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将糠酸莫米松载入环糊精金属有机框架以优化鼻腔给药

Incorporation of Mometasone Furoate into a Cyclodextrin Metal-Organic Framework to Optimize Nasal Administration.

作者信息

Li Jie, Guo Yuhua, Liu Yan, Gao Qingfang, Wang Siwen, Wu Li, Wang Caifen, Ren Xiaohong, Zhang Jiwen

机构信息

Biological and Pharmaceutical Sciences, Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.

Yangtze Delta Drug Advanced Research Institute, Nantong 226126, China.

出版信息

Pharmaceutics. 2025 Jun 17;17(6):788. doi: 10.3390/pharmaceutics17060788.

Abstract

Mometasone furoate (MF) is a topical corticosteroid used to reduce allergic and inflammation symptoms. In this study, MF was incorporated into the hydrophobic cavities of γ-cyclodextrin metal-organic frameworks (CD-MOFs) to prepare MF@MOF powders for nasal delivery. : MF@MOF particles were characterized by scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), and thermogravimetry. A transparent biomimetic model of the human nasal cavity was produced by 3D printing and used to evaluate intra-nasal depositions patterns. : Drug loading was optimized by incubating MF with a CD-MOF at a ratio of 4% for 1 h at 40 °C, and the cubic morphology and particle size of the nanoparticles were not altered using an incubation method. PXRD and FTIR analyses confirmed the successful loading of MF into the CD-MOF. Using a 3D biomimetic nasal cavity model, a 30° administration angle was found to result in reduced drug accumulation in the nasal vestibule and enhanced deposition in the respiratory and olfactory regions, compared with administration at 45°. Approximately 51% of the drug reached the respiratory zone in the model of the nasal cavity from male subjects, while almost 60% of the drug reached this zone in the model associated with female subjects. Compared with nasal sprays, nasal powder sprays had less deposition in the nasal vestibule and more deposits in the middle and inferior nasal concha. : MF@MOF is suitable for intranasal administration. Delivery of MF as a nasal powder shows potential in the treatment of chronic rhinosinusitis.

摘要

糠酸莫米松(MF)是一种用于减轻过敏和炎症症状的局部用皮质类固醇。在本研究中,MF被包封于γ-环糊精金属有机框架(CD-MOFs)的疏水腔内,以制备用于鼻腔给药的MF@MOF粉末。:通过扫描电子显微镜(SEM)、粉末X射线衍射(PXRD)、傅里叶变换红外光谱(FTIR)和热重分析对MF@MOF颗粒进行了表征。通过3D打印制作了人体鼻腔的透明仿生模型,并用于评估鼻内沉积模式。:通过在40℃下以4%的比例将MF与CD-MOF孵育1小时来优化载药量,并且使用孵育方法未改变纳米颗粒的立方形态和粒径。PXRD和FTIR分析证实MF成功负载到CD-MOF中。使用3D仿生鼻腔模型,发现与45°给药相比,30°给药角度可减少鼻腔前庭中的药物积聚,并增加在呼吸区和嗅觉区的沉积。在男性受试者鼻腔模型中,约51%的药物到达呼吸区,而在女性受试者相关模型中,近60%的药物到达该区域。与鼻喷雾剂相比,鼻用粉末喷雾剂在鼻腔前庭中的沉积较少,而在中鼻甲和下鼻甲中的沉积较多。:MF@MOF适用于鼻内给药。以鼻用粉末形式递送MF在慢性鼻-鼻窦炎的治疗中显示出潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ff42/12197233/9fe448d3194d/pharmaceutics-17-00788-g001.jpg

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