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Purpose <p>Azelaic acid (AZE) is a widely used agent in acne treatment, but its poor water solubility limits its therapeutic potential. In this study, the effectiveness of azelaic acid (AZE)—a compound with limited therapeutic efficacy due to its poor water solubility—was investigated in HPMC-based hydrogel formulations, in which solubility was enhanced through complexation with hydroxypropyl-<i>β</i>-cyclodextrin (HβCD).</p> Methods <p>The developed AZE-HβCD hydrogel (F1) was evaluated in comparison with a conventional AZE hydrogel (G1) and a commercial cream formulation. In vitro antiacne activity was tested by the disk diffusion method. COX-1 and COX-2 enzyme inhibition and quantification of TNF-α levels were determined to evaluate the anti-inflammatory effectiveness. On the other hand, cytotoxicity, irritation, ex vivo penetration, and short-term stability studies were carried out.</p> Results <p>The F1 formulation exhibited significant antimicrobial activity, particularly against <i>Cutibacterium acnes</i> and <i>Staphylococcus aureus</i> compared to the control groups (at least <i>p</i> &lt; 0.01). The In vitro COX-2 inhibition rate and the 4.7-fold reduction in TNF-α levels in LPS-stimulated RAW 264.7 macrophages demonstrated the notable anti-inflammatory properties of F1. Cytotoxicity assays revealed that F1 was highly biocompatible in both human keratinocyte (HaCaT) and HEK293 cells. In ex vivo studies using Franz diffusion cells, F1 showed significantly higher AZE accumulation and skin penetration compared to the commercial product (<i>p</i> &lt; 0.05).</p> Conclusion <p>These findings suggest that HPMC-based hydrogel formulations containing AZE-HβCD may serve as promising alternatives for acne treatment by enhancing anti-inflammatory and antimicrobial efficacy as well as skin penetration.</p>

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Hydroxypropyl-β-Cyclodextrin-Enhanced Azelaic Acid Hydrogel for Acne Treatment: Evaluation of Antimicrobial, Anti-inflammatory, and Skin Penetration Properties

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年6月12日

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  • Muhammet Davut Arpa,
  • Sevde Nur Biltekin Kaleli,
  • Nilay Doğan

摘要

Purpose

Azelaic acid (AZE) is a widely used agent in acne treatment, but its poor water solubility limits its therapeutic potential. In this study, the effectiveness of azelaic acid (AZE)—a compound with limited therapeutic efficacy due to its poor water solubility—was investigated in HPMC-based hydrogel formulations, in which solubility was enhanced through complexation with hydroxypropyl-β-cyclodextrin (HβCD).

Methods

The developed AZE-HβCD hydrogel (F1) was evaluated in comparison with a conventional AZE hydrogel (G1) and a commercial cream formulation. In vitro antiacne activity was tested by the disk diffusion method. COX-1 and COX-2 enzyme inhibition and quantification of TNF-α levels were determined to evaluate the anti-inflammatory effectiveness. On the other hand, cytotoxicity, irritation, ex vivo penetration, and short-term stability studies were carried out.

Results

The F1 formulation exhibited significant antimicrobial activity, particularly against Cutibacterium acnes and Staphylococcus aureus compared to the control groups (at least p < 0.01). The In vitro COX-2 inhibition rate and the 4.7-fold reduction in TNF-α levels in LPS-stimulated RAW 264.7 macrophages demonstrated the notable anti-inflammatory properties of F1. Cytotoxicity assays revealed that F1 was highly biocompatible in both human keratinocyte (HaCaT) and HEK293 cells. In ex vivo studies using Franz diffusion cells, F1 showed significantly higher AZE accumulation and skin penetration compared to the commercial product (p < 0.05).

Conclusion

These findings suggest that HPMC-based hydrogel formulations containing AZE-HβCD may serve as promising alternatives for acne treatment by enhancing anti-inflammatory and antimicrobial efficacy as well as skin penetration.