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Innovations and Future Prospects of Dermal Delivery Systems
Published in Tapash K. Ghosh, Dermal Drug Delivery, 2020
Rashmi Upasani, Anushree Herwadkar, Neha Singh, Ajay K. Banga
Cosmeceuticals for pigmentation is another popular market. These products are based upon vitamins and botanicals that are able to interrupt melanin production at key steps. In recent years efforts have been focused on developing a hydroquinone alternative without the melanocyte toxicity associated with the oxidized version of hydroquinone. Hydroquinone is a recognized gold standard for its skin lightening properties. Till date, no single ingredient has been able to measure up to hydroquinone. Kojic acid (5 hydroxymethyl-4H pyrane 4-one) is one of the most popular skin lightening agents worldwide, however it has been removed from Japan due to its sensitizing properties (Reszko et al. 2009). The newer cosmeceutical skin lightening preparations contain multiple ingredients for optimal efficacy. For example, one cosmeceutical product contains Kojic acid in combination with embelica fruit extract and glycolic acid.
Acne Scarring and Patients of African Descent
Published in Antonella Tosti, Maria Pia De Padova, Gabriella Fabbrocini, Kenneth R. Beer, Acne Scars, 2018
Aldo D. Galvez, Amy J. McMichael
Arbutin, available over the counter, is a derivative of hydroquinone used in PIH. Obtained from the leaves of the bearberry plant, it decreases tyrosinase activity and inhibits melanosome maturation. Aleosin is a glycoprotein derived from Aloe vera that inhibits tyrosinase without cytotoxicity. It has limited ability to penetrate the skin due to its hydrophilic property. It is commonly used with Arbutin. Licorice extract is considered the safest pigment-lightening agent [29]. Its mechanism of action is similar to kojic acid. The main component is glabridin.
Aesthetic
Published in Tor Wo Chiu, Stone’s Plastic Surgery Facts, 2018
Glycolic acid (40%–70%) is an AHA from sugar cane, similar to lactic (milk), tartaric (grapes), malic (apples) and citric acids. Hence, the alternative collective term is ‘fruit acids’ (but most can be synthesised in the laboratory). Kojic acid peels are more irritant and are thus second-line treatment. The effects are less dramatic than dermabrasion/chemical peel/facelifts but with less risk. The depth of effect is related to concentration and time of contact (neutralising with bicarbonate/rinsing with water). There is no significant downtime (i.e. typical ‘lunch time peel’, although some get crusting several days later). There may be temporary irritation and thinning of skin that needs sun protection.
Cosmetic skin lightening use and side effects
Published in Journal of Dermatological Treatment, 2022
Natasha Masub, Amor Khachemoune
Other skin lightening agents include glutathione, kojic acid, and arbutin. Glutathione is an oral, topical and intravenous agent that causes skin depigmentation both directly by inhibiting the copper-containing active site of tyrosinase and indirectly via antioxidant scavenging of reactive oxygen species (53). While intravenous glutathione skin lightening has long been popular in Asia, there is increasing demand in the US for intravenous glutathione among patients who have experienced side effects from topical skin lightening (54). Among available OTC skin lightening agents, kojic acid and arbutin are among the most effective (55). Kojic acid is a fungus-derived agent that primarily acts as a copper-binding tyrosinase inhibitor. Side effects of kojic acid include contact dermatitis and increased UV sensitivity (56–58). Arbutin is a botanical agent structurally similar to hydroquinone. Arbutin acts by reversibly inhibiting tyrosinase activity and melanosome transfer. The primary side effects of arbutin include contact dermatitis and paradoxical hyperpigmentation at higher concentrations (59–61).
Evaluation of the of the efficacy of Fractional Erbium-Doped Yttrium Aluminum Garnet Laser-Assisted Drug Delivery of Kojic Acid in the Treatment of Melasma; A split face, comparative clinical study
Published in Journal of Cosmetic and Laser Therapy, 2021
Muhsin A. Al-Dhalimi, Raya Hamid Yasser
The treatment protocol of patients with melasma often begins with the efforts of avoidance of aggravating factors like sun exposure and topical lightening drugs with or without the use of some energy-based devices. Although topical drugs and interventions may temporarily reduce the pigmentation, the condition often gets recurrence or relapse. The mechanism of treatment may involve the inhibition of mechanism of melanin synthesis, reduction of melanosome transference from melanocytes to keratinocytes, and acceleration of melanin pigment removal (3). Kojic acid is a fungal metabolic product produced from fermentation of Aspergillus (especially Aspergillus oryzae) and Penicillium. It inhibits the catecholate activity of tyrosinase. It is a potent antioxidant (4). It is increasingly used as lightening agent in treatment of melasma as alternative of the hydroquinone (HQ) (5–7). HQ was the golden agent in treatment of melasma until governing organizations in Japan, Europe and the United States questioned its safety and prohibits its use except in very low percentages (8).
A promising and effective platform for delivering hydrophilic depigmenting agents in the treatment of cutaneous hyperpigmentation: kojic acid nanostructured lipid carrier
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2021
Khadijeh Khezri, Majid Saeedi, Katayoun Morteza-Semnani, Jafar Akbari, Akbar Hedayatizadeh-Omran
Skin melanin is a biological pigment, which is produced by melanocytes. Melanin is a main factor in determining skin colour which protects human skin from the hazardous effects of ultraviolet (UV) sun radiation. Over synthesis of melanin is called hyperpigmentation [1]. Treatment of hyperpigmentation has always been challenging and discouraging for most people, especially women [2]. Kojic acid (KA) is a natural bleaching agent and a well-known tyrosinase inhibitor with hydrophilic character which is used to treat hyperpigmentation. KA inactivates the tyrosinase enzyme and suppresses the tautomerization of dopachrome by chelating copper atoms. It is synthesized by several fungal species such as the Aspergillus and Penicillum [3]. Despite the unique properties of KA and its derivatives, their use is very limited in the cosmetic industries. KA is a hydrophilic ingredient due to the presence of two hydroxyl functional groups in its chemical structure and because of its hydrophilic nature. It has inadequate absorption from the skin [4].