Skin Lightening Agents

There are several skin lightening treatments used commercially to attempt to lighten the skin, and in particular treat sun spots, age spots, liver spots or solar lentigines.

Some of the most popular skin lightening and age spot treatments are listed below:

Aloesin

Aloesin comes from the aloe plant.  Aloesin can achieve reasonably successful penetration of the skin, but it is difficult to synthesize in commercial quantities.

Hydroquinone

Many of the most popular skin lightening agents, vanishing creams and age spot removal treatments used to have 2-4% Hydroquinone.  Unfortunately, it was shown to cause cancer in some animal testing, and is either banned or limited to 1-2% in solution.

Azeliac acid

Azeliac acid inhibits tyrosinase, oxid enz and DNA synthesis;

Kojic acid

Kojic acid is another inhibitor of tyrosinase, but users of Kojic acid have had a high incidence of skin reactions.

Reinoids, Vitamin A metabolites

Retin- A is a common ingredient in cosmetics and other over the counter (OTC) preps;

Trentinoin

Trentinoin lightens pigmented scars in Af-AM but produce unwanted lightening of skin

Melatonin

Melatonin-hormone from pineal gland inhibits melanogenesis in dose depend manner but difficult to prepare in quantity and potentially antigenic.

Linoleic Acid


Linoleic acid-induces tyrosinase degradation and inc skin desquamation-poorly absorbed in aqueous phase but has good cell membrane penetration

Combinations of the skin lightening agents listed are can increase efficacy but increase potential AEs-Senegal experience
Slide 14

Aloesin-from aloe, reasonable penetration, difficult to synthesize
Hydroquinone 2-4% but now banned or lim to 1-2%
Azeliac acid- inhibits tyrosinase, oxid enz and DNA synthesis; Kojic also tyrosinase inhib but high incidence of skin reactions
Reinoids-vit A metabolites, common in cosmetics and othe OTC preps; Trentinoin lightens pigmented scars in Af-AM but produce unwanted lightening of nl skin
Melatonin-hormone from pineal gland inhibits melanogenesis in dose depend manner but difficult to prepare in quantity and potentially antigenic
Linoleic acid-induces tyrosinase degradation and inc skin desquamation-poorly absorbed in aqueous phase but has good cell membrane penetration
Combos increase efficacy but increase potential AEs-Senegal experience
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