66 DELIVERY SYSTEMS Tyrosinase inhibition (%) NeoC101™ ■ Ascorbic acid ■
120 100 80 60 40 20 0
100
*** 99
516 ± 13.1 µM 1381 ± 46.4 µM
*** 100
Microbiome modulation 15 * 13 1000 Concentration (µM)
Figure 7: Tyrosinase inhibition profiles and IC50 values of diascorbyl azelate and ascorbic acid
derived species—including mono-intermediate, ascorbic acid, and azelaic acid—reach a consistent maximum penetration depth of ~120 µm. Quantitative analysis shows comparable relative penetration levels (diascorbyl azelate: 12.06%, mono-intermediate: 12.39%, azelaic acid: 12.83%, ascorbic acid: 12.38%). Notably, all species converge at the DEJ, a key
physiological interface associated with collagen synthesis and melanin regulation, indicating synchronized penetration behaviour and sustained presence at relevant target depths.
Mechanistic insight (integrated from Raman analysis) Raman spectral signatures over the 24-hour period confirm progressive and synchronous in situ generation of ascorbic acid and azelaic acid from the parent co-drug. The combined penetration–storage–conversion behaviour supports a targeted delivery mechanism, characterized by controlled epidermal retention, sustained release, and depth-dependent bioavailability across the skin.
Multi-target clinical efficacy Supported by this precise delivery to the DEJ, diascorbyl azelate translates its high molar efficiency into broad-spectrum clinical results:
DEJ-focused collagen boost It significantly stimulates the gene expression of collagen Type I by 285%, Type IV (the core structure of the basement membrane) by 103%, and Type VII (anchoring fibrils) by 70%, fortifying the skin’s structural integrity.
Hyper-antioxidant capacity Because the C6-OH position of the ascorbic acid is protected before skin entry, the intact 2,3-enediol core yields an ultimate radical scavenging DPPH EC50 of 27 µM, making it nearly two times more potent than native ascorbic acid (49 µM).
Advanced brightening In tyrosinase inhibition assays, diascorbyl azelate achieved an IC50 of 516 µM, demonstrating approximately 2.7 times stronger inhibitory potency than pure ascorbic acid (1381 µM).
PERSONAL CARE MAGAZINE July 2026 10000 1 hour incubation
Figure 8: Comparative anti-microbiome effect of diascorbyl azelate and azelaic acid
Microbiome modulation for clearer glowing skin Traditional water-soluble actives struggle to penetrate lipid-rich microbial environments. Thanks to its amphiphilic molecule design, diascorbyl azelate successfully modulates the skin’s micro- environment with exceptional molar efficiency. At an identical 0.1% concentration, diascorbyl
azelate exhibited an 85-fold greater log reduction against C. acnes compared to native azelaic acid, an efficiency that dramatically surges to a 340-fold advantage when the dosage is slightly increased to 0.3%.
Soothing from within (UV-induced stress) In a separate in vitro evaluation targeting UV-damaged human epidermal keratinocytes, diascorbyl azelate demonstrated a profound soothing capacity. It successfully achieved up to a 100% blockade of UV-induced inflammatory cytokines, significantly suppressing both IL-6 and IL-8 secretions to protect the skin from environmental photo-stress and secondary inflammation.
The formulator’s perspective: mastering waterless polyol systems & advanced trends From a formulation chemistry standpoint, diascorbyl azelate liberates R&D from the strict aqueous pH and solubility constraints of traditional acids. Demonstrating up to 19.30% solubility in
propylene glycol and 11.00% in 1,3-Propanediol while remaining insoluble in pure lipids, it is the ultimate active for the booming ‘waterless/polyol- based’ trend.
The proven baseline: translucent polyol serums In standard stability testing, a translucent double- layer serum comprising 90.50% Propylene Glycol, 2.00% diascorbyl azelate, 2.25% Dimethicone, and 5.25% Octyldodecanol was evaluated. After three months of accelerated stability
testing at 45°C, the active HPLC assay remained remarkably high at 83.32% to 98.10%, translating to an estimated 1.5 to 2-year shelf life at room temperature. This system effectively eliminates the oxidation-induced discoloration typical of ascorbic acid and the chalky precipitation issues of azelaic acid.
Expanding into eco-friendly waterless trends: balms & pseudo- emulsions Beyond fluid serums, this unique solubility profile paves the way for highly sought-after, sustainable formats such as solid serum sticks (balms) and hybrid gels. Inspired by the viral ‘water-free multi-balm’ trend popularized by leading K-Beauty and indie brands, formulators can theoretically leverage a ‘glycol-in-oil’ matrix to deliver diascorbyl azelate. By pre-dissolving the active in a polyol phase
at room temperature and incorporating it into the wax/lipid base during the cooling phase, formulators can protect the molecule from high- temperature thermal degradation while achieving high-payload delivery in a convenient, on-the-go solid format. Additionally, for advanced textural
modifications, formulators are exploring the incorporation of silicone elastomer crosspolymers into these polyol systems. Due to the refractive index mismatch between
polar glycols and non-polar elastomers, this combination yields a luxurious, soft-focus ‘pseudo-emulsion’ appearance, all while keeping the diascorbyl azelate safely solubilized in the active glycol phase. Together, these conceptual approaches align perfectly with the modern Clean Beauty ethos, utilizing Green Chemistry to reduce water footprint while maximizing efficacy
Conclusion Guided by Corum’s core R&D philosophy, “We only give what the skin truly needs”, diascorbyl azelate represents a paradigm shift in targeted dermatological delivery. By utilizing a Co-drug mechanism to establish an active reservoir and penetrate precisely to the 120 µm DEJ layer, it eliminates the need for aggressive, high- concentration acid stacking, delivering exact cellular nourishment without irritation. Beyond its remarkable clinical efficacy,
diascorbyl azelate achieves 360° sustainability by fulfilling all 12 Principles of Green Chemistry. Synthesized via a low-temperature enzymatic process with reusable biocatalysts, the manufacturing ensures high conversion rates with absolutely no SVHC solvents, heavy metals, or
www.personalcaremagazine.com 22 *
400 350 300 250 200 150 100 50 0
340 x4 85 1 0.1% Azelaic Acid 0.1% NeoC101 x3 0.3% NeoC101
Tyrosinase inhibition (%)
Anti-Microbiome Effect
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