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<p> Therapeutic applications of Resveratrol (RV) are hindered because of its poor aqueous solubility and rapid metabolic degradation. This study aimed to enhance RV’s solubility, stability, and antibacterial efficacy by formulating ternary inclusion complexes (TC) using sulfobutyl ether β-cyclodextrin (SBEβCD) and hydrophilic polymers, polyethylene glycol 4000 (PEG), and polyvinylpyrrolidone (PVP). Inclusion complexes were prepared via freeze-drying and characterized by FTIR, DSC, SEM, TGA, XRD, and DLS. Phase solubility and equilibrium solubility studies were conducted to determine complexation efficiency (CE), stability constants (Kₛ). <i>In vitro</i> dissolution profiles were determined in phosphate buffer (pH 7.4), and molecular docking simulations were performed to evaluate host guest interactions. The antibacterial efficacy was tested against<i>Staphylococcus aureus</i>, <i>Bacillus subtilis</i>, and<i>Escherichia coli</i> using broth microdilution and standard disc diffusion methods. The TC-PVP formulation showed highest CE (3.12) and Kₛ (1730.76 M⁻¹), achieving a favorable 1:1 molar ratio and reduced formulation bulk. The characterization confirmed formation of amorphous inclusion complexes with improved properties. <i>In vitro</i> dissolution was significantly improved (TC-PVP &gt;TC-PEG &gt;BC &gt;RV; p &lt; 0.001). Molecular docking revealed hydrogen bonding between RV and SBEβC. Antibacterial activity was markedly enhanced against <i>S. aureus</i> and <i>B. subtilis</i>, with MIC values reduced two-fold (from 312.5 to 156.25 µg/mL), and disc diffusion assays confirmed significant zones of inhibition (ZOI). Molecular docking supports the experimental data, indicating strong host-guest interactions, while the antimicrobial results underscore the translational potential of these systems for targeting Gram-positive pathogens. Accelerated stability studies confirmed that TC-PVP and TC-PEG maintained &gt;96 % RV content with no significant impurity growth after 12 weeks, indicating good chemical stability. Our study exhibited a promising potential for future antimicrobial applications due to enhanced solubility, physical stability, and broad-spectrum efficacy of RV- SBEβCD BM and TCs.</p>

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SBEβCD-Enabled Resveratrol Complexes: Ternary Systems with Hydrophilic Polymers for Enhanced Stability and Antimicrobial Efficacy

  • 期刊论文

  • 发表日期：

    2025年11月8日

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  • Teejan Ameer Abed Alahmed,
  • Thong Ke Xin,
  • Liew Lai Sheong,
  • Thevashree Rajanderan,
  • Ahmad Salawi,
  • Awaji Y Safhi,
  • Osama A Madkhali,
  • Yosif Almoshari,
  • Mohammad Intakhab Alam,
  • Fahad Y Sabei,
  • Durgaramani Sivadasan,
  • Shahnaz Majeed,
  • Farheen Sami,
  • Mohammed Tahir Ansari,
  • Md Sajid Ali

摘要

Therapeutic applications of Resveratrol (RV) are hindered because of its poor aqueous solubility and rapid metabolic degradation. This study aimed to enhance RV’s solubility, stability, and antibacterial efficacy by formulating ternary inclusion complexes (TC) using sulfobutyl ether β-cyclodextrin (SBEβCD) and hydrophilic polymers, polyethylene glycol 4000 (PEG), and polyvinylpyrrolidone (PVP). Inclusion complexes were prepared via freeze-drying and characterized by FTIR, DSC, SEM, TGA, XRD, and DLS. Phase solubility and equilibrium solubility studies were conducted to determine complexation efficiency (CE), stability constants (Kₛ). In vitro dissolution profiles were determined in phosphate buffer (pH 7.4), and molecular docking simulations were performed to evaluate host guest interactions. The antibacterial efficacy was tested againstStaphylococcus aureus, Bacillus subtilis, andEscherichia coli using broth microdilution and standard disc diffusion methods. The TC-PVP formulation showed highest CE (3.12) and Kₛ (1730.76 M⁻¹), achieving a favorable 1:1 molar ratio and reduced formulation bulk. The characterization confirmed formation of amorphous inclusion complexes with improved properties. In vitro dissolution was significantly improved (TC-PVP >TC-PEG >BC >RV; p < 0.001). Molecular docking revealed hydrogen bonding between RV and SBEβC. Antibacterial activity was markedly enhanced against S. aureus and B. subtilis, with MIC values reduced two-fold (from 312.5 to 156.25 µg/mL), and disc diffusion assays confirmed significant zones of inhibition (ZOI). Molecular docking supports the experimental data, indicating strong host-guest interactions, while the antimicrobial results underscore the translational potential of these systems for targeting Gram-positive pathogens. Accelerated stability studies confirmed that TC-PVP and TC-PEG maintained >96 % RV content with no significant impurity growth after 12 weeks, indicating good chemical stability. Our study exhibited a promising potential for future antimicrobial applications due to enhanced solubility, physical stability, and broad-spectrum efficacy of RV- SBEβCD BM and TCs.