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用于鼻腔给药的黄芪多糖/壳聚糖微球:制备、优化、表征及药效学

Astragalus Polysaccharides/Chitosan Microspheres for Nasal Delivery: Preparation, Optimization, Characterization, and Pharmacodynamics.

作者信息

Wang Saisai, Sun Yuqing, Zhang Jingjing, Cui Xiaoming, Xu Zhilu, Ding Dejun, Zhao Limin, Li Wentong, Zhang Weifen

机构信息

School of Pharmacy, Weifang Medical University, Weifang, China.

Department of Otolaryngology, Head and Neck Surgery, Central Hospital of Zibo, Zibo, China.

出版信息

Front Pharmacol. 2020 Mar 18;11:230. doi: 10.3389/fphar.2020.00230. eCollection 2020.

DOI:10.3389/fphar.2020.00230
PMID:32256349
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7093564/
Abstract

Chitosan (CTS) constitutes a promising area in treatment of nose-related diseases as a nasal drug delivery carrier. Astragalus polysaccharide (APS) significantly attenuates eosinophils and neutrophil-dominant airway inflammation, and it has a potential pharmaceutical application in the treatment of severe asthma. The purpose of this work was to prepare APS/CTS microspheres intended for nasal drug delivery by the spray-drying method. The characteristics of APS/CTS microspheres were evaluated by a scanning electron microscope, Fourier transform infrared spectroscopy, differential scanning calorimetry, and drug release. The effect of APS/CTS microspheres on rats with allergic rhinitis (AR) was investigated by eosinophil and neutrophil counts in nasal lavage fluid. Results of SEM showed that microspheres were spherical and wrinkled. release showed that 67.48-93.76% APS was released from APS/CTS microspheres at pH 6.8 within 24 h. The effects showed that APS/CTS microspheres alleviated allergic symptoms and reduced eosinophils infiltration and the expression of interleukin-4 in the nasal mucosa tissue of rats that had no liver and kidney toxicity by hematoxylin-eosin staining observation. In conclusion, these results indicated that APS/CTS microspheres had excellent characteristics for the treatment of AR.

摘要

壳聚糖(CTS)作为一种鼻腔给药载体,在治疗鼻腔相关疾病方面具有广阔的应用前景。黄芪多糖(APS)能显著减轻以嗜酸性粒细胞和中性粒细胞为主的气道炎症,在重症哮喘治疗中具有潜在的药物应用价值。本研究旨在通过喷雾干燥法制备用于鼻腔给药的APS/CTS微球。通过扫描电子显微镜、傅里叶变换红外光谱、差示扫描量热法和药物释放实验对APS/CTS微球的特性进行了评价。通过检测鼻腔灌洗液中嗜酸性粒细胞和中性粒细胞的数量,研究了APS/CTS微球对变应性鼻炎(AR)大鼠的影响。扫描电子显微镜结果显示微球呈球形且表面有褶皱。药物释放实验表明,在pH 6.8条件下,24小时内APS/CTS微球中67.48 - 93.76%的APS被释放出来。实验结果表明,通过苏木精-伊红染色观察,APS/CTS微球可减轻大鼠的过敏症状,减少嗜酸性粒细胞浸润以及鼻黏膜组织中白细胞介素-4的表达,且对大鼠无肝肾毒性。综上所述,这些结果表明APS/CTS微球在治疗AR方面具有优异的特性。

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