Purpose

The aim of this study was to develop a nasal powder formulation of the antifibrinolytic drug, tranexamic acid (TXA), in combination with the wound-healing agent hyaluronic acid (HA) for the local treatment of epistaxis (nose bleeding).

Methods

Formulations of TXA alone and with different concentrations of HA were freeze-dried and characterised according to their physicochemical properties. Aerosol performance was assessed to ensure nasal deposition with minimal lung deposition. Nasal epithelial cells were used to assess cytotoxicity, transport across the nasal epithelium, antioxidant, wound-healing and anti-inflammatory properties of all formulations.

Results

Formulations containing TXA and HA were produced and found to be mostly deposited in the nasal cavity (more than 90%). Formulation of TXA + 0.3%HA showed wound reduction of 29.3% when assessed in ALI culture. At this concentration, formulations also reduced ROS production in RPMI 2650, and IL-8 production in primary nasal epithelial cells. Furthermore, for formulations containing HA, the higher viscosity may lead to larger residence time in the nasal cavity.

Conclusions

Combination of TXA with HA shows promising results for the treatment of nasal epistaxis.

中文翻译：

---

氨甲环酸和透明质酸鼻粉剂用于治疗鼻出血。

目的

这项研究的目的是开发一种抗纤溶药物氨甲环酸（TXA）与伤口愈合剂透明质酸（HA）的鼻用粉剂，用于局部治疗鼻axis（鼻出血）。

方法

将单独的TXA制剂和不同浓度的HA冷冻干燥，并根据其理化性质进行表征。评估气雾剂性能以确保鼻腔沉积并减少肺部沉积。鼻上皮细胞用于评估所有制剂的细胞毒性，跨鼻上皮运输，抗氧化剂，伤口愈合和抗炎特性。

结果

产生了含有TXA和HA的制剂，发现它们大部分沉积在鼻腔中（超过90％）。当在ALI培养中评估时，TXA + 0.3％HA的配方显示伤口减少了29.3％。在此浓度下，制剂还降低了RPMI 2650中的ROS产生，以及原发性鼻上皮细胞中的IL-8产生。此外，对于含有HA的制剂，较高的粘度可能导致其在鼻腔中的停留时间更长。

结论

TXA与HA的结合显示出鼻鼻窦治疗的有希望的结果。