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<p>Jet milling is a commonly used technique in the field of ultrafine powder preparation, but it is rarely employed for drug delivery systems. This study aimed to enhance the aqueous solubility of phillyrin (PHI)—a bioactive lignan compound isloated from <i>Forsythia suspensa</i> leaves—by developing ternary solid dispersions (SDs) using dimethyl-β-cyclodextrin (DM-β-CD) and Tween 80 via different techniques.&#xa0;Phase solubility studies identified DM-β-CD as the optimal carrier. Ternary SDs with a weight ratio of PHI: DM-β-CD: Tween 80 = 1:4.75:0.25 were prepared via co-grinding (SD1), spray drying (SD2), and jet milling (SD3). Comprehensive physicochemical characterization (FT-IR, PXRD, SEM, <sup>1</sup>H NMR, DSC) revealed structural modifications. Evaluations included solubility, antioxidant activity, antibacterial, and cytotoxicity profiles. Structural analyses confirmed amorphous transformation and reduced particle size in the SDs. In PHI SD3, the water solubility of PHI was enhanced 7-fold to 1.75&#xa0;mg/mL. The SDs exhibited enhanced antioxidant and antibacterial activities relative to pure PHI. Cytotoxicity assays indicated no significant toxicity, with cell viability exceeding 70% at concentrations ≤ 200&#xa0;µg/mL. Jet milling successfully produced solvent-minimized ternary PHI solid dispersions, significantly improving solubility and bioactivity. This approach demonstrates considerable potential for optimizing the delivery of poorly soluble natural compounds such as PHI.</p>

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Comparative study of PHI ternary solid dispersions prepared by different techniques: structural characterization, solubility, and cytocompatibility

  • 期刊论文

  • 发表日期：

    2026年6月19日

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  • Guoyu Sun,
  • Hejie Wang,
  • Jie Guo,
  • Qing Wen,
  • Shenghua Zha,
  • Yuqing Liu,
  • Rongrong Tian,
  • Qingsheng Zhao

摘要

Jet milling is a commonly used technique in the field of ultrafine powder preparation, but it is rarely employed for drug delivery systems. This study aimed to enhance the aqueous solubility of phillyrin (PHI)—a bioactive lignan compound isloated from Forsythia suspensa leaves—by developing ternary solid dispersions (SDs) using dimethyl-β-cyclodextrin (DM-β-CD) and Tween 80 via different techniques. Phase solubility studies identified DM-β-CD as the optimal carrier. Ternary SDs with a weight ratio of PHI: DM-β-CD: Tween 80 = 1:4.75:0.25 were prepared via co-grinding (SD1), spray drying (SD2), and jet milling (SD3). Comprehensive physicochemical characterization (FT-IR, PXRD, SEM, 1H NMR, DSC) revealed structural modifications. Evaluations included solubility, antioxidant activity, antibacterial, and cytotoxicity profiles. Structural analyses confirmed amorphous transformation and reduced particle size in the SDs. In PHI SD3, the water solubility of PHI was enhanced 7-fold to 1.75 mg/mL. The SDs exhibited enhanced antioxidant and antibacterial activities relative to pure PHI. Cytotoxicity assays indicated no significant toxicity, with cell viability exceeding 70% at concentrations ≤ 200 µg/mL. Jet milling successfully produced solvent-minimized ternary PHI solid dispersions, significantly improving solubility and bioactivity. This approach demonstrates considerable potential for optimizing the delivery of poorly soluble natural compounds such as PHI.