Scholarlink

Purpose <p>Fungal infections remain a major concern due to rising incidence related to immunosuppression and chemotherapy, alongside growing antifungal resistance. Though Voriconazole (VCZ) displays robust potential against infections like <i>aspergillosis</i> and <i>candidemia</i>, its limited formulation availability highlights the need for alternative delivery approaches. Nanovesicle-based systems like novasomes (NV) have emerged as promising systems capable of enhancing delivery and overcoming current therapeutic limitations.</p> Methods <p> 2<sup>3</sup> factorial design was adopted to develop VCZ-loaded NV, with optimization based on entrapment efficiency (EE), vesicle size (VS), polydispersity index (PDI), and zeta potential (ZP), alongside evaluation of <i>in-vitro</i> release behavior, antifungal activity, Fourier transform infrared spectroscopy (FTIR), morphological characteristics, and stability of the optimized formula. The optimized formulation was incorporated into a Carbopol gel (DN1G) for <i>ex vivo</i> permeation studies.</p> &#xa0;Results <p> The formulation was optimized through a 2³ factorial design with EE%, VS, PDI, and ZP as critical responses, yielding the optimized VCZ-loaded NVs (DN1) with EE% (97.27±0.12 %), VS (256.93±4.40 nm), PDI (0.27±0.00), and ZP (-47.63±0.92 mV).<i>In-vitro</i> release studies confirmed controlled and sustained release. FTIR showed compatibility with the excipient, TEM analysis revealed spherical, non-aggregated vesicles, and stability evaluation revealed no significant alterations in selected parameters. DN1 demonstrated potent antifungal activity (MIC of 0.25 µg/mL) against <i>C. albicans,</i> and its incorporation into gel (DN1G) enhanced VCZ permeation by 1.89-fold.</p> Conclusion <p> This study highlights the potential of NV as a promising approach for VCZ, offering an effective alternative to conventional VCZ formulations, and encourages further exploration of vesicular systems for antifungal therapy.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Tailoring Voriconazole Novasomes: Formulation, Characterization, Statistical Optimization, Ex-vivo Permeation, and Microbiological Revelations

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年11月17日

查看全文
  • Khaled M. Abdel-Haleem,
  • Rehab Nabil Shamma,
  • Mahmoud M. Abd El Gawad,
  • Nermin M. Sheta

摘要

Purpose

Fungal infections remain a major concern due to rising incidence related to immunosuppression and chemotherapy, alongside growing antifungal resistance. Though Voriconazole (VCZ) displays robust potential against infections like aspergillosis and candidemia, its limited formulation availability highlights the need for alternative delivery approaches. Nanovesicle-based systems like novasomes (NV) have emerged as promising systems capable of enhancing delivery and overcoming current therapeutic limitations.

Methods

23 factorial design was adopted to develop VCZ-loaded NV, with optimization based on entrapment efficiency (EE), vesicle size (VS), polydispersity index (PDI), and zeta potential (ZP), alongside evaluation of in-vitro release behavior, antifungal activity, Fourier transform infrared spectroscopy (FTIR), morphological characteristics, and stability of the optimized formula. The optimized formulation was incorporated into a Carbopol gel (DN1G) for ex vivo permeation studies.

 Results

The formulation was optimized through a 2³ factorial design with EE%, VS, PDI, and ZP as critical responses, yielding the optimized VCZ-loaded NVs (DN1) with EE% (97.27±0.12 %), VS (256.93±4.40 nm), PDI (0.27±0.00), and ZP (-47.63±0.92 mV).In-vitro release studies confirmed controlled and sustained release. FTIR showed compatibility with the excipient, TEM analysis revealed spherical, non-aggregated vesicles, and stability evaluation revealed no significant alterations in selected parameters. DN1 demonstrated potent antifungal activity (MIC of 0.25 µg/mL) against C. albicans, and its incorporation into gel (DN1G) enhanced VCZ permeation by 1.89-fold.

Conclusion

This study highlights the potential of NV as a promising approach for VCZ, offering an effective alternative to conventional VCZ formulations, and encourages further exploration of vesicular systems for antifungal therapy.

Graphical Abstract