Skin Lightening Agents


Summary and Key Features

  • Hyperpigmentation is a common skin problem that is particularly prevalent in middle-aged and elderly individuals that can detract from appearance and quality of life.

  • Hydroquinone depigments skin by inhibiting the conversion of tyrosine to melanin by 90%.

  • Kojic acid is used in concentrations between 1 and 4% and is often more effective in combination with other ingredients, but has been reported to have a high sensitizing potential and may cause irritant contact dermatitis.

  • Soy induces interference with the PAR-2 pathway and has been shown to reduce dyspigmentation by reducing the phagocytes of melanosomes by keratinocytes, reducing melanin transfer.

  • Bearberry contains a crystallizable glucoside, known as arbutin and methyl arbutin, both with skin lightening properties.

Introduction

Hyperpigmentation is a common skin problem that is particularly prevalent in middle-aged and elderly individuals. It is cosmetically important and can greatly detract from both appearance and quality of life, particularly in cultures where smooth skin is valued as a sign of health or in cultures that are beauty conscious. Hyperpigmented skin lesions may be postinflammatory as a sequel to acne, trauma, chemical peels, or laser therapy. Exogenous causes, particularly ultraviolet (UV) light exposure, are a common factor in pigmentary abnormalities such as melasma, solar lentigines, and ephelides ( Fig. 12.1 ). Exposure to certain drugs and chemicals as well as the existence of certain disease states can result in hyperpigmentation ( Box 12.1 ).

Figure 12.1, The typical appearance of melasma with reticulated hyperpigmented plaques: ( A ) before cosmeceutical treatment; ( B ) 8 weeks after cosmeceutical treatment

Box 12.1
Acquired hyperpigmentation

Skin diseases and conditions

  • Melasma

  • Riehl's melanosis

  • Poikiloderma of Civatte

  • Erythromelanosis follicularis

  • Linea fusca

  • Postinflammatory hyperpigmentation

Exogenous causes

  • Ultraviolet exposure (e.g. melasma, solar lentigines, ephelides)

  • Photosensitizing agents (e.g. berloque dermatitis due to bergamot oil, furocoumarins)

  • Drugs (e.g. estrogens, tetracyclines, amiodarone, phenytoin, phenothiazines, sulfonamides)

  • Cosmetics

Other causes

  • Pregnancy

  • Liver disease

  • Addison's disease

  • Hemochromatosis

  • Pituitary tumors

The treatment of acquired hyperpigmentation has traditionally been challenging and frequently discouraging. Many of the agents that have been used cause skin irritation, require many months of regular use before results are apparent, or are only partly effective. Patient compliance with therapy must be strict. Sun avoidance and the religious use of a high sun protection factor (SPF) sunblock are mandatory for successful treatment.

Skin lightening cosmeceuticals

Multiple depigmenting cosmeceuticals are currently available, although published clinical evidence to support their effectiveness is lacking. These skin lightening compounds work by removing undesired pigment by acting at one or more steps in the pigmentation process ( Box 12.2 ). Since tyrosinase is the rate-limiting enzyme for melanin biosynthesis, many of the cosmeceuticals for skin lightening exert their effect on this enzyme.

Box 12.2
Modified from Briganti, S., Camera, E., Picardo, M., 2003. Chemical and instrumental approaches to treat hyperpigmentation. Pigment Cell Research 16, 1–11.
Depigmenting agents and reported effect on the melanin synthetic pathway

Before melanin synthesis

  • Tyrosinase transcription:

    • Tretinoin

During melanin synthesis

  • Tyrosinase inhibition:

    • Hydroquinone

    • 4-Hydroxyanisole

    • 4-S-Cystaminylphenol and derivatives

    • Arbutin

    • Aloesin

    • Azelaic acid

    • Kojic acid

    • Emblica

    • Tyrostat

  • Peroxidase inhibition:

    • Phenols

  • Product reduction and ROS scavengers:

    • Ascorbic acid

    • Ascorbic acid palmitate

After melanin synthesis

  • Tyrosinase degradation:

    • Linoleic acid

    • α-Linolenic acid

  • Inhibition of melanosome transfer:

    • Serine protease inhibitors

    • Lecthins and neoglycoproteins

    • Soybean/milk extracts

    • Niacinamide

  • Skin turnover acceleration:

    • Glycolic acid

    • Lactic acid

    • Linoleic acid

    • Liquiritin

    • Retinoic acid

    • Helix aspersa Müller

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