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Dasatinib loaded nanostructured lipid carriers for effective treatment of corneal neovascularization
Qingqing Li1, Xianwei Yang, Peipei Zhang
1School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, 710061, P. R. China. zjy2011@mail.xjtu.edu.cn.
Abstract:
Corneal neovascularization (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 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 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, a key component in the angiogenesis cascade. Therefore, Dasa-NLC showed considerable promise in the treatment of CNV.
Insights
Dasatinib, encapsulated in nanostructured lipid carriers (Dasa-NLC), effectively treats corneal neovascularization (CNV). This novel formulation enhances drug solubility, reduces toxicity, and inhibits angiogenesis, offering a promising therapeutic strategy for vision impairment.
Area of Science:
- Ophthalmology
- Nanotechnology
- Pharmacology
Background:
- Corneal neovascularization (CNV) is a leading cause of vision loss globally.
- Dasatinib, a tyrosine kinase inhibitor, shows potential for CNV treatment but suffers from poor water solubility.
- Developing effective drug delivery systems is crucial for treating ocular diseases like CNV.
Purpose of the Study:
- To develop and characterize dasatinib-loaded nanostructured lipid carriers (Dasa-NLC) for corneal neovascularization treatment.
- To evaluate the solubility, ocular toxicity, and corneal penetration of Dasa-NLC.
- To assess the in vitro and in vivo anti-angiogenic efficacy of Dasa-NLC against CNV.
Main Methods:
- Dasatinib was encapsulated into nanostructured lipid carriers (NLC).
- In vitro studies involved assessing HUVEC cell proliferation, migration, and tube formation.
- In vivo efficacy was evaluated using an alkaline-induced CNV mouse model, followed by immunohistochemistry analysis.
Main Results:
- Dasa-NLC formulation achieved approximately 78 nm size with enhanced dasatinib solubility (>1220 times).
- Dasa-NLC demonstrated sustained drug release, reduced ocular toxicity, and improved corneal penetration.
- Significant inhibition of HUVEC angiogenesis and in vivo CNV development was observed, alongside reduced Src family kinase expression and activation.
Conclusions:
- Dasa-NLC formulation significantly improves dasatinib's properties for ocular delivery.
- Dasa-NLC effectively inhibits angiogenesis and shows considerable promise for treating corneal neovascularization.
- This nanocarrier system offers a viable strategy to combat CNV-related vision impairment.
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