Zhou Yixian, Niu Boyi, Wu Biyuan, Luo Sulan, Fu Jintao, Zhao Yiting, Quan Guilan, Pan Xin, Wu Chuanbin
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
College of Pharmacy, Jinan University, Guangzhou 510632, China.
Acta Pharm Sin B. 2020 Dec;10(12):2404-2416. doi: 10.1016/j.apsb.2020.07.018. Epub 2020 Aug 3.
Pulmonary drug delivery has attracted increasing attention in biomedicine, and porous particles can effectively enhance the aerosolization performance and bioavailability of drugs. However, the existing methods for preparing porous particles using porogens have several drawbacks, such as the inhomogeneous and uncontrollable pores, drug leakage, and high risk of fragmentation. In this study, a series of cyclodextrin-based metal-organic framework (CD-MOF) particles containing homogenous nanopores were delicately engineered without porogens. Compared with commercial inhalation carrier, CD-MOF showed excellent aerosolization performance because of the homogenous nanoporous structure. The great biocompatibility of CD-MOF in pulmonary delivery was also confirmed by a series of experiments, including cytotoxicity assay, hemolysis ratio test, lung function evaluation, lung injury markers measurement, and histological analysis. The results of fluorescence imaging showed the high deposition rate of CD-MOF in lungs. Therefore, all results demonstrated that CD-MOF was a promising carrier for pulmonary drug delivery. This study may throw light on the nanoporous particles for effective pulmonary administration.
肺部药物递送在生物医药领域已引起越来越多的关注，多孔颗粒能够有效提高药物的雾化性能和生物利用度。然而，现有的使用致孔剂制备多孔颗粒的方法存在若干缺点，如孔隙不均匀且不可控、药物泄漏以及破碎风险高。在本研究中，一系列含有均匀纳米孔的基于环糊精的金属有机框架（CD-MOF）颗粒在无致孔剂的情况下被精心设计。与市售吸入载体相比，由于具有均匀的纳米孔结构，CD-MOF表现出优异的雾化性能。一系列实验，包括细胞毒性测定、溶血率测试、肺功能评估、肺损伤标志物测量和组织学分析，也证实了CD-MOF在肺部递送中具有良好的生物相容性。荧光成像结果显示CD-MOF在肺部的沉积率很高。因此，所有结果表明CD-MOF是一种有前途的肺部药物递送载体。本研究可能为有效的肺部给药的纳米多孔颗粒提供启示。
