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Research
Dasatinib loaded nanostructured lipid carriers for effective treatment of corneal neovascularization
Jiye Zhang
Xi'an Jiaotong University
Corresponding Author
ORCiD: https://orcid.org/0000-0003-4200-7043
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This work is licensed under a CC BY 4.0 License. Read Full License
Corneal neovasularization (CNV) is one of the most important causes of visual impairment worldwide. Dasatinib, a poorly water-soluble tyrosine kinase inhibitor with dual Src family kinase and platelet derived growth factor receptor inhibiting capability, has a great potential in the treatment of CNV. In this study, dasatinib was successfully encapsulated into a nanostructured lipid carrier (dasa-NLC) and the size was approximately 78 nm with a small polydispersity index. The NLC increased the solubility of dasatinib by more than 1220 times, sustained the drug release, reduced the ocular toxicity and facilitated its penetration into the cornea. Dasa-NLC significantly inhibited the proliferation, migration and tube formation of HUVEC cells, the three most important angiogenesis-related cellular changes of the CNV. Next, the in vivo anti-CNV effect of dasa-NLC was evaluated by using an alkaline burned mice CNV model, in which the development of the CNV and pathological changes of the cornea were significantly inhibited. The immunohistochemistry analysis indicated that dasa-NLC could inhibit both the expression and activation of Src family kinase. Therefore, dasa-NLC showed considerable promise in the treatment of CNV.
Keywords
Corneal neovascularization, Nanostructured lipid carriers, Dasatinib, Src family kinase
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This is a preprint. It has not completed peer review.
Research
Dasatinib loaded nanostructured lipid carriers for effective treatment of corneal neovascularization
Jiye Zhang
Xi'an Jiaotong University
Corresponding Author
ORCiD: https://orcid.org/0000-0003-4200-7043
Badges
Prescreen
This manuscript passed our Prescreen assessment
Complete author information
Appropriate declaration statements
Potential risks to human health
Prescreen
History
CURRENT STATUS: Posted
Version 1
Posted 23 Jun, 2020
No community comments so far
Metrics
Comments: 0
PDF Downloads: ...
HTML Views: ...
Subject Areas
Nanoscience
License:
This work is licensed under a CC BY 4.0 License. Read Full License
Corneal neovasularization (CNV) is one of the most important causes of visual impairment worldwide. Dasatinib, a poorly water-soluble tyrosine kinase inhibitor with dual Src family kinase and platelet derived growth factor receptor inhibiting capability, has a great potential in the treatment of CNV. In this study, dasatinib was successfully encapsulated into a nanostructured lipid carrier (dasa-NLC) and the size was approximately 78 nm with a small polydispersity index. The NLC increased the solubility of dasatinib by more than 1220 times, sustained the drug release, reduced the ocular toxicity and facilitated its penetration into the cornea. Dasa-NLC significantly inhibited the proliferation, migration and tube formation of HUVEC cells, the three most important angiogenesis-related cellular changes of the CNV. Next, the in vivo anti-CNV effect of dasa-NLC was evaluated by using an alkaline burned mice CNV model, in which the development of the CNV and pathological changes of the cornea were significantly inhibited. The immunohistochemistry analysis indicated that dasa-NLC could inhibit both the expression and activation of Src family kinase. Therefore, dasa-NLC showed considerable promise in the treatment of CNV.
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6