Pazopanib Loaded PLGA Nanoparticles for the Treatment of Age-related Macular Degeneration

Age-related macular degeneration (AMD) is a reason of severe vision loss worldwide. Pazopanib is a multitargeted tyrosine kinase inhibitor drug that can reduce neovascularization by mainly acting on vascular endothelial growth factor receptor (VEGFR). An intraocular injection to posterior segment of eye of anti-VEGF agent at present represents the cornerstone of therapies for AMD. However, challenges in targeting and delivering drug to eye’s posterior segment well as difficulties arising from repetitive frequent intraocular injections, which requires novel drug delivery method. In this study, pazopanib loaded PLGA‐NPs were prepared and the studied formulation had particle size of 132.1 ± 1.4 nm with PDI of 0.125 ±0.023 and 0.004± 0.13 mV for zeta potential. Entrapment efficiency was found 33.9 ± 2.5%. In vitro drug release study showed sustained drug lease. In vitro characterization in human retinal pigmented epithelial cell line described MTT assay, cellular uptake, wound scratch and anti-VEGF assay, which indicated that nanoparticles formulation had less toxicity, higher uptake, had superior anti-angiogenic potential and showed prolonged inhibition of VEGF activity. Therefore, pazopanib loaded PLGA nanoparticles were successfully developed, characterized and demonstrated its treatment of AMD.