Effective Ocular Delivery of Eplerenone Using Nanoengineered Lipid Carriers in Rabbit Model.
chronic central serous chorioretinopathy
eplerenone
modified nanostructured lipid carriers
surface modifiers
Journal
International journal of nanomedicine
ISSN: 1178-2013
Titre abrégé: Int J Nanomedicine
Pays: New Zealand
ID NLM: 101263847
Informations de publication
Date de publication:
2021
2021
Historique:
received:
13
05
2021
accepted:
06
07
2021
entrez:
2
8
2021
pubmed:
3
8
2021
medline:
15
10
2021
Statut:
epublish
Résumé
Eplerenone (Epl) is a selective mineralocorticoid-receptor antagonist used for chronic central serous chorioretinopathy treatment. Our goal was to enhance the corneal performance of Epl-loaded nanostructured lipid carriers (NLCs) through surface modification using different coating polymers. Epl-loaded modified NLCs (Epl-loaded MNLCs) were prepared by coating the surface of Epl-loaded NLCs using different polymers, namely hyaluronic acid, chitosan oligosaccharide lactate, and hydrogenated collagen. A 3 Epl-loaded MNLCs were successfully prepared with high drug-entrapment efficiency and nanosized particles with low size distribution. Transmission electron microscopy revealed nanosized spherical particles surrounded by a coating layer of the surface modifier. The pH, refractive index, and viscosity results of the Epl-loaded MNLCs confirmed the ocular compatibility of the systems with no blurring of vision. The safety and ocular tolerance of the optimal MNLCs were confirmed using the hen's egg test on chorioallantoic membrane and by histopathological evaluation of rabbit eyes treated with the optimal systems. Confocal laser-scanning microscopy of corneal surfaces confirmed successful transcorneal permeation of the Epl-loaded MNLCs compared to the unmodified Epl-loaded NLCs, revealed by higher corneal fluorescence intensity at all time intervals. Overall, the results confirmed the potential of Epl-loaded MNLCs as a direct approach for Epl ocular delivery.
Sections du résumé
BACKGROUND
BACKGROUND
Eplerenone (Epl) is a selective mineralocorticoid-receptor antagonist used for chronic central serous chorioretinopathy treatment. Our goal was to enhance the corneal performance of Epl-loaded nanostructured lipid carriers (NLCs) through surface modification using different coating polymers.
METHODS
METHODS
Epl-loaded modified NLCs (Epl-loaded MNLCs) were prepared by coating the surface of Epl-loaded NLCs using different polymers, namely hyaluronic acid, chitosan oligosaccharide lactate, and hydrogenated collagen. A 3
RESULTS
RESULTS
Epl-loaded MNLCs were successfully prepared with high drug-entrapment efficiency and nanosized particles with low size distribution. Transmission electron microscopy revealed nanosized spherical particles surrounded by a coating layer of the surface modifier. The pH, refractive index, and viscosity results of the Epl-loaded MNLCs confirmed the ocular compatibility of the systems with no blurring of vision. The safety and ocular tolerance of the optimal MNLCs were confirmed using the hen's egg test on chorioallantoic membrane and by histopathological evaluation of rabbit eyes treated with the optimal systems. Confocal laser-scanning microscopy of corneal surfaces confirmed successful transcorneal permeation of the Epl-loaded MNLCs compared to the unmodified Epl-loaded NLCs, revealed by higher corneal fluorescence intensity at all time intervals.
CONCLUSION
CONCLUSIONS
Overall, the results confirmed the potential of Epl-loaded MNLCs as a direct approach for Epl ocular delivery.
Identifiants
pubmed: 34335024
doi: 10.2147/IJN.S319814
pii: 319814
pmc: PMC8318821
doi:
Substances chimiques
Drug Carriers
0
Lipids
0
Eplerenone
6995V82D0B
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
4985-5002Informations de copyright
© 2021 Abdelhakeem et al.
Déclaration de conflit d'intérêts
The authors report no conflicts of interest in this work.
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