Apatinib-loaded nanoparticles suppress vascular endothelial growth factor-induced angiogenesis and experimental...

Area of Science:

• Ophthalmology
• Biomedical Engineering
• Nanomedicine

Background:

• Pathological angiogenesis, particularly corneal neovascularization, is a hallmark of severe ocular diseases.
• Blocking vascular endothelial growth factor (VEGF) is a validated strategy for managing corneal neovascularization.

Purpose of the Study:

• To evaluate nanoparticle-mediated delivery of apatinib, a VEGF receptor 2 inhibitor, for treating experimental corneal neovascularization.
• To assess the efficacy of apatinib-loaded human serum albumin-conjugated polyethylene glycol (HSA-PEG) nanoparticles in inhibiting angiogenesis and neovascularization.

Main Methods:

• Apatinib was encapsulated into HSA-PEG nanoparticles (Apa-HSA-PEG).
• In vitro assays assessed the inhibition of VEGF-induced endothelial cell proliferation, migration, and tube formation.
• In vivo studies utilized a rat alkali burn model for corneal neovascularization, with subconjunctival injections of Apa-HSA-PEG nanoparticles.
• In vivo nanoparticle distribution was tracked using fluorescently labeled nanoparticles.

Main Results:

• Apa-HSA-PEG nanoparticles significantly inhibited VEGF-induced endothelial cell functions in vitro.
• Subconjunctival injection of Apa-HSA-PEG nanoparticles markedly reduced corneal neovascularization in rats compared to free apatinib or PBS.
• Nanoparticles were found in the corneal stroma within 24 hours post-injection, indicating effective ocular delivery.

Conclusions:

• Apatinib-loaded HSA-PEG nanoparticles demonstrate potent anti-angiogenic and anti-neovascularization effects.
• This nanoparticle formulation offers a promising therapeutic strategy for corneal neovascularization and related ocular disorders.
• Effective corneal accumulation of nanoparticles supports their potential for localized ocular drug delivery.