclohexene ring is replaced by
a benzene ring; synthetic analogues of vitamin A
(etretinate, acitretin)
 Third generation – polyaromatic retinoids formed as a
result of cyclization of polyene side chain and
characterized by selective activity towards receptor
(arotinoid, adapalene, tazarotene)

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 Hydroxyl acids
 Hydroxy acids are organic carboxylic acids classified into alpha hydroxy acids (AHAs) and
betahydroxy 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 the following: glycolic acid, lactic acid, citricacid, 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, a combination of AHAs and BHAs, have appeared as
ingredients in these skin care products. While both AHAs and BHAs act as
exfoliants, it has been claimed that BHAs are effective in reducing the
appearance of fine lines and wrinkles, and improving overall skin texture, without
the occasional irritation associated with the use of AHAs.

 Salicylic acid is the reference BHA; it has dermolytic properties and helps in various xerotic and
ichthyotic disorders.
 Other BHAs include 2-hydroxy-5-octanoyl benzoic acid, also knownas betalipohydroxyacid (B-
LHA), and tropic acid.
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 Studies show that AHAs may increase sensitivity to UV radiation and that sunscreen application
may be advisable when these products are used.
 Salicylic acid is widely used in cosmetic formulations
(concentration 2%–4%) and also therapeutically as a
keratolytic (peeling) agent to treat skin conditions, such
as calluses, keratoses, acne, and photoaging.
 It is applied in various concentrations, vehicles, and pHs,
depending on the numbers of lesions. Several studies
have found that topically applied SA is photoprotective.
 The antibacterial action of SA has been known for many
decades. SA acts at the level of transcription to
downregulate the production of fibrinogen, fibronectin,
and α-hemolysin virulence factors necessary for bacterial
replication in host tissues. Whether SA affects bacterial
growth in acne was not reported

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Hydroxyl acids

 Source:
• Organic carboxylic acids classified into alpha hydroxy
acids (AHAs) and betahydroxy acids (BHAs) according
to their molecular structure.
 Function:
• AHAs: glycolic acid, lactic acid, citric acid, mandelic
acid, malic acid, and tartaric acid
• Decrease the signs of aging
• BHAs: aromatic compounds. Eg. Salicylic acid, it has
dermolytic properties and helps in various xerotic and
ichthyotic disorders.

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 Use:
 βLHA was shown to have a good safety profile with
lower irritation when compared to glycolic acid
 βLHA also showed activity in reducing melanosome
clustering and epidermal pigmentation. Contrary to
αHAs, βLHA increased the skin’s resistance to UV-
induced damage.
 βLHA has antibacterial effects, which are ideal for the
treatment of acne.
 Have antimicrobial, anti-inflammatory, antifungal, and
anti-comedogenic properties

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Antioxidants

 Antioxidants
 In addition to these external insults like UVradiation, drugs,
air pollutants, and heat and/or cold, theskin also has to
cope with endogenous mitogens, mostimportantly
reactive oxygen species (ROS) and other free radicals.
 These species are continuously produced during
physiological cellular
 metabolism. To counteract theharmful effects of ROS, the
skin is equipped with anantioxidant system to maintain
equilibrium between thepro-oxidants, or damaging
agents, and the antioxidants, or protective agents; these
antioxidants intervene atdifferent levels in the protective
process. Vitamin C Vitamin E Lipoic acid Niacinamide
Dimethylaminoethanol (DMAE) are some of the
antioxidants.

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 Vitamin C
 Vitamin C is necessary for the hydroxylation of
procollagen, proline, and lysine. Vitamin C improves
andnormalizes the changes caused by
photodamage.
 VitaminC has been used effectively to stimulate
collagen repair, thus diminishing some of the effects of
photoaging on skin. However, vitamin C is easily
degraded by heat and light, which along with its high
acidity, presents certain challenges for use in a
multipurpose skin careformulation.

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 Source: Fruits
 Function:
• Hydroxylation of procollagen, proline, and lysine.
• Improves and normalizes the changes caused by
photo damage
• Use:

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 Vitamin E (alpha-tocopherol) is the majorlipophilic
antioxidant in plasma, membranes, and tissues.
 The term vitamin E collectively refers to 30
naturallyoccurring molecules (4 tocopherols and 4
tocotrienols), all of which exhibit vitamin E activity.
 Its major role is generally considered to be the arrest of
chain propagationin lipid peroxidation by scavenging
lipid peroxyl radicals, hence protecting the cell
membrane from destruction.
 Vitamin E topically applied before UV irradiation has
been shown to reduce erythema, edema, sunburn
cells, immune suppression caused by sunlight, and
DNA adducts formation.

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 Description: (alpha-tocopherol) major lipophilic
antioxidant in plasma

 Function:
• Arrest of chain propagation in lipid peroxidation by
scavenging lipid peroxyl radicals, hence protecting
the cell membrane from destruction.
• Vitamin E topically applied before UV irradiation has
been shown to reduce erythema, edema, sunburn
cells, immune suppression caused by sunlight, and
DNA adducts formation.
 Use

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 Lipoic acid
 Lipoic acid is a unique free radical protector.
 It is fat and water soluble.
 Once lipoic acid crosses the cell membrane, it is broken
down into dihydrofolic acid,which is also an antioxidant.
Alpha lipoic acid alsorecycles other key antioxidants,
such as vitamin C
 Function:
 Lipoic acid crosses the cell membrane; it is broken down
into dihydrofolic acid, which is also an antioxidant.


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 Niacinamide
 Niacinamide is stable in the presence of oxygen, acid, and
high temperatures, and it is inexpensive to formulate.
 Most of its known effects are the result ofincreased
epidermal turnover and exfoliation.
 Topical kinetin and niacinamide have been found to exert
asynergistic antiaging cutaneous effect
 Function:
• Increased epidermal turnover and exfoliation
• Topical kinetin and niacin amide has a synergistic antiaging
cutaneous effect in people

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 Dimethylaminoethanol
 Topical preparations containing dimethylaminoethanol (DMAE)
have been touted for their ability to improve skin firmness and
to lift sagging skin.
 DMAE is able to diminish the cross-linking of proteins that
occurs during aging, probably acting as a free radical
scavenger.
 Spin traps Free radical are species that react with reactive free
radicals to produce fairly stable, unreactive free radicals, thus
blocking the free radicals from damaging cellular
components.

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Skin Lightening Agents

 Hyperpigmentation is the changing of color intensity

of the skin to darker hue, which is due to an increased
amount of melanin in the epidermis, the dermis, or
both.
 Standard dermatologic agent for skin lighteningis
hydroquinone but its safety is questionable, leading to
the use of alternative agents such as retinoid,
mequinol etc

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Depigmenting Agent

 Hyperpigmentation is the result of an increased

amount of melanin in the epidermis, the dermis, or
both.
 This pigmentary change can be divided into
2pathophysiologic processes: melanocytosis
(increased number of melanocytes) and melanosis
(increased amount of melanin).
 Depigmenting agents work bestwhen melanosis or
melanocytosis is restricted to the epidermis.

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 Depigmenting agents can be divided into several groups
 Phenolic compounds include the following:
 · Hydroquinone
 · Monobenzylether of hydroquinone
 · 4-Methoxyphenol
 · 4-Isopropylcatechol
 · 4-Hydroxyanisol
 · N -acetyl-4-S-cysteaminylphenol
 Nonphenolic compounds include the following:
 · Corticosteroids
 · Tretinoin
 · Azelaic acid
 · N -acetylcystein
 · L-ascorbyl-2-phosphate

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Sunscreen Agents

 Use of sunscreen agents and limiting the exposure to

sun prevents early wrinkling and skin cancer.
Sunscreen agents are used to prevent sunburns.
 There are two kinds of sunscreen agents: chemical
and physical.
 Chemical sunscreen agents protect the skin from the
sun by absorbing the ultraviolet (UV) and visible sun
rays, while physical sunscreen agents reflect, scatter,
absorb, or block the rays.

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 • Cycloform (isobutyl p‐amino benzoate) • Propylene glycol
p‐amino benzoate • Monoglyceryl p‐amino benzoate
 • Digalloyl trioleate • Benzyl salicylate and benzyl cinnamate
(2% each) are used widely.
 Besides these, chemical sunscreens mainly based on
para‐aminobenzoic acid, its derivatives, cinnamates, various
salicylates and benzophenones, dibenzoylmethanes, anthraline
derivatives,octocrylene and homosalate are frequently
employed as sunblocking agents.
 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 sun block invisible on the skin.

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 Hair cosmeceuticals
 The appearance of the hair is a feature of the body over which
humans, unlike all other land mammals, has direct control. One can
modify the length; color and style of hair according to how one wish
to appear.
 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.
 Special care ingredients are aimed at modifying specific problems
relating to the superficial scalp
 current antidandruff ingredients are virtually all-effective antifungal
agents - zinc pyrithione, octopirox, and ketoconazole

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Other Cosmeceuticals

 Eye: 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.
 The 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.
 The eye wrinkle cream helps forestall the signs of aging
and generally contains wheat germ and corn oil,
squalene and carrot extract.

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