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<p>This research focuses on formulating a microemulsion (ME)-based lyotropic liquid crystal (LC) system to enhance the topical delivery of apremilast for psoriasis treatment. Using Captex 300 as the oil phase and a 3:1 ratio of TPGS to Tween 80 as surfactants, pseudo-ternary phase diagrams were constructed to identify ME regions capable of transitioning into LC phases upon water addition. The optimized system formed a structurally stable LC matrix beyond 20% water content. Structural characterization by FTIR and DSC confirmed drug-excipient compatibility and the absence of degradation. Cryo-SEM imaging revealed interconnected aqueous channels indicative of mesophase development, while polarized microscopy confirmed the formation of birefringent LC phases. The in vitro drug release from the LC matrix was significantly sustained, with less than 40% release over 72&#xa0;h, in contrast to the rapid release (&gt; 90%) from the pure drug suspension. Time-lapse studies on agar confirmed gradual lateral expansion and prolonged structural integrity of the LC matrix. Drug release kinetics best fit the Higuchi and Korsmeyer–Peppas models, indicating diffusion-driven release. In vivo studies in mice demonstrated enhanced skin retention: 11.77 ± 1.42&#xa0;µg/cm<sup>2</sup> in the stratum corneum and 8.50 ± 0.94&#xa0;µg/cm<sup>2</sup> in viable layers at 12&#xa0;h—far superior to plain gel counterparts. Histological analysis showed no signs of irritation or structural damage following application, confirming excellent skin compatibility. The LC system provided a stable, biocompatible platform for controlled apremilast release and deep skin retention, positioning it as a promising topical alternative to oral administration for psoriasis management.</p> Graphical Abstract <p></p>

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Development of a microemulsion-based lyotropic liquid crystal system for enhanced topical delivery of apremilast in psoriasis

  • 期刊论文

  • 发表日期：

    2025年8月5日

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  • Sonam M. Gandhi,
  • Purva S. Patil,
  • Naitikkumar D. Trivedi,
  • Devesh U. Kapoor,
  • Omar Awad Alsaidan

摘要

This research focuses on formulating a microemulsion (ME)-based lyotropic liquid crystal (LC) system to enhance the topical delivery of apremilast for psoriasis treatment. Using Captex 300 as the oil phase and a 3:1 ratio of TPGS to Tween 80 as surfactants, pseudo-ternary phase diagrams were constructed to identify ME regions capable of transitioning into LC phases upon water addition. The optimized system formed a structurally stable LC matrix beyond 20% water content. Structural characterization by FTIR and DSC confirmed drug-excipient compatibility and the absence of degradation. Cryo-SEM imaging revealed interconnected aqueous channels indicative of mesophase development, while polarized microscopy confirmed the formation of birefringent LC phases. The in vitro drug release from the LC matrix was significantly sustained, with less than 40% release over 72 h, in contrast to the rapid release (> 90%) from the pure drug suspension. Time-lapse studies on agar confirmed gradual lateral expansion and prolonged structural integrity of the LC matrix. Drug release kinetics best fit the Higuchi and Korsmeyer–Peppas models, indicating diffusion-driven release. In vivo studies in mice demonstrated enhanced skin retention: 11.77 ± 1.42 µg/cm2 in the stratum corneum and 8.50 ± 0.94 µg/cm2 in viable layers at 12 h—far superior to plain gel counterparts. Histological analysis showed no signs of irritation or structural damage following application, confirming excellent skin compatibility. The LC system provided a stable, biocompatible platform for controlled apremilast release and deep skin retention, positioning it as a promising topical alternative to oral administration for psoriasis management.

Graphical Abstract