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Background <p>Respiratory diseases are a major global health burden, and inhalation therapy offers efficient pulmonary targeting and therapeutic effectiveness. Dihydromyricetin (DMY), a natural flavonoid with anti-inflammatory and antiviral activities, shows limited clinical application due to poor solubility, instability, and low oral bioavailability caused by extensive first-pass metabolism.</p> Methods <p>A nebulized inhalation formulation of DMY was developed to enhance solubility, stability, and bioavailability. Pharmacokinetics were evaluated in rats following inhalation and oral administration. Safety was assessed through pulmonary function testing and histological examination of major organs.</p> Results <p>Inhalation delivery significantly improved DMY bioavailability in both lung and systemic circulation compared with oral dosing. No differences in pulmonary function or tissue morphology were observed between the inhalation and saline groups after short-term administration, suggesting preliminary safety, which warrants further investigation.</p> Conclusion <p>The nebulized DMY formulation demonstrates enhanced bioavailability, effective pulmonary targeting, and favorable safety, providing a promising therapeutic strategy for respiratory diseases.</p>

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Development and evaluation of a novel nebulized dihydromyricetin formulation: enhanced pulmonary delivery and pharmacokinetic properties

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年12月15日

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  • Kunyan Xu,
  • Jianing Yang,
  • Meng Yan,
  • Dan Li,
  • Wenli Du,
  • Jing Bai,
  • Bai Xiang

摘要

Background

Respiratory diseases are a major global health burden, and inhalation therapy offers efficient pulmonary targeting and therapeutic effectiveness. Dihydromyricetin (DMY), a natural flavonoid with anti-inflammatory and antiviral activities, shows limited clinical application due to poor solubility, instability, and low oral bioavailability caused by extensive first-pass metabolism.

Methods

A nebulized inhalation formulation of DMY was developed to enhance solubility, stability, and bioavailability. Pharmacokinetics were evaluated in rats following inhalation and oral administration. Safety was assessed through pulmonary function testing and histological examination of major organs.

Results

Inhalation delivery significantly improved DMY bioavailability in both lung and systemic circulation compared with oral dosing. No differences in pulmonary function or tissue morphology were observed between the inhalation and saline groups after short-term administration, suggesting preliminary safety, which warrants further investigation.

Conclusion

The nebulized DMY formulation demonstrates enhanced bioavailability, effective pulmonary targeting, and favorable safety, providing a promising therapeutic strategy for respiratory diseases.