Acta Pharmaceutica Sinica B (Sep 2020)

Glycoside scutellarin enhanced CD-MOF anchoring for laryngeal delivery

  • Kena Zhao,
  • Tao Guo,
  • Caifen Wang,
  • Yong Zhou,
  • Ting Xiong,
  • Li Wu,
  • Xue Li,
  • Priyanka Mittal,
  • Senlin Shi,
  • Ruxandra Gref,
  • Jiwen Zhang

Journal volume & issue
Vol. 10, no. 9
pp. 1709 – 1718

Abstract

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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.

Keywords