Micro-(MPs) and nanoparticles (NPs) have been recently studied for their application in ophthalmic drug delivery. These drug delivery systems are able to circumvent the ocular barriers that currently limit the efficacy of conventional treatments, as well as provide a more sustained release of drug, reducing the frequency of administration and increasing patient compliance. This review summarizes the recent trends in ophthalmic research from conventional treatment to the utilization of MPs and NPs as drug carriers.
Background:
The current treatment of ocular neovascularization requires frequent intravitreal
injections of anti-vascular endothelial growth factor (VEGF) agents that cause severe side effects.
Objective:
The purpose of this study is to prepare and characterize a novel nanoscale delivery system of
apatinib for ocular neovascularization.
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Methods: The optimized formulation showed a particle size of 135.04 nm, polydispersity index (PDI)
of 0.28 ± 0.07, encapsulation efficiency (EE) of 65.92%, zeta potential (ZP) of -23.70 ± 8.69 mV, and
pH of 6.49 ± 0.20. In vitro release was carried out to demonstrate a 3.13-fold increase in the
sustainability of apatinib-loaded nanoparticles versus free apatinib solution.
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Result: Cell viability and VEGFA and VEGFR2 expression were analyzed in animal retinal pigment
epithelial (ARPE-19) cells.
The results confirmed the hypothesis that apatinib nanoparticles decreased toxicity (1.36 ±
0.74 fold) and efficient VEGF inhibition (3.51 ± 0.02 fold) via VEGFR2 mediation.
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