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      Applications of hydroxy acids: classification, mechanisms, and photoactivity

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          Abstract

          Hydroxy acids (HAs) represent a class of compounds which have been widely used in a number of cosmetic and therapeutic formulations in order to achieve a variety of beneficial effects for the skin. We review and discuss the most frequently used classes of these compounds, such as α-hydroxy acids, β-hydroxy acids, polyhydroxy acids, and bionic acids, and describe their applications as cosmetic and therapeutic agents. Special emphasis is devoted to the safety evaluation of these formulations, in particular on the effects of their prolonged use on sun-exposed skin. Furthermore, we summarize the very limited number of studies dealing with the modifications evoked by topical application of products containing HAs on photocarcinogenesis. In spite of the large number of reports on the cosmetic and clinical effects of HAs, their biological mechanism(s) of action still require more clarification. Some of these mechanisms are discussed in this article along with important findings on the effect of HAs on melanogenesis and on tanning. We also emphasize the important contribution of cosmetic vehicles in these types of studies. Thus, HAs play an important role in cosmetic formulations, as well as in many dermatologic applications, such as in treating photoaging, acne, ichthyosis, rosacea, pigmentation disorders, and psoriasis.

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          Most cited references28

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          Clinical and cosmeceutical uses of hydroxyacids.

          The hydroxyacids are represented by the alpha-hydroxyacids, beta-hydroxyacids, polyhydroxy acids, and bionic acids. Together, these ingredients form a class of compounds with unparalleled benefits to the skin and unprecedented usage in the cosmeceutical market in cosmetic and therapeutic formulations alike. The most commonly used hydroxyacid is glycolic acid, an alpha-hydroxyacid that has been used extensively in cosmetic antiaging formulations, moisturizers, and peels, and in treatment products to improve hyperpigmentation and acne. The newer polyhydroxy and bionic acids offer the benefits of alpha-hydroxyacids without irritation, making them suitable for use on sensitive skin, rosacea, and after cosmetic procedures. They also provide additional antioxidant/chelation, barrier strengthening, and moisturizing effects. Bionic acids inhibit matrix metalloproteinase enzymes in skin, providing a preventative antiaging benefit. The hydroxyacids as a class can be combined with therapeutically active materials and cosmetic procedures to increase therapeutic effects and improve tolerability and outcomes of medicinal agents and procedures.
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            The inhibitory effect of glycolic acid and lactic acid on melanin synthesis in melanoma cells.

            Alpha-hydroxy acids (AHAs) such as glycolic acid (GA) and lactic acid (LA) have been reported to be effective in treating pigmentary lesions such as melasma, solar lentigines, and postinflammatory hyperpigmentation. The mechanism of this effect might be due to epidermal remodeling and accelerated desquamation, which would result in quick pigment dispersion. However, the direct effect of AHAs on melanin synthesis has not yet been well studied. To elucidate such a direct effect of AHAs on melanogenesis, we performed melanin assays, growth curve determinations, Northern and Western blotting for melanogenic proteins [tyrosinase, tyrosinase related protein (TRP)-1 and TRP-2], and tyrosinase and, 4-dihydroxyphenylalaninechrome tautomerase enzyme activity assays using mouse B16 and human melanoma cells. GA or LA (at doses of 300 or 500 microg/ml) inhibited melanin formation in similar dose-dependent manner, without affecting cell growth. Although the mRNA and protein expression or molecular size of tyrosinase, TRP-1 and TRP-2 were not affected, tyrosinase activity was inhibited. To see whether GA and/or LA directly inhibit tyrosinase catalytic function, the effect of GA and LA on human tyrosinase purified from the melanosome-rich large granule fraction of human melanoma cells was performed. GA or LA were shown to inhibit tyrosinase enzyme activity directly, but this effect was not due to the acidity of GA or LA, because adjusting the pH to 5.6 (the pH of GA and LA at concentrations of 2500 microg/ml), did not affect tyrosinase activity. Taken together, these results show that GA and LA suppress melanin formation by directly inhibiting tyrosinase activity, an effect independent of their acidic nature. GA and LA might work on pigmentary lesions not only by accelerating the turnover of the epidermis but also by directly inhibiting melanin formation in melanocytes.
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              Glycolic acid treatment increases type I collagen mRNA and hyaluronic acid content of human skin.

              Chronic solar irradiation results in both morphologic and functional changes in affected skin. alpha-hydroxy acids, such as glycolic acid, have been shown to improve photodamaged skin. To investigate alterations in collagen gene induction and epidermal and dermal hyaluronic acid production as a result of administered glycolic acid. In this study we compared collagen gene expression from skin biopsy specimens, and epidermal and dermal hyaluronic acid immunohistochemical staining between glycolic acid-treated and vehicle-treated skin. Forearm skin was treated with 20% glycolic acid lotion or a lotion vehicle control twice a day for 3 months. Epidermal and dermal hyaluronic acid and collagen gene expression were all increased in glycolic acid-treated skin as compared to vehicle-treated controls. Our data suggest that epidermal and dermal remodeling of the extracellular matrix results from glycolic acid treatment. Longer treatment intervals may result in collagen deposition as suggested by the measured increase in mRNA.
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                Author and article information

                Journal
                Clin Cosmet Investig Dermatol
                Clinical, Cosmetic and Investigational Dermatology
                Clinical, cosmetic and investigational dermatology : CCID
                Dove Medical Press
                1178-7015
                2010
                24 November 2010
                : 3
                : 135-142
                Affiliations
                [1 ]US Food and Drug Administration [retired], Annandale, VA, USA;
                [2 ]Laboratory of Cell Biology, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA
                Author notes
                Correspondence: Andrija Kornhauser, 4517 Pinecrest Hgts Dr, Annandale, VA 22003, USA, Tel +1 703 941 4221, Email akornhause@ 123456aol.com
                Article
                ccid-3-135
                10.2147/CCID.S9042
                3047947
                21437068
                6e2b4ca8-d2d1-4b84-a52d-dc019b66c1a5
                © 2010 Kornhauser et al, publisher and licensee Dove Medical Press Ltd.

                This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.

                History
                : 23 November 2010
                Categories
                Review

                Dermatology
                uv,glycolic acid,hydroxy acids,salicylic acid,erythema,cosmetics
                Dermatology
                uv, glycolic acid, hydroxy acids, salicylic acid, erythema, cosmetics

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