Skin Research and Technology最新文献

Purpose: This study investigated the enhanced skin permeation and pigmentation reduction effects of an ion-pair complex formed between tranexamic acid (TXA) and mandelic acid (MA). The TXA-MA complex demonstrated superior skin permeability and greater inhibition of cytokine expression compared to TXA alone, ultimately proving more effective in reducing skin pigmentation.

Methods: After spectroscopic analysis of the TXA-MA ion-pairing complex (TXA-MA complex) structure, an in vitro skin permeation study was conducted using a Franz cell system with porcine skin. Additionally, the effect of the TXA-MA complex on UVB (ultraviolet B)-induced expression changes of inflammation-related genes (IL-1α, IL-6, IL-8, COX2) was evaluated using a human epidermal keratinocyte cell lines (HaCaT) cell model. Finally, an in vivo human study was performed to analyze the efficacy of TXA-MA in reducing actual skin pigmentation.

Results: The formation of the TXA-MA complex was confirmed through zeta-potential measurements, ¹H NMR study, and Fourier-transform infrared spectroscopy (FT-IR) spectroscopy. Skin permeation studies using porcine skin showed enhanced permeability of the TXA-MA complex compared to TXA at equivalent concentrations. In the HaCaT cell model, the TXA-MA complex exhibited greater inhibition of inflammatory markers IL-1α, IL-6, IL-8, and COX-2 expression than TXA alone. Finally, a 4-week human clinical study using ANTERA 3D imaging demonstrated that the TXA-MA complex was significantly more effective than TXA alone in reducing skin pigmentation.

Conclusion: This study successfully formed a TXA-MA complex. Compared to TXA, the TXA-MA complex showed superior effects in skin permeability, inhibition of inflammatory marker expression, and actual skin pigmentation reduction. These results suggest that the TXA-MA complex holds greater potential as an effective cosmetic ingredient for pigmentation improvement than TXA alone.

Background: Melanin synthesis plays a crucial role in skin pigmentation, and inhibiting tyrosinase, the key enzyme in melanin production, is a primary strategy for developing skin-lightening agents. This study investigates the tyrosinase inhibitory potential of CHP-9, a novel cyclopeptide, and evaluates its cytotoxicity and efficacy as a cosmetic depigmenting agent.

Methods: CHP-9 was synthesized via a solid-phase peptide synthesis strategy. The tyrosinase inhibitory activity was assessed using an enzymatic assay, while its effects on melanin content were evaluated in cultured human melanocytes. The MTT assay was performed to assess cytotoxicity across a range of CHP-9 concentrations (0.0781-10 mg/mL). Molecular docking simulations were conducted to elucidate the interaction between CHP-9 and human tyrosinase (PDB ID: 5M8M). Statistical analysis was performed using GraphPad Prism Software, and significance was determined via one-way ANOVA.

Results: CHP-9 exhibited significant tyrosinase inhibition (28.57% at 1% concentration) and reduced melanin content in treated melanocytes from 30.90 ± 1.13 to 23.51 ± 1.14 µg/mL. Cytotoxicity assays confirmed CHP-9's high biocompatibility, with cell viability exceeding 90% at concentrations up to 2.5 mg/mL. Docking studies revealed strong binding affinity between CHP-9 and key tyrosinase residues via hydrogen bonding, supporting its inhibitory mechanism.

Conclusions: CHP-9 exhibited significant tyrosinase inhibition (28.57% at 1% concentration) and reduced melanin content in melanocytes, while maintaining over 90% cell viability at effective doses. These findings suggest that CHP-9 is a safe and effective candidate for cosmetic skin-lightening applications. Further research is needed to enhance formulation stability and evaluate long-term efficacy in vivo.