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Purpose <p>To develop a dual-action beeswax nanoemulsion encapsulating beta-sitosterol (BS) and cholecalciferol (VD3) for enhanced prostate bioavailability and synergistic therapy of Benign Prostatic Hyperplasia (BPH) and prostate cancer, overcoming limitations of poor solubility and rapid metabolism.</p> Methods <p>A Quality by Design (QbD)-optimized nanoemulsion was formulated using beeswax and Tween 80. Characterization included particle size, zeta potential, encapsulation efficiency (EE%), XRD, FTIR, and SEM. Molecular docking against androgen receptor (AR), PI3K, and AKT was performed. In vitro studies assessed drug release kinetics (in various pH media), antimicrobial activity (against Gram-positive/-negative bacteria <i>via</i> MIC/MBC), and cytotoxicity against PC-3 prostate cancer cells (MTT assay).</p> Results <p>The optimal formulation (F6) exhibited a small particle size (95.2 ± 5.12&#xa0;nm), high negative zeta potential (-34.70 mV), low PDI (0.18), and exceptional EE% (94.34% BS, 91.34% VD3). Molecular docking revealed strong binding affinities (BS: -7.6&#xa0;kcal/mol with AR; VD3: -7.5&#xa0;kcal/mol with AR). The nanoemulsion showed Sustained release followed non-Fickian diffusion kinetics, achieving 80.4% cumulative release of encapsulated drugs at pH 6.8 and 90.2% at pH 7 (with 0.5% SLS) over 24&#xa0;h. The nanoemulsion showed significant bactericidal activity (MBC/MIC ratio = 2) against pathogens like E. coli (MIC = 36.47&#xa0;µg/mL). Crucially, it demonstrated potent synergistic cytotoxicity against PC-3 cells (IC₅₀ = 95.61 ± 2.71&#xa0;µg/mL), significantly outperforming free BS (IC₅₀=176.55&#xa0;µg/mL) and VD3 (IC₅₀=410.07&#xa0;µg/mL).</p> Conclusion <p>This beeswax nanoemulsion successfully enhanced the stability, bioavailability, and prostate-targeted delivery of BS and VD3. The formulation demonstrated significant synergistic anticancer activity against prostate cancer cells and notable antibacterial effects, presenting a promising dual-action therapeutic strategy for managing BPH and prostate cancer with reduced systemic side effects.</p> Graphical Abstract <p></p>

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Dual-Action Beeswax Nanoemulsion for Enhanced Prostate Bioavailability and Synergistic Therapy in BPH and Prostate Cancer

  • 期刊论文

  • 发表日期：

    2025年11月4日

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  • Samar M. Mahgoub,
  • Hassan A. Rudayni,
  • Ahmed A. Allam,
  • Doaa R. I. Abdel-Gawad,
  • Abdullah S. Alawam,
  • Sahar Abdel Aleem Abdel Aziz,
  • M Ramadan Mahmoud,
  • Khaled Hesham Ezzat,
  • Ahmed G. Soliman,
  • Eman A. Mohamed,
  • Rehab Mahmoud

摘要

Purpose

To develop a dual-action beeswax nanoemulsion encapsulating beta-sitosterol (BS) and cholecalciferol (VD3) for enhanced prostate bioavailability and synergistic therapy of Benign Prostatic Hyperplasia (BPH) and prostate cancer, overcoming limitations of poor solubility and rapid metabolism.

Methods

A Quality by Design (QbD)-optimized nanoemulsion was formulated using beeswax and Tween 80. Characterization included particle size, zeta potential, encapsulation efficiency (EE%), XRD, FTIR, and SEM. Molecular docking against androgen receptor (AR), PI3K, and AKT was performed. In vitro studies assessed drug release kinetics (in various pH media), antimicrobial activity (against Gram-positive/-negative bacteria via MIC/MBC), and cytotoxicity against PC-3 prostate cancer cells (MTT assay).

Results

The optimal formulation (F6) exhibited a small particle size (95.2 ± 5.12 nm), high negative zeta potential (-34.70 mV), low PDI (0.18), and exceptional EE% (94.34% BS, 91.34% VD3). Molecular docking revealed strong binding affinities (BS: -7.6 kcal/mol with AR; VD3: -7.5 kcal/mol with AR). The nanoemulsion showed Sustained release followed non-Fickian diffusion kinetics, achieving 80.4% cumulative release of encapsulated drugs at pH 6.8 and 90.2% at pH 7 (with 0.5% SLS) over 24 h. The nanoemulsion showed significant bactericidal activity (MBC/MIC ratio = 2) against pathogens like E. coli (MIC = 36.47 µg/mL). Crucially, it demonstrated potent synergistic cytotoxicity against PC-3 cells (IC₅₀ = 95.61 ± 2.71 µg/mL), significantly outperforming free BS (IC₅₀=176.55 µg/mL) and VD3 (IC₅₀=410.07 µg/mL).

Conclusion

This beeswax nanoemulsion successfully enhanced the stability, bioavailability, and prostate-targeted delivery of BS and VD3. The formulation demonstrated significant synergistic anticancer activity against prostate cancer cells and notable antibacterial effects, presenting a promising dual-action therapeutic strategy for managing BPH and prostate cancer with reduced systemic side effects.

Graphical Abstract