期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 109, 期 2, 页码 1136-1144出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.xphs.2019.10.007
关键词
ibrutinib; nanoparticle; chitosan; sulfobutylether-beta-cyclodextrin; nanoformulation
资金
- Sichuan Science and Technology Program [2018JY0188]
- Fundamental Research Funds for the Central Universities, China [2018SCU12043]
In this study, a novel Bruton's tyrosine kinase inhibitor, ibrutinib, was loaded into chitosan/sulfobutylether-beta-cyclodextrin nanoparticles (NPs). NPs have gained high loading efficiency for the hydrophobic drug due to the inclusion of cyclodextrin. Ibrutinib-loaded NPs with an average diameter of 277.9 nm and zeta-potential of +19.1 mV were obtained after regulating several influencing factors. Electrostatic reaction between mucin and NPs indicated that the NPs had a mucoadhesive property. Kinase catalytic phosphorylation was monitored by capillary zone electrophoresis and found that chitosan/sulfobutylether-beta-cyclodextrin NPs did not weaken ibrutinib activity on the target kinase. In vitro drug release studies revealed that ibrutinib-loaded NPs exhibited a significantly slower gastric-release rate. This study applied a feasible nanocarrier for ibrutinib delivery, and the potential nanoformulation maintains drug activity and shows a sustained release property. These outcomes are helpful for the formulation exploitation of tyrosine kinase inhibitors. (c) 2020 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.
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