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Micelle-solubilized axitinib for ocular administration in anti-neovascularization.

Authors :
Shi S
Peng F
Zheng Q
Zeng L
Chen H
Li X
Huang J
Source :
International journal of pharmaceutics [Int J Pharm] 2019 Apr 05; Vol. 560, pp. 19-26. Date of Electronic Publication: 2019 Jan 30.
Publication Year :
2019

Abstract

The development of new blood vessels is directly related to the occurrence of eye diseases. Anti-angiogenic drugs can theoretically be extended to the treatment of ophthalmic diseases. In this study, axitinib, a class of tyrosine kinase inhibitors, was loaded via the amphiphilic copolymer MPEG-PCL, improving its dispersibility in water. Axitinib-loaded micelles showed low toxicity in concentration gradient assays. Additionally, multiple doses by scratch assay confirmed that axitinib had no significant effect on normal cell migration, and biosafety test results showed good cell compatibility. After we established the corneal neovascularization model after an alkali burn in rats, the anti-angiogenic efficacy was tested, with dexamethasone as a positive control. The results showed that axitinib-loaded micelles had anti-angiogenic effects without obvious tissue toxicity. As a class of targeted tyrosine kinase inhibitors, axitinib can be used in the treatment of ocular neovascular diseases through nanocrystallization.<br /> (Copyright © 2019 Elsevier B.V. All rights reserved.)

Details

Language :
English
ISSN :
1873-3476
Volume :
560
Database :
MEDLINE
Journal :
International journal of pharmaceutics
Publication Type :
Academic Journal
Accession number :
30710659
Full Text :
https://doi.org/10.1016/j.ijpharm.2019.01.051