Formulation and Characterization of Epalrestat-Loaded Polysorbate 60 Cationic Niosomes for Ocular Delivery.
HET-CAM
cationic lipid
diabetic eye
epalrestat
niosome
zebrafish
Journal
Pharmaceutics
ISSN: 1999-4923
Titre abrégé: Pharmaceutics
Pays: Switzerland
ID NLM: 101534003
Informations de publication
Date de publication:
14 Apr 2023
14 Apr 2023
Historique:
received:
24
02
2023
revised:
30
03
2023
accepted:
11
04
2023
medline:
28
4
2023
pubmed:
28
4
2023
entrez:
28
4
2023
Statut:
epublish
Résumé
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.
Identifiants
pubmed: 37111732
pii: pharmaceutics15041247
doi: 10.3390/pharmaceutics15041247
pmc: PMC10142600
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : European Union
ID : 813440
Organisme : MCIN
ID : PID 2020-113881RB-I00
Organisme : MCIN
ID : PID2020-115121GB-I00
Organisme : Xunta de Galicia
ID : ED431C 2020/17
Organisme : European Regional Development Fund
ID : FEDER
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