Effective lightening of facial melasma during the summer with a dual regimen: A prospective, open‐label, evaluator‐blinded study

Abstract

Background Melasma is a chronic pigmentary condition that can have significant negative effects on quality of life. Vitamin C can be effective in the treatment melasma, but its delivery often proves to be challenging due to instability of the drug and subsequent cutaneous irritation at higher concentrations. Aim In this prospective, open‐label, evaluator‐blinded study, we aimed to assess the efficacy and tolerability of twice‐daily application of a novel, highly potent, non‐irritating 30% tetrahexyldecyl (THD) ascorbate serum in combination with 100% mineral‐based sunscreen in the treatment of melasma during the summer months. Patients/Methods Ten female subjects of ages ranging from 18 to 60 years underwent twice‐daily application of 30% THD ascorbate serum in combination with an anti‐aging 100% mineral tinted broad‐spectrum protection SPF 45 sunscreen moisturizer for 12 weeks during the summer months (July to September). Two blinded evaluators scored baseline and post‐treatment photographs using the Griffiths’ 10‐point scale and global aesthetic improvement scale. Results All subjects showed an improvement in hyperpigmentation with an average improvement of 33.7%. Seventy percent of subjects showed an improvement in skin tone evenness (redness), and among those subjects, the average improvement was 33.3%. The median global aesthetic improvement score was 2.0 (very much improved). Conclusion Our study demonstrated efficacy and safety in treating the pigmentary as well as vascular components of melasma with a novel 30% THD ascorbate serum and a purely mineral‐based tinted moisturizing sunscreen.

Tetrahexyldecyl Ascorbate (THDC) Degrades Rapidly under Oxidative Stress but Can Be Stabilized by Acetyl Zingerone to Enhance Collagen Production and Antioxidant Effects

“…Consistent with this, treatment of RHE with THDC alone (but not THDC + AZ) led to up-regulation of genes belonging to the "unhealthy skin signature" [52] (Figure 5A) as well as the STAT1-57 gene module (Figure 5K), which is also activated under pathological conditions such as wounding and skin cancers [53]. To our knowledge, no prior study has demonstrated a detrimental pro-inflammatory effect of topically-applied THDC as a standalone ingredient [21,[44][45][46]. It is possible that degradation of THDC leads to increased H 2 O 2 production, which contributes to an overall imbalance between antioxidant and prooxidant factors that results in downstream activation of the type I interferon pathway [66].…”

“…The topical delivery of L-Ascorbic acid (AA) has been a challenge due to its poor stability and dermal penetration. Formulations that include the AA pre-cursor tetrahexyldecyl ascorbate (THDC) have gained widespread use [21,[44][45][46], but THDC may itself lack stability within the dermal microenvironment. This study showed that THDC has limited oxygen radical absorbance capacity and undergoes rapid degradation when exposed to singlet oxygen (Figure 1D).…”

“…Topical AA delivery has been reported to improve some aspects of intrinsic skin aging [11][12][13], although stronger evidence supports a role for AA in the antioxidant-mediated prevention of extrinsic aging due to UV radiation exposure [14][15][16]. Further evidence has supported a role for topically-applied AA or AA-derivatives for treatment of wound healing and scar formation [17][18][19], allergic contact dermatitis [20], hyperpigmentation [21][22][23][24][25], atopic dermatitis [26,27], striae distensae [28], cutaneous malignancies [29][30][31], and psoriasis [32].…”

“…Tetrahexyldecyl ascorbate (THDC) is a lipid-soluble AA precursor esterified with branched chain fatty acid (2-hexyldecanoic acid), which is reported to have an improved stability and ability to penetrate the lipophilic stratum corneum [21,44]. It is essentially an AA pro-drug that can penetrate the dermis where it may then undergo intracellular enzymatic conversion to AA.…”

“…Moreover, the lipid-soluble property of THDC may facilitate its incorporation into cell membranes to confer added protective benefit [44]. When combined with other ingredients, THDC has been shown to decrease signs of photodamage, such as skin wrinkling [44,45] and reduce hyperpigmentation [21,46]. As such, THDC has become the most popular lipophilic ascorbic acid derivative in the skin care market.…”