Related Experiment Video
Updated: Apr 7, 2026
Ocular Therapeutic Delivery and Advanced Tissue Retrieval in Adult Rats
Published on: May 23, 2025
Sorafenib nanoparticles coated with Eudragit RL for ocular drug delivery: a potential treatment for diabetic
Yu Chen1, Bo Liu2, Xiaoyu Zhang1
1School of Pharmacy, Jinzhou Medical University, Jinzhou 121001, China.
Abstract:
Diabetic retinopathy, a leading cause of vision impairment, is characterized by pathological retinal neovascularization driven by chronic hyperglycemia. Current treatments, including laser therapy and intravitreal injections, are invasive, limiting patient compliance. To address these challenges, we developed Eudragit RL (EUD)-coated hyaluronic acid (HA)-bovine serum albumin (BSA) nanoparticles (HB㊏EUD) loaded with sorafenib (SFB@(HB㊏EUD)) for targeted ocular drug delivery. The nanoparticles were prepared using an emulsification-evaporation thermal cross-linking method assisted by electrostatic interaction, yielding spherical particles of uniform size, with a particle size of 242.2 ± 1.9 nm (PDI = 0.19). The EUD coating significantly altered the nanoparticles' surface, transitioning the zeta potential from -40.6 ± 0.9 mV to -20.6 ± 0.5 mV. This change indicated a reduction in overall negative charge density and potential exposure of positively charged functional groups, facilitating electrostatic interactions with ocular mucin and prolonging corneal retention. Compared to unmodified nanoparticles, SFB@(HB㊏EUD) exhibited a 1.55-fold improvement in transcorneal transport and a 2.46-fold higher vitreous accumulation. In the chick chorioallantoic membrane assay, a 17.33% reduction in neovascularization was observed, further demonstrating the potent anti-angiogenic effects. In streptozotocin (STZ)-induced DR mice, treatment with SFB@(HB㊏EUD) via topical eye drops significantly reduced vascular leakage, preserved retinal structure, and suppressed vascular endothelial growth factor (VEGF) expression by 32.1%, outperforming non-functionalized nanoparticles. Fundus imaging and fluorescein angiography confirmed restored retinal perfusion and minimal vascular abnormalities. These findings highlight the potential of SFB@(HB㊏EUD) as a non-invasive, targeted therapy for DR, leveraging EUD's mucoadhesive properties and sorafenib's anti-angiogenic activity.
Insights
New nanoparticles offer a non-invasive treatment for diabetic retinopathy (DR). These Eudragit RL-coated nanoparticles improve drug delivery to the eye, reducing pathological neovascularization and preserving retinal structure in preclinical models.
Area of Science:
- Ophthalmology
- Nanotechnology
- Pharmacology
Background:
- Diabetic retinopathy (DR) causes vision loss through retinal neovascularization.
- Current invasive treatments for DR have limitations in patient compliance.
- Novel drug delivery systems are needed for effective and non-invasive DR therapy.
Purpose of the Study:
- To develop Eudragit RL (EUD)-coated hyaluronic acid (HA)-bovine serum albumin (BSA) nanoparticles loaded with sorafenib (SFB@(HB㊏EUD)) for targeted ocular drug delivery.
- To evaluate the mucoadhesive properties, transcorneal transport, and ocular distribution of SFB@(HB㊏EUD).
- To assess the anti-angiogenic efficacy of SFB@(HB㊏EUD) in preclinical models of DR.
Main Methods:
- Nanoparticles were synthesized using emulsification-evaporation and thermal cross-linking.
- Particle size, polydispersity index (PDI), and zeta potential were characterized.
- Transcorneal transport and vitreous accumulation were quantified.
- Anti-angiogenic effects were evaluated using the chick chorioallantoic membrane assay and in streptozotocin (STZ)-induced DR mice models.
Main Results:
- Spherical nanoparticles with a size of 242.2 ± 1.9 nm and PDI of 0.19 were obtained.
- EUD coating modified zeta potential and enhanced mucoadhesion, leading to 1.55-fold improved transcorneal transport and 2.46-fold higher vitreous accumulation.
- SFB@(HB㊏EUD) reduced neovascularization by 17.33% in the CAM assay.
- Topical application in STZ-induced DR mice significantly reduced vascular leakage, preserved retinal structure, and decreased VEGF expression by 32.1%.
Conclusions:
- SFB@(HB㊏EUD) nanoparticles demonstrate enhanced ocular drug delivery and mucoadhesive properties.
- The developed nanoparticles exhibit significant anti-angiogenic effects, reducing neovascularization and vascular leakage.
- SFB@(HB㊏EUD) represents a promising non-invasive therapeutic strategy for diabetic retinopathy.
