Efficacy and safety of Politranexamide® liposomal emulsion on facial melasma: A comparative study

Melasma is a human melanogenesis dysfunction that results in localized, chronic acquired hypermelanosis of the skin difficult to treat.

hypopigmenting agents, such as hydroquinone, kojic acid, azelaic acid or on laser therapy, pulsed light, chemical peels and dermabrasion. 2,3 Recently, several studies have evaluated the efficacy of tranexamic acid [trans-4-(Aminomethyl) cyclohexane-carboxylic acid] (TA) in melasma as oral, topical, and intra-lesional agent. 3 TA is an antiplasmin and antifibrinolytic agent, commonly used as a hemostatic drug.
TA competitively inhibits the plasminogen activator, blocking the conversion of plasminogen to plasmin. 4 Ultraviolet radiation acts as trigger factor in the activation of plasminogen, which subsequently results in the conversion into plasmin. Plasmin triggers the release of basic factor of fibroblasts, a powerful stimulator of melanocyte growth. 5 It was also observed that plasmin represents a strong activator towards the dendritic connections of the melanic unit between melanocytes and keratinocytes. The inhibition of the conversion from plasminogen to plasmin would prevent these connections, decreasing the pigmentation of the areas subjected to treatment with TA. 5,6 Furthermore, an increase in vascularization and a high expression of angiogenic factors have been demonstrated in the affected skin. [7][8][9] TA may also reverse the abnormal dermal changes associated with melasma, such as the aforementioned increased vasculature. 10 Additionally, TA has a structural similarity with tyrosine, thereby competitively inhibiting tyrosinase enzyme. 11 Nevertheless, the exact rationale through which TA would act in inhibiting melanogenesis is still partially unknown. 12 Politranexamide® has been recently introduced as a patented topical therapy of melasma. The product consists of a liposomal emulsion, which facilitates skin absorption. Liposomes are microscopic spherical vesicles, consisting of a phospholipid double layer, which contain the functional substances necessary for the treatment. The particular vehicle of this liposomal emulsion allows Politranexamide® to reach its target, thus increasing its effectiveness. visits at the end of Weeks 6 and 12, after initiation of therapy. All patients were subjected to photo documentation using DermaView camera and Antera 3D camera. Antera software, by means of a multispectral analysis, compares skin color variation in before and after images, measuring the average level of melanin (average melanin concentration per unit area relative to the area selected).

| MATERIAL S AND ME THODS
All the adverse events observed or referred by the patients such as erythema, irritation, burned sensation, and skin exfoliation were recorded. Data were statistically analyzed using SPSS 20 software.
Numerical variables age, pre-and post-treatment MASI score and decrease in MASI score were presented by mean ± SD. Categorical variable, that is, gender was presented by frequency and percentage.
A paired t-test was used to verify whether the reduction in MASI score and in Antera average level of melanin were statistically significant in each of the two groups. Independent sample t-test was applied to compare the mean decrease between the two groups.
Statistical significance was set at p ≤ 0.05. significance ( Figure 2). In group A, 53.85% of patients rated the efficacy of the treatment as good, 46.15% as sufficient. The average score on the pleasantness VAS scale was 7.25 ± 0.45. In group B, 53.85% of patients rated the efficacy of the treatment as good, 38.46% as sufficient, 7.69% as insufficient and the average score on the pleasantness VAS scale was 7.5 ± 0.52. No adverse events occurred in either group.  The improvement of MASI-score was greater in group A than in group B. This difference was quite statistically significant after 6 weeks and statistically significant after 12 weeks (p-values in bold).

F I G U R E 1 Improvement of Melasma
Area Severity Index score from baseline to Week 12 in Group A and Group B.

| CON CLUS ION
The current results, even if based on a small cohort of patients evaluated over a 12 weeks period of application, indicate Politranexamide® as suitable, effective and safe therapeutic option in treating melasma.

FU N D I N G I N FO R M ATI O N
FB dermo s.r.l. provided supplies to perform this study.

CO N FLI C T O F I NTE R E S T
The authors declare no conflict of interest.

DATA AVA I L A B I L I T Y S TAT E M E N T
The data that support the findings of this study are available on request from the corresponding author. The data are not publicly available due to privacy or ethical restrictions.

E TH I C S S TATEM ENT
This study was conducted in compliance with the ethical principles originating in or derived from the Declaration of Helsinki and in compliance with the guidelines of Good Clinical Practice. All subjects provided signed informed consent.