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PEER-REVIEW | COSMECEUTICALS |


Table 6 Overview of clinical studies with pigment- reducing agents


has been shown to cause depigmentation by interfering with the melanin metabolic pathway44


. A double-blinded


5% Vitamin C vs. 4% HQ


16 – Melasma Niacinamide 18 + Hyper-


Kojic acid vs HQ


extract Orchid


extract Soy


extract vs 3% pigmentation Topical 16 weeks 62.5% vs 93% 70/LOE-II


6.2% vs 68.7% side-effects


Topical 4 weeks Significant


80 – Mild/moderate Topical 12 weeks Equivalent dyschromia


Grape seed 12 – Chloasma


vitamin C Coffeeberry 30 + Hyper-


moisturizer Licorice


48 – Melasma, lentigo


pigmentation


extract 2% NAG + 4% 202 + Hyper-


niacinamide Natural


ingredient product vs HQ


65 + Moderate 20 – Melasma


56 – Hyper- photodamage


pigmentation pigmentation


Oral 6 months Significant


Topical 8 weeks Equivalent efficacy


Topical 6 weeks Global im-


provement in skin lightening


Topical 12 weeks Significant Topical 4 weeks Topical 8 weeks


Significant Significant


Topical 12 months Equivalent prescription pigmentation conditions. The gold standard and most


effective agent for pigment-lightening was hydroquinone, however due to its side effects and safety profile its use has been restricted in cosmeceuticals41


. As an alternative, a variety


of vitamins and botanics have also been evaluated and a summary of their clinical studies for pigment-reduction is presented in (Table 6).


Ascorbic acid Vitamin C is a naturally occurring antioxidant, a property that has been shown to reduce tyrosinase activity and melanin synthesis42


. Topical


vitamin C derived from fruits and vegetables is unstable, hence derivatives such as magnesium- ascorbyl-phosphate (MAP) have been developed43


.


Alpha tocopherol (vitamin E) Vitamin E is a major lipophilic antioxidant and


improvement with


pigmentation efficacy


decrease in hyper-


46/LOE-


71/LOE-II 72/LOE-III 73/LOE-III


48/LOE-II


74/LOE-II 75/LOE-II 76/LOE-I 77/LOE-II


study on the therapeutic effects of a combination preparation of vitamins E and C in comparison with single preparations of both vitamins in the treatment of chloasma or pigmented contact dermatitis (PCD) revealed that the combination treatment resulted in significantly better clinical improvement as compared to vitamin C alone, in both diseases45


.


Niacinamide Niacinamide is the active amide of vitamin B3 interferes with the interaction between keratinocytes and melanocytes, thereby inhibiting melanogenesis46


.


Kojic acid Kojic acid is a fungal product derived from certain species of Acetobacter, Aspergillus, and Penicillium, and reduces hyperpigmentation by inhibiting the production of free tyrosinase47


.


Plant extracts Various plant extracts have been studied for pigment- reduction due to the lack of side-effects. Grape seed, orchid, coffeeberry, soy, licorice or herbal blend extracts have shown inhibition of melanin synthesis through their antioxidant and other enzymatic properties48


.


N-Acetyl glucosamine N-acetylglucosamine (NAG) is a monosaccharide that inhibits the conversion of protyrosinase to tyrosinase, thus decreasing pigmentation49


.


Erythema-reducing agents Erythema, commonly associated with inflammation and UV-exposure, has been a treatment target for cosmeceutical agents


(Table 7). Topical application of anti- inflammatory plant extracts immediately after irradiation can reduce erythema symptoms. Polypodium leucotomos, marketed in some countries as Heliocare, comes from a tropical fern plant. The antioxidant and photoprotective properties of the plant extract have been used for the treatment of inflammatory disorders and skin diseases. Oral and topical administration has been clinically shown to prevent sunburn and UV-induced erythema. One possible molecular


mechanism for this protection seems to be the inhibition of UV-induced


20 ❚


Grape seed, orchid, coffeeberry, soy, licorice or herbal blend extracts have shown inhibition of melanin synthesis through their antioxidant and other enzymatic properties.


March 2015 | prime-journal.com


Active ingredient


Patients


Placebo controlled Study


endpoints


Route of administration Treatment


Results/ improvement


Reference/ level of evidence


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