Anhui University of Chinese Medicine, Anhui, 230000, China.
Yangtze Delta Drug Advanced Research Institute, Jiangsu, 226133, China.
AAPS PharmSciTech. 2024 May 28;25(5):117. doi: 10.1208/s12249-024-02839-1.
Eugenol (Eug) holds potential as a treatment for bacterial rhinosinusitis by nasal powder drug delivery. To stabilization and solidification of volatile Eug, herein, nasal inhalable γ-cyclodextrin metal-organic framework (γ-CD-MOF) was investigated as a carrier by gas-solid adsorption method. The results showed that the particle size of Eug loaded by γ-CD-MOF (Eug@γ-CD-MOF) distributed in the range of 10-150 μm well. In comparison to γ-CD and β-CD-MOF, γ-CD-MOF has higher thermal stability to Eug. And the intermolecular interactions between Eug and the carriers were verified by characterizations and molecular docking. Based on the bionic human nasal cavity model, Eug@γ-CD-MOF had a high deposition distribution (90.07 ± 1.58%). Compared with free Eug, the retention time Eug@γ-CD-MOF in the nasal cavity was prolonged from 5 min to 60 min. In addition, the cell viability showed that Eug@γ-CD-MOF (Eug content range 3.125-200 µg/mL) was non-cytotoxic. And the encapsulation of γ-CD-MOF could not reduce the bacteriostatic effect of Eug. Therefore, the biocompatible γ-CD-MOF could be a potential and valuable carrier for nasal drug delivery to realize solidification and nasal therapeutic effects of volatile oils.
丁香酚(Eug)通过鼻粉药物输送具有治疗细菌性鼻-鼻窦炎的潜力。为了稳定和固化挥发性 Eug,本文通过气固吸附法研究了鼻可吸入 γ-环糊精金属有机骨架(γ-CD-MOF)作为载体。结果表明,负载在 γ-CD-MOF 上的 Eug(Eug@γ-CD-MOF)的粒径分布在 10-150 μm 范围内良好。与 γ-CD 和 β-CD-MOF 相比,γ-CD-MOF 对 Eug 具有更高的热稳定性。通过特征和分子对接验证了 Eug 与载体之间的分子间相互作用。基于仿生人类鼻腔模型,Eug@γ-CD-MOF 具有高沉积分布(90.07±1.58%)。与游离 Eug 相比,Eug@γ-CD-MOF 在鼻腔中的保留时间从 5 分钟延长至 60 分钟。此外,细胞活力表明 Eug@γ-CD-MOF(Eug 含量范围 3.125-200μg/mL)无细胞毒性。并且 γ-CD-MOF 的包封不会降低 Eug 的抑菌作用。因此,生物相容性 γ-CD-MOF 可以作为鼻用药物输送的潜在有价值载体,以实现挥发性油的固化和鼻腔治疗效果。