SKIN WHITENING PRODUCTS

B Y: S O P H I A M A R I E D A PA R
INTRODUCTION

 Since times immemorial fair skin is associated with lineage of nobility, aristocracy and
wealth. Regardless of this idiosyncrasy, majority of the people have a penchant to
possess an even, unblemished skin tone.
 So man has made attempts to artificially color, bleach and in other ways alter the normal
appearance of his skin.
 This need is fulfilled by the cosmetic industry with a huge plethora of products specially
offering skin lightening and bleaching properties. These products contain special active
ingredients which lightens skin, thus giving an enhanced whiter appearance.
INTRODUCTION
 Skin lightening creams – are also known as
bleaching creams, skin whiteners, skin
brighteners or fading creams.
 These work by reducing a pigment called
“melanin” in the skin.
 Most people who use lighteners do so to treat
skin problems such as freckles, age spots,
acne scars, discoloration related to
hormones or lighten skin tone.
 HOW DO THESE
CREAMS BRIG ABOUT
SKIN LIGHTENING?
THE SKIN

 Skin is composed of 2 main layers –

“Epidermis” and “Dermis”
 Skin color results from the presence and
proportion of several chromophores like
Oxyhaemoglobin (bright red), Reduced
Haemoglobin (Bluish red) and
bilirubin(yellow) are found in small blood vessels
of dermis, whereas Eumelanin (deep brown
or black) and Phaeomelanin (Yellowish to
reddish brown) and some Carotenoid pigments
are the main pigments in Epidermis.
Melanin is a pigment that is produced by cells known as melanocytes in the skin
and impart colour to the skin.
The control of melanin production is due to both direct stimulatory effect of
ultraviolet light and a hormone MSH, secreted by anterior pituitary gland.
Melanin comes in two basic forms and can range from yellowish- red to dark
brown. Eumelanin is the most common form of melanin and is brownish in colour.
The other basic form is called Pheomelanin, which produces reddish-brown
colour that is often associated with freckles and red hair.
THE DIFFERENCE IN THE PRODUCTION OF MELANIN IS
AFFECTED BY:
 Exposure to UV radiation: Melanin is produced as a response to UV radiation in order to prevent damage to

the DNA. Individuals, who are exposed to UV light, will produce more melanin for protection.
 Genetic makeup: Different ethnicities and cultures are genetically pre-disposed to producing particular shades

and amounts of melanin due to inheritance. This is, essentially, one of the primary indicators used in determining

race in the human population.

 Size of melanocytes: Melanocyte size varies in different individuals and may lead to a difference in the amount

of melanin produced per cell.

 Disease conditions: Several diseases may affect melanin production, including albinism, a genetic inability to

produce melanin, and vitiligo, a progressive loss of

MELANIN SYNTHESIS PATHWAY
MECHNISM OF DEPIGMENTATION
The various active ingredients generally used to bring about skin lightening adopt the following pathways to reduce Melanin production:
 Selective destruction of melanocytes.
 Inhibiting/Interfering with the biosynthesis of Melanin- By changing the melanin present in the melanosome from dark coloured, oxidized
form to a light colour, reduced form by using a reducing agent bringing about discoloration.
 Inhibit the formation of melanosome or deform their structure
 Inhibit the biosynthesis of tyrosinase.
 Interfere with the transfer of melanosome.
 Activate desquamation to remove the uppermost layer of melanocytes of skin containing keratinocytes bringing about exfoliation.
HYDROQUINONE
 It is considered as one of the best inhibitor of the melanogenesis, by decreasing the
tyrosinase activity by 90% and hence is used in the treatment of melanosis and other
hyper pigmentary disorders. This phenolic compound causes reversible inhibition of
cellular metabolism by affecting both DNA and RNA synthesis.
 It is also a very good depigmenter when used at concentration levels of less that 2%.
Hence products containing higher HQ concentrations than 2% is considered as a
pharmaceutical product and is strictly to be used when prescribed by a medicinal
practitioner. HQ concentration above 5% is not advisable because of the side effects like
skin irritation problems and sometimes may
even cause permanent depigmentation with long term
 HQ solution turns brown on exposure to air , hence use of stabilizer like sodium meta-
bisulphite or sodium sulphite become compulsory with addition of little ascorbic acid.

 High concentration not used due to various side effects Hydroquinone is highly reactive
and potent melanocyte cytotoxic and mutagenic compound, therefore not authorized in
cosmetics anymore.
 Mono benzyl ether Hydroquinone(MBEH)
MBEH causes depigmentation by eclectic melanocytic destruction through free radical
formation and competitive inhibition of tyrosinase enzyme system. However unlike its parent
compound HQ, MBEH almost causes irreversible pigmentation of skin and hence should be
used only in treatment of severe vitiligo.
 Arbutin (hydroquinone-O-beta-D-glucopyranoside)

It is one of the naturally occurring glucopyranoside found in cranberry and blueberry leaves. It causes decreased
tyrosinase activity and is known to inhibit melanosome maturation. It is nontoxic to melanocytes and is used in
variety of pigments in concentration less than 3%.
 Kojic acid (5-hydoxy-4-pyran-4-one-2-methyl)
Kojic acid, is another popular antibiotic skin whitening substance produced in an aerobic process by a variety of
micro-organisms, usually derived from species such as aspergillus and penicillium, is a well-known skin
lightening agent which inhibits tyrosinase activity thereby reducing melanin production. Copper ions are an
essential metal of the active tyrosinase site of melanin synthesis. It functions by chelating Copper at the active
site of tyrosinase enzyme. It also acts as a free radical scavenger However, it is reported to have high
sensitizing potential but is useful to patients who cannot tolerate HQ, and can be combined with topical
corticoid to reduce skin irritation.
Ascorbic acid and its derivatives Vitamin C in the ascorbyl form has been studied by various reporters and is reported to inhibit the
production of melanin.

Glycolic acid

Glycolic acid is an alpha-hydroxy acid derived from sugar cane (Saccharum) and it may have two skin lightening effects. At low
concentrations, it results in a rapid desquamation of pigmented keratinocytes. At higher concentrations, glycolic acid results in
epidermolysis. At concentrations of 3%–7%, they can increase the penetration of other topical skin lighteners such as hydroqu17inone.
 Tretinoin (retinoic acid/ Vitamin A)

• Tretanoin by itself acts as a weak depigmenting agent and is known to show synergistic effect by increasing the depigmenting of
hydroquionone and its derivative.

Niacinamide ( form of vitamin B3)

• Biological active form of vitamin B3 and inhibits melanosome transfer.

Linolenic and Alpha lipoic acid

• Studies have shown that they can decrease UV induced pigmentation.

Mercury

 It is one of the earliest used skin bleach products, however due to its toxicity it is banned in many countries.
 Mushroom
 Matsutake (Trichloma matsutuke) mushroom, the Korean Pine mushroom, is popularly known as Song-Yi mushroom is traditionally used
as a decoction, dipped overnight in water and used as a facial wash to remove summer sun tanned facial spots and for lightening of
facial wrinkles. Song-Yi mushroom liquid concentrate is said to possess better whitening power that Kojic acid and is non-irritating and
stable in most skin whitening formulations. Song-Yi also provides a physical UV blocking effect preventing melanin re-oxidation and
subsequent re- darkening of the skin that can occur in case of hydroquinone or kojic acid usage.

Gluconic acid (HOOC–CHO-CHOH-CHOHCHOH-CH2OH)

 It chelates copper thereby inhibiting oxidation reaction slowing down the enzyme activity. Gluconic acid along with other actives
effectively inhibit melanogenesis to prevent skin discoloration and improve skin complexion.
OTHER COMMONLY USED HOME MADE INGREDIENTS
G ree n t ea e xt r act s P apa ya Ju i ce L emo n Ju ice

Toma to Jui ce Tur me ri c Po w de r

COMPONENTS % WT SPECIFIC EXAMPLES
Moisturizing ingredients 70% Stearyl, palmityl, lauryl, myristyl,
oleyl, sunflower seed oil, cholesterol,
soy sterol, dimethicone, petroleum
jelly, mineral oils.

Emulsifier 1 - 15% Stearic acid, non-ionic and

anionic surfactants, cationic
surfactants, acrylic- based
polymers
Emollient 1 – 20% Lanolin, squalene, jojoba oil and
other oils and esters

Skin lightening active(s) 1 – 10% Kojic acid, vitamin C,

hydroquinone

UV absorbing actives 1- 35% Avobenzone

COMPONENTS % WT SPECIFIC
EXAMPLES

Anti-oxidant actives 0 – 5% Vitamin C, botanicals,

Vitamin E

Rheology modifier 0 - 10% Acrylic based polymers,

xanthan gum

Pigments or Colorants 0 - 10% Iron oxides

Silicone compound 0 - 10% Dimethicone

COMPONENTS % WT SPECIFIC
EXAMPLES

Water resistance agent) 0 - 2% Hydrophobic polymers

such as Soltex
OPT™ water resistance
agent
(trademark of Dow
Fatty alcohols 0 - 5% Thickener, skin feel agent
Water, preservative, Balance to 100%
fragrance
DISADVANTAGES AND CONCLUSION
 Skin lightening products interfere with the normal human biological processing in
deeper skin layers leading to damage of dermal physiology and evokes unwanted
effects like denaturation of cells, contact skin dermatitis, pigment disorder which may
further lead to skin cancer and pigment cell death.
 Melanin present on the skin offers some amount of protection from UV A and UV B
radiation. However, the increased use of skin lightening products leads to loss of cell
pigments thereby increasing the risk of skin cancer.
 Skin lightening is not permanent and the lightened areas become darken on exposure to
light. Hence the presence of sunscreen agent in a topical skin lightening preparation is
highly desirable, to get ideal protection from sunlight. Nevertheless in all these efforts
product stability and its safety in use that is of paramount importance cannot be ignored.