Skin-Lightening Agents

Ariski Pratama Johan

Kang S. Fitzpatrick's Dermatology, 2-Volume Set (EBOOK). McGraw Hill Professional; 2018 Apr 27.
 Skin Pigmentation
Skin pigment (melanin) is produced by melanocytes ↑

Sunscreen use and sun avoidance :

SPF for Amulations, polypodium leukotomes and
pycnogenols

Inhibiting the tyrosinase enzyme :

vitamin C, hydroquinone, kojic acid, arbutin, mulberry Hyperpigmentation or
Skin Tone extract, and licorice extract dyschromia
on the face

Preventing melanosome transfer into keratinocytes by blocking

the PAR-2 receptor : Both soy and niacinamide, a derivative of
vitamin B3

Increasing desquamation of the SC:

Mechanical such as microdermabrasion, scrubs, rotating brushes, or
rough fabrics, or chemical such as hydroxy acids and retinoids
Hydroquinone
Hydroquinone is an effective and widely used skin lightening agent for the
treatment of melasma, postinflammatory hyperpigmentation, and other
hyperpigmentation disorders. It acts by inhibiting the conversion of tyrosine to
melanin.
Four to 6 weeks of monotherapy with hydroquinone is generally required before
depigmenting effects are seen.
Common side effects associated with hydroquinone are skin irritation and contact
dermatitis. A rare side effect is the development of exogenous ochronosis, a sooty
hyperpigmentation in the treatment area,
Arbutin
Arbutin (hydroquinone--D-glucopyranoside) and methylarbutin are skin-lightening
glucosides found in bearberry (arctostaphylos uva ursi), a fruit enjoyed by bears
but not by humans. Arbutin is also present in certain herbs and pear trees.
Hydroxy Acids
Hydroxy acids are organic carboxylic acids classified into alphahydroxy acids
(AHA), beta‐hydroxy acids (BHA), polyhydroxy acids, and bionic acids on the
basis of their molecular structure.
Hydroxy acids are found to be present in antiaging formulations, moisturizers,
and peels, and in treatment products to improve hyperpigmentation and acne.
The skin appears to be smoother and more uniform.
Property of AHAs to enhance epidermal shedding. Some claim that AHAs increase
the synthesis of glycosaminoglycans (GAGs), improve the quality of elastic
fibers, and increase the density of collagen.
Glycolic acid
Glycolic acid is an alfa-hydroxy acid derived from sugarcane. In low
concentrations, glycolic acid produces rapid desquamation of pigmented
keratinocytes.
In higher concentrations, glycolic acid results in epidermolysis. Removal of
superficial layers of epidermis with glycolic acid peels using glycolic acid in
concentrations of 30 to 70% can enhance the penetration of other topical skin
lighteners, such as hydroquinone.
The addition of glycolic acid to hydroquinone enhances efficacy.
Kojic Acid
Kojic acid is a tyrosinase inhibitor derived from fungi species and is used widely
in Asia in concentrations of 1 to 4%.
Combining kojic acid with a topical corticosteroid can reduce irritation.
Skin-lightening products that contain kojic acid are typically used twice per day for
1 or 2 months.
Licorice Extract
The principal active compound of licorice root extract is glabridin,
which is used in concentrations of 10 to 40% in skin-lightening
products.
The depigmenting effect of glabridin has been shown to be 16 times
greater than that of hydroquinone. It is also faster acting: in one study,
the skin-lightening effect of pure glabridin was apparent after 7
days of use.
In a Thai study in which 0.4% licorice extract was combined with
0.05% betamethasone and 0.05% retinoic acid, 70% of patients reported
the effects of their treatment to be “excellent.”
Niacinamide
Vitamin B3, commonly known as nicotinamide or niacinamide, is available in
cosmetic and cosmeceutical products and can be used as a complementary agent for
some types of acne, as well as aging skin
Niacinamide, the amide form of vitamin B3, inhibits the transfer of melanosomes
to the epidermal keratinocytes.
Paper Mulberry
Paper mulberry extract, a popular skin-lightening agent in Europe and South
America, is isolated from the roots of the Broussonetia papyrifera tree.
In a Korean study, the tyrosinase inhibition activity of paper mulberry was
compared with that of hydroquinone and kojic acid.
The 50% inhibitory concentration of paper mulberry extract was reported to be
0.396% versus 5.5% for hydroquinone and 10% for kojic acid.
A patch test using 1% paper mulberry extract revealed no significant skin irritation
at 24 and 28 hours
Retinoids and Retinoid Combination
Therapy
The retinoids are vitamin A derivatives constituting the most
effective comedolytic agents. They function by normalizing
desquamation of the follicular epithelium, preventing the formation of
new microcomedo, and minimizing the formation of comedones and
inflammatory lesions.
Retinoids and Retinoid Combination
Therapy
Retinoids such as tretinoin and retinol are derived from vitamin A. These
products are used successfully to treat melasma, postinflammatory
hyperpigmentation, and other pigmentation disorders.
Retinol is less effective and less irritating than tretinoin.
The actual mechanism of depigmentation has not been established. In animal
studies, retinol has been shown to inhibit tyrosinase induction. Retinoids may also
interfere with pigment transfer to keratinocytes and accelerate pigment loss by
causing the epidermis to be shed more quickly.
Soy
Natural soybeans contain Bowman-Birk inhibitor and soybean trypsin inhibitor,
two serine protease inhibitors that interfere with the protease-activated receptor 2
pathway, thereby reducing melanin transfer and inducing depigmentation.
Only with unpasteurized soy milk. Soy has proven to be both efficacious and safe.
Several skin care products containing total soy are available to improve mottled
hyperpigmentation and solar lentigines. Skin-lightening benefit is seen after 12
weeks of twice daily application.
Vitamin C
Vitamin C interferes with pigment production by interacting with copper ions at the
tyrosinase activity site and reducing dopaquinone. Magnesium L-ascorbic acid-2-
phosphate (MAP), a stable derivative of vitamin C, has been shown to lighten
pigmentation.
In one study of patients with melasma and solar lentigines, a cream containing 10%
MAP produced significant skin-lightening effects in 19 of the 34 participants.
Daftar Pustaka
Kang S. Fitzpatrick's Dermatology, 2-Volume Set (EBOOK). McGraw Hill
Professional; 2018 Apr 27.
Rendon MI, Gaviria JI. Review of skin‐lightening agents. Dermatologic surgery.
2005 Jul;31:886-90.
Mukul S, Surabhi K, Atul N. Cosmeceuticals for the skin: An overview. Asian J.
Pharm. Clin. Res. 2011;4(2):1-6.