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Glycoside scutellarin enhanced CD-MOF anchoring for laryngeal delivery
Acta Pharmaceutica Sinica B ( IF 14.7 ) Pub Date : 2020-05-07 , DOI: 10.1016/j.apsb.2020.04.015
Kena Zhao 1, 2 , Tao Guo 2 , Caifen Wang 2 , Yong Zhou 2, 3 , Ting Xiong 2, 3 , Li Wu 2 , Xue Li 4 , Priyanka Mittal 2, 5 , Senlin Shi 1 , Ruxandra Gref 4 , Jiwen Zhang 2, 3, 5, 6
Affiliation  

It is essential to develop new carriers for laryngeal drug delivery in light of the lack of therapy in laryngeal related diseases. When the inhalable micron-sized crystals of γ-cyclodextrin metal-organic framework (CD-MOF) was utilized as dry powder inhalers (DPIs) carrier with high fine particle fraction (FPF), it was found in this research that the encapsulation of a glycoside compound, namely, scutellarin (SCU) in CD-MOF could significantly enhance its laryngeal deposition. Firstly, SCU loading into CD-MOF was optimized by incubation. Then, a series of characterizations were carried out to elucidate the mechanisms of drug loading. Finally, the laryngeal deposition rate of CD-MOF was 57.72 ± 2.19% improved by SCU, about two times higher than that of CD-MOF, when it was determined by Next Generation Impactor (NGI) at 65 L/min. As a proof of concept, pharyngolaryngitis therapeutic agent dexamethasone (DEX) had improved laryngeal deposition after being co-encapsulated with SCU in CD-MOF. The molecular simulation demonstrated the configuration of SCU in CD-MOF and its contribution to the free energy of the SCU@CD-MOF, which defined the enhanced laryngeal anchoring. In conclusion, the glycosides-like SCU could effectively enhance the anchoring of CD-MOF particles to the larynx to facilitate the treatment of laryngeal diseases.



中文翻译:

灯盏花苷糖苷增强 CD-MOF 锚定用于喉部递送

鉴于喉相关疾病缺乏治疗方法,开发新的喉部给药载体至关重要。当γ的可吸入微米级晶体-环糊精金属有机骨架(CD-MOF)被用作具有高细颗粒分数(FPF)的干粉吸入器(DPI)载体,在本研究中发现糖苷化合物,即灯盏花乙素(SCU)的包封在 CD-MOF 中可显着增强其喉部沉积。首先,通过孵育优化 SCU 加载到 CD-MOF 中。然后,进行了一系列表征以阐明载药机制。最后,当通过下一代撞击器 (NGI) 以 65 L/min 测定时,SCU 使 CD-MOF 的喉部沉积率提高了 57.72 ± 2.19%,大约是 CD-MOF 的两倍。作为概念验证,咽喉炎治疗剂地塞米松 (DEX) 在 CD-MOF 中与 SCU 共同封装后改善了喉部沉积。分子模拟证明了 SCU 在 CD-MOF 中的构型及其对 SCU@CD-MOF 自由能的贡献,这定义了增强的喉部锚定。综上所述,糖苷类SCU可有效增强CD-MOF颗粒对喉部的锚定,促进喉部疾病的治疗。

更新日期:2020-05-07
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