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Purpose <p>Skin disorders are a widespread public health problem worldwide, affecting individuals irrespective of age. To enhance the solubility and stability of tocopherol (vitamin E) in topical formulations, Eudragit<sup>®</sup> RS100 nanoparticles were developed in the present study.</p> Methods <p>The nanoparticles were optimized using a Box–Behnken statistical design, enabling a systematic evaluation of formulation variables including polymer amount, stirring speed and organic solvent volume to achieve optimal particle size and ζ-potential. The optimized nanoparticles were characterized using Fourier-transform infrared spectroscopy and scanning electron microscopy. Their antioxidant and anti-inflammatory potentials were further assessed. Then, tocopherol-loaded nanoparticles were incorporated into a skin-compatible cream formulation which was subsequently characterized, its accelerated stability was assessed, and its cytotoxicity was finally evaluated using an LDH assay on A549 cell lines.</p> Results <p>The optimized formulation produced spherical nanoparticles with an average diameter of 157&#xa0;nm, a ζ-potential of + 55 mV and an encapsulation efficiency of 99.3 ± 0.8%. The nanoparticles exhibited strong antioxidant activity, exceeding that of butylated hydroxytoluene, with IC₅₀ value of 6.5 ± 0.2&#xa0;µg/mL and an anti-inflammatory activity comparable to that of diclofenac, with an IC₅₀ value of 245.8 ± 5.3&#xa0;µg/mL. Moreover, the developped cream maintained uniform distribution, desirable physicochemical properties (pH, spreadability, and viscosity), stability over one month under varying temperature and humidity conditions and biocompatibility.</p> Conclusion <p>Overall, the findings indicate that tocopherol-nanoparticles significantly enhance the therapeutic potential of vitamin E for managing inflammatory skin disorders.</p> Graphical Abstract <p></p>

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Response Surface Design Study for Preparation and Optimization of Polymethylmethacrylate-derived Nanoparticles for Tocopherol-based Topical Therapy of Skin Disorders

  • 期刊论文

  • 发表日期：

    2026年3月19日

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  • Narimane Lammari,
  • Marwa Boumaza,
  • Hadjira Rabti,
  • Mehdi Louaer,
  • Chawki Bensouici,
  • Ouahida Louaer,
  • Abdelhamid Elaissari,
  • Abdeslam Hassen Meniai

摘要

Purpose

Skin disorders are a widespread public health problem worldwide, affecting individuals irrespective of age. To enhance the solubility and stability of tocopherol (vitamin E) in topical formulations, Eudragit® RS100 nanoparticles were developed in the present study.

Methods

The nanoparticles were optimized using a Box–Behnken statistical design, enabling a systematic evaluation of formulation variables including polymer amount, stirring speed and organic solvent volume to achieve optimal particle size and ζ-potential. The optimized nanoparticles were characterized using Fourier-transform infrared spectroscopy and scanning electron microscopy. Their antioxidant and anti-inflammatory potentials were further assessed. Then, tocopherol-loaded nanoparticles were incorporated into a skin-compatible cream formulation which was subsequently characterized, its accelerated stability was assessed, and its cytotoxicity was finally evaluated using an LDH assay on A549 cell lines.

Results

The optimized formulation produced spherical nanoparticles with an average diameter of 157 nm, a ζ-potential of + 55 mV and an encapsulation efficiency of 99.3 ± 0.8%. The nanoparticles exhibited strong antioxidant activity, exceeding that of butylated hydroxytoluene, with IC₅₀ value of 6.5 ± 0.2 µg/mL and an anti-inflammatory activity comparable to that of diclofenac, with an IC₅₀ value of 245.8 ± 5.3 µg/mL. Moreover, the developped cream maintained uniform distribution, desirable physicochemical properties (pH, spreadability, and viscosity), stability over one month under varying temperature and humidity conditions and biocompatibility.

Conclusion

Overall, the findings indicate that tocopherol-nanoparticles significantly enhance the therapeutic potential of vitamin E for managing inflammatory skin disorders.

Graphical Abstract