Allyl isothiocyanate dry powder inhaler based on cyclodextrin-metal organic frameworks for pulmonary delivery

基于环糊精-金属有机框架的异硫氰酸烯丙酯干粉吸入剂,用于肺部给药

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Abstract

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, n (CD): n (AITC) = 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.

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