RT Journal Article
T1 Formulation and Characterization of Epalrestat-Loaded Polysorbate 60 Cationic Niosomes for Ocular Delivery
A1 Kattar, Axel
A1 Quelle Regaldie, Ana
A1 Sánchez Piñón, Laura
A1 Concheiro Nine, Ángel Joaquín
A1 Álvarez Lorenzo, Carmen
K1 Niosome
K1 Diabetic eye
K1 HET-CAM
K1 Zebrafish
K1 Epalrestat
K1 Cationic lipid
AB The aim of this work was to develop niosomes for the ocular delivery of epalrestat, a drug that inhibits the polyol pathway and protects diabetic eyes from damage linked to sorbitol production and accumulation. Cationic niosomes were made using polysorbate 60, cholesterol, and 1,2-di-O-octadecenyl-3-trimethylammonium propane. The niosomes were characterized using dynamic light scattering, zeta-potential, and transmission electron microscopy to determine their size (80 nm; polydispersity index 0.3 to 0.5), charge (−23 to +40 mV), and shape (spherical). The encapsulation efficiency (99.76%) and the release (75% drug release over 20 days) were measured with dialysis. The ocular irritability potential (non-irritating) was measured using the Hen’s Egg Test on the Chorioallantoic Membrane model, and the blood glucose levels (on par with positive control) were measured using the gluc-HET model. The toxicity of the niosomes (non-toxic) was monitored using a zebrafish embryo model. Finally, corneal and scleral permeation was assessed with the help of Franz diffusion cells and confirmed with Raman spectroscopy. Niosomal permeation was higher than an unencapsulated drug in the sclera, and accumulation in tissues was confirmed with Raman. The prepared niosomes show promise to encapsulate and carry epalrestat through the eye to meet the need for controlled drug systems to treat the diabetic eye
PB MDPI
SN 1999-4923
YR 2023
FD 2023
LK http://hdl.handle.net/10347/30459
UL http://hdl.handle.net/10347/30459
LA eng
NO Pharmaceutics 2023, 15(4), 1247
NO This research was funded by the European Union’s Horizon 2020 research and innovation program under the Marie Sklodowska-Curie Actions (grant agreement-No 813440).
DS Minerva
RD 22 abr 2026