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已发表论文
依维莫司纳米混悬剂制剂的开发与评估：增强依维莫司的递送
Authors Zeng Q , Chen J, Zhang H, Yu W , Xu H, Wang Q , Tang Z
Received 20 August 2025
Accepted for publication 15 December 2025
Published 31 December 2025 Volume 2025:20 Pages 16149—16165
DOI https://doi.org/10.2147/IJN.S562002
Checked for plagiarism Yes
Review by Single anonymous peer review
Peer reviewer comments 2
Editor who approved publication: Dr Kamakhya Misra
Qiao Zeng,1,* Jie Chen,1,* Han Zhang,1,* Wenying Yu,1,2 Haonan Xu,1 Qiao Wang,1,2 Zhan Tang1,2
1School of Pharmacy, Hangzhou Medical College, Hangzhou, Zhejiang, People’s Republic of China; 2Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province, Hangzhou Medical College, Hangzhou, Zhejiang, People’s Republic of China
*These authors contributed equally to this work
Correspondence: Qiao Wang, School of Pharmacy, Hangzhou Medical College, Hangzhou, Zhejiang, 310013, People’s Republic of China, Email wangqiao-1@163.com Zhan Tang, School of Pharmacy, Hangzhou Medical College, Hangzhou, Zhejiang, 310013, People’s Republic of China, Email tangzhan1986@126.com
Purpose: To develop everolimus-loaded nanosuspensions (EV-sus) for the in vitro and in vivo corneal neovascularization (CNV) treatment.
Results: Everolimus was encapsulated into nanosuspensions using a solvent volatilization technique. The developed nanosuspensions exhibited a drug concentration of 0.96 mg·mL− 1, an average particle size of 141.0 ± 1.0 nm, and a zeta potential of − 12.2 ± 0.4 mV. C6-labeled EV-sus uptake by Human Corneal Epithelial Cells-Transformed (HCE-T) was time-dependent, energy-dependent, and involved multiple endocytic pathways, including caveolae- and lipid raft-mediated endocytosis, clathrin-mediated endocytosis, and caveolae-mediated endocytosis. The nanosuspensions exhibited efficacy in inhibiting VEGF-induced proliferation, migration, and tube formation in Human Umbilical Vein Endothelial Cells (HUVECs). According to RT-qPCR, the in vivo CNV model showed that EV-sus effectively reduced neovascularization, decreased vascular length and area, and diminished the expression of IL-1, IL-6, MMP-9, VEGF, and TNF-α. Additionally, the rabbit eye irritation test confirmed the safety and tolerability of the formulation.
Conclusion: These findings indicate that EV-sus might be an effective therapy for corneal neovascularization. The formulation exhibits excellent biocompatibility, efficient cellular uptake, and robust anti-angiogenic activity, suggesting its suitability for ocular administration and the potential to mitigate CNV progression with minimal irritation.
Keywords: everolimus, nanosuspensions, HUVECs, HCE-Ts, corneal neovascularization
1School of Pharmacy, Hangzhou Medical College, Hangzhou, Zhejiang, People’s Republic of China; 2Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province, Hangzhou Medical College, Hangzhou, Zhejiang, People’s Republic of China
*These authors contributed equally to this work
Correspondence: Qiao Wang, School of Pharmacy, Hangzhou Medical College, Hangzhou, Zhejiang, 310013, People’s Republic of China, Email wangqiao-1@163.com Zhan Tang, School of Pharmacy, Hangzhou Medical College, Hangzhou, Zhejiang, 310013, People’s Republic of China, Email tangzhan1986@126.com
Purpose: To develop everolimus-loaded nanosuspensions (EV-sus) for the in vitro and in vivo corneal neovascularization (CNV) treatment.
Results: Everolimus was encapsulated into nanosuspensions using a solvent volatilization technique. The developed nanosuspensions exhibited a drug concentration of 0.96 mg·mL− 1, an average particle size of 141.0 ± 1.0 nm, and a zeta potential of − 12.2 ± 0.4 mV. C6-labeled EV-sus uptake by Human Corneal Epithelial Cells-Transformed (HCE-T) was time-dependent, energy-dependent, and involved multiple endocytic pathways, including caveolae- and lipid raft-mediated endocytosis, clathrin-mediated endocytosis, and caveolae-mediated endocytosis. The nanosuspensions exhibited efficacy in inhibiting VEGF-induced proliferation, migration, and tube formation in Human Umbilical Vein Endothelial Cells (HUVECs). According to RT-qPCR, the in vivo CNV model showed that EV-sus effectively reduced neovascularization, decreased vascular length and area, and diminished the expression of IL-1, IL-6, MMP-9, VEGF, and TNF-α. Additionally, the rabbit eye irritation test confirmed the safety and tolerability of the formulation.
Conclusion: These findings indicate that EV-sus might be an effective therapy for corneal neovascularization. The formulation exhibits excellent biocompatibility, efficient cellular uptake, and robust anti-angiogenic activity, suggesting its suitability for ocular administration and the potential to mitigate CNV progression with minimal irritation.
Keywords: everolimus, nanosuspensions, HUVECs, HCE-Ts, corneal neovascularization