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Anthocyn-TX, Non-Steroidal Oral And Topical Treatment For Management Of Melasma

Author: Dr. Madan Mohan

MBBS, M.D., Consultant Dermatologist, Professor and Head Dept. of Dermatology, Dr. B.R. Ambedkar Medical College, Bangalore

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Melasma is a common pigmentary disorder occurring mostly in women. The pigmentation on face have seeked attention on treating it with various remedies available.  Different external and internal factors act as the cause of melasma. The various treatments have variety of side effects, though new advance studies and technologies are being introduced. The search for safe alternatives has given rise to the development of many newer agents, several of them from natural sources. The need of non-steroidal treatment with depigmentation action is needed which have no side effects in overall average age group and can be used for long term.

Keywords: Melasma, Tranexamic acid, Anthocyn-TX, Steroids, Non-steroidal treatment



Melasma is very well-known with common patches of discoloration and pigmentation on face, cheeks, bridge of nose, neck and even forearms. It is mainly characterized by brown patches or macules. The hyperpigmentation disorder mainly occurs on the exposed area of skin to the sun. Melasma is seen more prevalent in women than men and is the most common pigmentary disorder among Indians. Study shows that 25.8% males of Indian origin have melasma [1]. At present, the female to male ratio is 4:1 of prevalence of melasma in India [2], while in other countries like Malaysia has 6:1 and Indonesia has 24:1 [3].

The conditions are more common in women and in the reproductive age. It also affects the self-esteem and mental health. Patients mostly go through nervous pressure because of appearance, which is very depressing. Studies have shown that women lack confidence and self-esteem due to melasma and often face isolation and social discrimination due to the appearance of black or brown patches on face [4].

The treatment and management of melasma takes long time which also needs patience and use of right products. The long-term treatment of melasma requires religious using of topical creams containing kojic acid, vitamin C, tretinoins etc. Earlier, Steroids were commonly used to treat pigmentation on skin. Promising oral therapies for melasma include tranexamic acid, Polypodium leucotomos, and glutathione [5]. Recurrence of melasma is also common and to avoid such conditions, daily use of broad spectrum sunscreen with SPF 30 or more needs to be applied. Recurrent melasma or stubborn melasma has in-clinic medical procedures done by experienced dermatologists like laser therapy, microdermabrasion and chemical peels etc.


Melasma and its Types

Melasma has been classified into three different types according to the patterns which affects the parts of face. The patterns of discoloration or pigmentation are as follows (figure 1) [6]: -

  1. Centrofacial pattern: The most common and prevalent type seen on cheeks, forehead, upper lip, nose and chin.
  2. Malar pattern: The pattern is seen covering cheeks and nose.
  3. Mandibular pattern: This type involves ramus of mandible.

Figure 1: Different patterns of melasma


According to Wood’s lamp, examination with wavelength of 320-400nm determines the intensity of melanin in the skin [7]. The examination classified melasma into four histological types, which are as follows: -

  1. Epidermal melisma: This is light brown in colour; its color contrast is intensified by Wood’s light. The melanin is distributed throughout the epidermis of the skin.
  2. Dermal melisma: This type of melasma is brown or bluish gray in colour by visible light; under Wood’s light this pattern has no prominent borders.
  3. Mixed melisma: This type is dark brown in colour and some parts of it is intensified under Wood’s light.
  4. Intermediate melisma: This is also known as inapparent melasma and found in dark-brown skin people.


Melasma and its Causes

Although the exact causes and process of occurrence of melasma is not known, some factors are there which triggers melasma. Triggering factors are as follows: -

  • Overexposure to sun rays
  • Pregnancy
  • Use of steroids and birth control pills
  • Ovarian tumours
  • Hormonal problems
  • Genetics
  • Hepatic dysfunction
  • Nutritional deficiency
  • Use of cosmetics and light sensitizing drugs
  • Stress

Ultraviolet radiation exposure is a major triggering factor in the melasma development. It stimulates the proliferation of the cells responsible for skin pigmentation known as melanocytes, while the pigment is known as melanin which is produced from melanosomes by the process of melanogenesis [8]. UV light also induces ROS (reactive oxygen species) by activating nitric oxide which further promotes melanogenesis. It has been found that individuals with melasma have higher levels of oxidative stress when compared to normal healthy individual [9]. At recent times, role of visible light inducing pigmentation is also seen.

Receptors of hormones play a major role in occurrence of melasma. Melasma is prevalent in women taking hormonal oral contraceptives (estrogen- progesterone). The estrogen receptors present on melanocytes may be the reason of stimulation of these cells for overproduction of melanin [10].

Chloasma, or also known as the ‘mask of pregnancy’ occurs due to melanogenesis because of the increased level of hormones like ovarian, placental and pituitary gland in the third trimester [11]. Increased level of progesterone and estrogen increase the tyrosinase transcription, which is also involved in melanin production [12].


Melasma and its Treatment

Over the decades, several forms of treatment have been introduced and are available for melasma. Although it varies from patient to patient in the effectiveness and type of treatment to be taken in the management of melasma.  Patients with chloasma, which is pregnancy associated melasma is for short duration and usually takes few months after delivery to resolve.

Topical treatments are common and also effective in the epidermal melasma, which is a very common form [13]. Topical treatments with photoprotection are mostly the first-line therapies of melasma. Treatment also involves use of various different topical therapies in combination, that are preferred to monotherapy [5].

Earlier, the use of topical steroids like corticosteroids, glucocorticosteroids and cortisones were used for treatment and skin lightening. Monotherapy of these topical steroids are discontinued in recent times due to its adverse effects on long-term treatment of stubborn and recurrent melasma.

Treatment of melasma comprises four methods [5] – Oral, Topical, Procedural and Combinational


Oral therapies for the treatment of melasma is considered to be additional treatment associated with topical ones. The most common oral medicine used in melasma is Tranexamic acid, an anti-plasmin agent which decreases arachidonic acid, which further reduces melanocyte-stimulating hormone [14]. Recent studies have shown that 90% of patients improved, after treated orally with tranexamic acid after 2-6 months [14,15]. Tranexamic acid has some adverse side effects like abdominal bloating, headache and menstrual irregularities.

Glutathione has also shown positive outcome as an adjunctive treatment in melasma. It acts as a potent antioxidant that decreases oxidative stress and inflammation. A randomized controlled trial has shown that glutathione has helped in reducing melanin compared to individuals taking placebo for 4 weeks [16].


The most common and studied topical treatment is with Hydroquinone, a bleaching agent which inhibits tyrosinase and blocks the conversion of DOPA (dihydroxyphenylalanine) to melanin [17]. Another commonly used topical treatment is corticosteroids which has anti-inflammatory properties and prevents pigmentation by non-selectively suppressing melanogenesis. Long term use of this topical agent is not recommended and has adverse effects.

Apart from hydroquinone and steroids, retinoids, azelaic acid, natural compounds like ascorbic acid, kojic acid, arbutin and niacinamide are also used as monotherapy or in combination. The compounds and natural extracts have multiple benefits of the properties apart from depigmentation. Topical retinoids stimulate cell turnover and thus there is rapid loss of melanin. Ascorbic acid, commonly known as vitamin C, decreases ROS as an antioxidant and thus decreases inflammation in melasma lesions [18]. Kojic acid is a natural hydrophilic fungal extract that helps in inhibiting the production of free tyrosinase and also is a potent antioxidant. These are mainly used in combination with one another, well tolerated by patients.


Advance technology has contributed in melasma therapies by Dermatologists. These procedures are carried out under the supervision of experienced and practicing Dermatologists and are in-clinic treatments. Chemical peels are beneficial in the management of epidermal melasma, increases keratinocyte turnover and used in combination therapies for best results. Glycolic acid and trichloroacetic acid of 10%-20% peels are efficacious with no adverse effects of burning sensation.

Laser and light therapies are third-line agents of treatment which target melanosomes and induces damage to it. There are several forms of procedures like CO2 laser, erbium (Er): YAG laser and non-ablative 1550nm fractional laser therapy etc. [19].  Microneedling is also known as mesotherapy, an adjunctive treatment that create channels in the skin to deliver topical drugs intradermally in very small amounts. This stimulates wound-healing response. The technique has the advantage of placing medication to the epidermis and deeper layer dermis, with no adverse effects.


Since monotherapy of steroids and hydroquinone have adverse effects, a very well-known combination of hydroquinone with retinoid and steroid is used. Hydroquinone is also combined with kojic acid and ascorbic acid for safety and also for demelanizing effect. The most important combination is the sunblock or the use of sunscreen daily with the therapies for protection to avoid triggering melasma or recurrent melasma.

Topical steroids like mometasone, hydrocortisone etc. have concerns in monotherapy as discussed earlier, especially on the face. Melasma is a disorder in which long-term therapies are essential to cure the disease. A significant concern over long-term usage of corticosteroids alone may cause epidermal atrophy, telangiectasia, perioral dermatitis, thinning of skin, erythemas and rosacea [20]. Even hydroquinone has shown side effects like exogenous ochronosis and mutagenicity which have increased the concerns of safety of hydroquinone over the decades.

Advancement of technology and new treatment options with non-steroidal medications both topical and oral are available like tranexamic acid, glutathione, vitamin C, kojic acid, natural plant extract derived compounds, which have lesser side effects or no adverse effects at all compared to topical steroids.


Anthocyn-TX Tablet

Anthocyn-TX tablet is a safe oral treatment for melasma. The oral tablet contains Tranexamic acid and Glutathione.

Tranexamic acid is a derivative of amino acid lysine often used as hemostatic. The hemostatic is known for its use based on antifibrinolytic effect. Tranexamic acid 250mg is recommended twice a day daily for 12 weeks [15]. As it is a plasmin inhibitor, it is also used in depigmentation of skin and in melasma.

Keratinocytes secrete urokinase type of plasminogen activator, that further increases the production of melanin in melanocytes. Tranexamic acid prevents the activation of melanocytes from various factors like UV rays and hormones. It inhibits the plasminogen activator process in epidermal cells and keratinocytes (figure 2) [21]. The production of prostaglandins is also suppressed, reducing melanocyte tyrosinase activity and also decreases the angiogenesis by inhibition of VEGF (vascular endothelium growth factor). By the mechanism of action, tranexamic acid gives an additional benefit of reducing the chances of recurrent melasma.

Figure 3 Mechanism of action of Tranexamic Acid in melasma

Figure 2: Mechanism of action of tranexamic acid in melasma


A major concern of tranexamic acid in treatment of melasma is its side effect like thrombosis as it is also used as an antifibrinolytic decreasing blood loss during surgeries and menorrhagia [21].

When tranexamic acid is used as a hemostatic, dosage of 1000mg thrice daily is recommended [22], while on the other part of melasma treatment, 250mg twice a day is prescribed, which suggests its safety profile. The common side effects reported are nausea, diarrhea and orthostatic hypotension. Tranexamic acid is considered as a safe and effective treatment for melasma. Risk of thrombosis may be there in patients of older age group.

Glutathione, is a powerful antioxidant that maintains the redox balance and assists in skin whitening in melasma. It directly binds with copper containing active sites and indirectly inhibits tyrosinase of melanogenesis [23]. It also switches the production of eumelanin to pheomelanin [24] and reduces oxidative stress in melasma. 


Anthocyn-TX Cream

Anthocyn-TX cream is a safe and non-steroidal topical treatment for melasma. The cream contains Tranexamic acid 10%, Arbutin 1.5%, Mulberry extract 1%, Kojic acid 2%, Magnesium ascorbyl phosphate 1% and Vitamin E 1%. A combination therapy of tranexamic acid with depigmenting agents have shown efficacy and safety in melasma [21]. The benefits of this topical treatment is its combination of natural extract and vitamins which can be used for long term without any adverse effects.

As discussed earlier, Tranexamic acid inhibits tyrosinase enzyme, which further reduces the melanocyte activation. Other compounds or extracts present in Anthocyn-TX cream are like:

Arbutin is a derivative of hydroquinone, a natural plant product also acts by inhibiting tyrosinase. The action of arbutin is dose- dependent while less toxic compared to hydroquinone and helps in skin lightening and also promotes even skin-tone.

Mulberry extract is a very potent antioxidant which is known to be rich in vitamin A, C, E and riboflavin beneficial for skin. It delays the maturation of tyrosinase and also acts as competitive inhibitor of the enzyme. Apart from this, it hydrates and nourishes skin with radiant and glowing complexion. It minimizes the signs of premature aging.

Kojic acid prevents melanin production and reduces the discolouration of scars.

Magnesium ascorbyl phosphate is a stable form of vitamin C and brightens the skin with UV protection.

Vitamin E acts by preventing sun damage and sunburn formation of cells.

The cream needs to be applied twice daily for six months with a sunscreen of SPF 30 or above applied on top of it for maximum protection and complete therapy of melasma.


Guide to Treat Melasma

Diet plays a great role to treat melasma, as it conditions deep inside the skin. Melasma needs to be treated with medication as well as proper diet.

  • Foods high in estrogen like flaxseeds, beans and peas etc. should be avoided as it can cause hormonal imbalance
  • Consumption of antioxidant rich food that are of low glycemic index is essential
  • Foods that an individual is allergic to; needs to be avoided
  • Packaged fruit juices, energy drinks, alcohol and other inflammatory drinks should be strictly avoided
  • Discontinuation of contraceptive pills
  • Round the year and lifelong sun protection should be practiced by using broad brimmed hat and sunscreen



Melasma needs patience to be treated as long-term topical treatment is needed. Universal treatment of melasma is still not there. With recent times, safety profile of treatment is a major concern. Awareness of harmful side effects of long term use of steroids have reduced the use of the popular treatment of triple combination with hydroquinone. Tranexamic acid has shown efficacy in treating melasma clinically (according to the Melasma Area and Severity Index (MASI), a validated scale used to measure the extent of facial hyperpigmentation). Tranexamic acid orally and in topical combination is a new, safe and effective treatment and has shown promising results in various trials for melasma that also reduces the chances of recurrence.



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