Sun Nianxia, Zhang Min, Zhu Wentao, Song Pingping, Dai Tingting, Huang Peng, Han Zhili, Wang Dianlei
School of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China.
Anhui Province Key Laboratory of Pharmaceutical Preparation Technology and Applicaiton, Hefei, Anhui 230012, China.
iScience. 2022 Dec 30;26(1):105910. doi: 10.1016/j.isci.2022.105910. eCollection 2023 Jan 20.
In this study, allyl isothiocyanate (AITC) was prepared as the dry powder inhalation by loading cyclodextrin metal-organic framework (CD-MOF) to enhance pulmonary delivery. β-CD-MOF and γ-CD-MOF both could be used to carry AITC with the optimal loading conditions (50˚C, : = 1:7, 7 h). Compared with β-CD-MOF, γ-CD-MOF had more advantages in AITC loading due to its high drug loading and stable crystal morphology. The particle size and the mass median aerodynamic diameter of γ-CD-MOF-AITC were accorded with the aerodynamic characteristics of lung inhalation. γ-CD-MOF-AITC might be deposited effectively in the deep lung, and the release rate of AITC reached over 90% within 5 min. Meanwhile, it had good pulmonary local tolerance, permeability, and no significant toxicity. Such results indicated that γ-CD-MOF could be used as a dry powder inhaler carrier to deliver safely AITC to lung and increase its pulmonary absorption.
在本研究中，通过负载环糊精金属有机框架（CD-MOF）制备了异硫氰酸烯丙酯（AITC）干粉吸入剂，以增强肺部给药效果。β-CD-MOF和γ-CD-MOF均可用于负载AITC，最佳负载条件为（50˚C， : = 1:7，7小时）。与β-CD-MOF相比，γ-CD-MOF在负载AITC方面具有更多优势，因其载药量高且晶体形态稳定。γ-CD-MOF-AITC的粒径和质量中值空气动力学直径符合肺部吸入的空气动力学特征。γ-CD-MOF-AITC可能有效地沉积在肺深部，且AITC的释放率在5分钟内达到90%以上。同时，它具有良好的肺部局部耐受性、通透性，且无明显毒性。这些结果表明，γ-CD-MOF可作为干粉吸入剂载体，将AITC安全地递送至肺部并增加其肺部吸收。
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