Kojic acid vis-a-vis its combinations with hydroquinone and betamethasone valerate in melasma: A randomized, single blind, comparative study of efficacy and safety

Abstract

Background:Melasma is a relatively common, acquired symmetric hypermelanosis characterized by irregular light to gray-brown macules involving sun-exposed areas. Kojic acid, with its depigmenting potential due to tyrosinase inhibition and suppression of melanogenesis, has become a vital component of the dermatologists’ armamentarium against melasma.Aim:To study and compare the efficacy of kojic acid 1% alone, vis-a-vis its separate combinations with 2% hydroquinone or 0.1% betamethasone valerate and a combination of all these three agents with respect to the duration of symptoms and level of pigmentation in the therapy of melasma.Materials and Methods:Eighty patients from a single tertiary care center objectively assessed by calculating the melasma area severity index (MASI) and randomized (simple randomization) into four parallel groups (A, B, C, and D) of 20 each were prescribed once daily local application at night, (participants blinded regarding the difference in identity of interventions), as follows:Group A – kojic acid 1% cream.Group B – kojic acid 1% and hydroquinone 2% cream.Group C – kojic acid 1% and betamethasone valerate 0.1% cream.Group D – kojic acid 1%, hydroquinone 2%, and betamethasone valerate 0.1% cream.Strict photoprotection and use of a SPF 15 sunscreen was advised during the day. Patients were evaluated every 2 weeks and a fall in MASI score was calculated at the end of the study period of 12 weeks by the same investigator.Results:The response was compared according to percentage decrease in MASI score. Efficacy was evaluated among the groups at the end of 3 months using bivariate analysis and calculated by using the paired ‘t’ test. The clinical efficacy of group B was the highest followed closely by group D and group A, that of group C being the lowest.Conclusion:Kojic acid in synergy with hydroquinone is a superior depigmenting agent as compared with other combinations.

Evaluation of the efficacy of cysteamine 5% cream in the treatment of epidermal melasma: a randomized double-blind placebo-controlled trial

“…2,15,16 Some of these treatments include hydroquinone-containing creams, [17][18][19] azelaic acid preparations, 20,21 topical retinoids (e.g. retinoic acid), 13,22 alpha-hydroxy acids, 23,24 kojic acid 25,26 and ascorbic acid, 27 responses to which are variable. Some treatments incorporate a combination approach such as triple-combination creams (hydroquinone, retinoic acid and a steroid).…”

Melasma: an Up-to-Date Comprehensive Review

“…Corticosteroids can prevent pigmentation by non-selective suppression of melanogenesis while also serving as an anti-inflammatory agent [ 52 ]. Corticosteroids alone are unlikely to be superior to depigmenting agents when used as monotherapy [ 52 ].…”

“…Corticosteroids can prevent pigmentation by non-selective suppression of melanogenesis while also serving as an anti-inflammatory agent [ 52 ]. Corticosteroids alone are unlikely to be superior to depigmenting agents when used as monotherapy [ 52 ]. Although they have an independent ability to suppress melanogenesis, the current literature shows that corticosteroids have not been demonstrated to have long-term benefits in treating melasma [ 50 ].…”

“…Ascorbic acid has a theorized benefit of decreasing reactive oxygen species, which decreases inflammation in melasma lesions [ 23 , 65 ]. However, both were shown to be inferior to HQ in improving MASI scores when used as monotherapies [ 51 , 52 , 66 ]. Another natural compound, azelaic acid (AA), was noted in an open-label study to be effective in improving pigmentation by inhibiting tyrosinase activity [ 43 ].…”

miR-330-5p Targets Tyrosinase and Induces Depigmentation

“…We tested whether miR-330-5p did indeed target TYR and act on melanin levels: we overexpressed miR-330-5p using mimics in highly pigmented human melanoma cells (MNT-1) and normal melanocytes for a period of 12 days. As controls, we used classic depigmenting agent Kojic acid (Deo et al, 2013), small interfering RNA against TYR, and miR-137/miR-7 mimics. Prediction score for miR-7 acting on MITF is low, whereas miR- 137 scored the highest (Supplementary Table S1 online).…”