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<p>Hyaluronic acid (HA) is a biocompatible, mucosal-interacting polysaccharide that offers unique advantages for oral drug delivery. Chemical modification with hydrophobic groups transforms HA into an amphiphilic polymer capable of self-assembly and encapsulation of poorly soluble compounds. In this work, we developed an oral delivery system based on oleyl-hyaluronate&#xa0;(O-HA) for coenzyme Q10 (CoQ10), a lipophilic antioxidant with limited solubility and low bioavailability. The coenzyme Q10-loaded oleyl-hyaluronate nanoparticles (O-HAQ10) were prepared using a multistep solvent evaporation method, achieving a high CoQ10 loading of up to 13.8&#xa0;g/L and an encapsulation efficiency typically exceeding 90%. Crucially, this platform achieved an exceptionally high drug loading capacity, substantially minimizing the surfactant burden typically required to stabilize highly lipophilic payloads. The nanoparticles exhibited nanoscale dimensions (200–300 nm), as confirmed by dynamic light scattering (DLS) and scanning electron microscopy (SEM). Comprehensive in vitro evaluation confirmed robust cytocompatibility with the Caco-2 human intestinal epithelial cell line. Furthermore, studies on porcine intestine demonstrated significantly enhanced mucosal accumulation compared to commercial liposomal and oil-based formulations, even following simulated gastric exposure. In vivo pharmacokinetic evaluation in mice confirmed a 72% increase in systemic bioavailability relative to the clinical gold-standard oil-based control. These findings highlight the potential of hydrophobically modified HA as a highly efficient, versatile platform for the peroral delivery of poorly soluble bioactives.</p> Graphical Abstract <p></p>

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Oleyl-hyaluronate nanoparticles for enhanced peroral bioavailability of encapsulated Coenzyme Q10

  • 期刊论文

  • 发表日期：

    2026年4月7日

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  • Martin Juhaščik,
  • František Fiala,
  • Dagmar Čožíková,
  • Hana Vágnerová,
  • Jaromír Kulhánek,
  • Anna Kocurková,
  • Matěj Šimek,
  • Anna Stránská,
  • Lukáš Kubala,
  • František Ondreáš

摘要

Hyaluronic acid (HA) is a biocompatible, mucosal-interacting polysaccharide that offers unique advantages for oral drug delivery. Chemical modification with hydrophobic groups transforms HA into an amphiphilic polymer capable of self-assembly and encapsulation of poorly soluble compounds. In this work, we developed an oral delivery system based on oleyl-hyaluronate (O-HA) for coenzyme Q10 (CoQ10), a lipophilic antioxidant with limited solubility and low bioavailability. The coenzyme Q10-loaded oleyl-hyaluronate nanoparticles (O-HAQ10) were prepared using a multistep solvent evaporation method, achieving a high CoQ10 loading of up to 13.8 g/L and an encapsulation efficiency typically exceeding 90%. Crucially, this platform achieved an exceptionally high drug loading capacity, substantially minimizing the surfactant burden typically required to stabilize highly lipophilic payloads. The nanoparticles exhibited nanoscale dimensions (200–300 nm), as confirmed by dynamic light scattering (DLS) and scanning electron microscopy (SEM). Comprehensive in vitro evaluation confirmed robust cytocompatibility with the Caco-2 human intestinal epithelial cell line. Furthermore, studies on porcine intestine demonstrated significantly enhanced mucosal accumulation compared to commercial liposomal and oil-based formulations, even following simulated gastric exposure. In vivo pharmacokinetic evaluation in mice confirmed a 72% increase in systemic bioavailability relative to the clinical gold-standard oil-based control. These findings highlight the potential of hydrophobically modified HA as a highly efficient, versatile platform for the peroral delivery of poorly soluble bioactives.

Graphical Abstract