Glycoside scutellarin enhanced CD-MOF anchoring for laryngeal delivery

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.

Marianna Porcino , Charlotte Martineau-Corcos , Weifeng Zhu , Gilles Patriarche , Christine Péchoux , Barbara Perronne , Alia Hassan , Rainer Kümmerle , Alexandre Michelet , Anne Zehnacker-Rentien , Kena Zhao , Tao Guo , Caifen Wang , Yong Zhou , Ting Xiong , Li Wu , Xue Li (1) , Priyanka Mittal , Senlin Shi , Ruxandra Gref (1) , Jiwen Zhang

1 ISMO - Institut des Sciences Moléculaires d'Orsay

Domaines: Chimie

Marianna Porcino, Charlotte Martineau-Corcos, Weifeng Zhu, Gilles Patriarche, Christine Péchoux, et al.. Glycoside scutellarin enhanced CD-MOF anchoring for laryngeal delivery. Acta Pharmaceutica Sinica B, 2020, 10 (9), pp.1709-1718. ⟨10.1016/j.apsb.2020.04.015⟩. ⟨hal-03095979⟩