<p>( +)-Pinoresinol (PIN), a bioactive lignan with antifungal, anti-inflammatory, and chemo-preventive properties, faces pharmaceutical challenges due to poor aqueous solubility, instability, and irritancy. To address these limitations, we engineered sodium alginate (SA)/sodium lignosulfonate (LS) composite gel beads (SA/LS@PIN) as a multifunctional drug carrier. The beads were fabricated through Ca<sup>2</sup>⁺-mediated cross-linking, where LS integration enhanced structural stability and drug-loading capacity by modulating the gel matrix architecture. Systematic characterization revealed that LS incorporation (1–3% w/v) optimized bead morphology and improved drug entrapment efficiency (0.85% vs. 0.53% for SA-only beads). Under simulated gastrointestinal conditions, SA/LS@PIN exhibited pH-triggered release kinetics: LS delayed PIN release in gastric fluid while promoting intestinal-specific delivery via Ca<sup>2</sup>⁺-dissociation mechanisms. The composite demonstrated dual functionality, combining controlled release with antioxidant activity (26.64% DPPH radical scavenging attributed to LS-derived sulfonate and hydroxyl groups) and high biocompatibility (&gt; 80% cell viability at 3% LS). This sustainable platform integrates pH-responsive drug delivery, oxidative stress mitigation, and low cytotoxicity, offering a promising strategy for biomedical and nutraceutical applications.</p>

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Sodium alginate/sodium lignosulfonate composite gel beads for controlled release of (+)-pinoresinol: synthesis, characterization, and applications

  • Yuhao Cheng,
  • Chaoqun You,
  • Junjie Zhang,
  • Xun Li,
  • Fei Wang,
  • Yu Zhang

摘要

( +)-Pinoresinol (PIN), a bioactive lignan with antifungal, anti-inflammatory, and chemo-preventive properties, faces pharmaceutical challenges due to poor aqueous solubility, instability, and irritancy. To address these limitations, we engineered sodium alginate (SA)/sodium lignosulfonate (LS) composite gel beads (SA/LS@PIN) as a multifunctional drug carrier. The beads were fabricated through Ca2⁺-mediated cross-linking, where LS integration enhanced structural stability and drug-loading capacity by modulating the gel matrix architecture. Systematic characterization revealed that LS incorporation (1–3% w/v) optimized bead morphology and improved drug entrapment efficiency (0.85% vs. 0.53% for SA-only beads). Under simulated gastrointestinal conditions, SA/LS@PIN exhibited pH-triggered release kinetics: LS delayed PIN release in gastric fluid while promoting intestinal-specific delivery via Ca2⁺-dissociation mechanisms. The composite demonstrated dual functionality, combining controlled release with antioxidant activity (26.64% DPPH radical scavenging attributed to LS-derived sulfonate and hydroxyl groups) and high biocompatibility (> 80% cell viability at 3% LS). This sustainable platform integrates pH-responsive drug delivery, oxidative stress mitigation, and low cytotoxicity, offering a promising strategy for biomedical and nutraceutical applications.