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Abstract This work aimed at improving the low oral bioavailability of Eplerenone along with evaluating its ocular effect in treatment of central serous chorioretinopathy (CSCR) using nano-structured lipid carrier as drug delivery system. A brief review was discussed about pharmacological aspects of Eplerenone, focusing on CSCR theories, and classification. Different Eplerenone drug delivery systems were carefully mentioned. Moving on, an inclusive survey of the PubMed database for articles and case studies up to 2020, relating CSCR patients with EPL were highlighted. As for Eplerenone nanostructured lipid carrier for oral delivery, they were prepared using emulsification solvent evaporation technique which proved to give nanometric size particles, high % entrapped drug and particles of uniform size distribution. Nanostructured lipid carriers were characterized in terms of particle size (PS), polydispersity index (PDI), zeta potential (ZP), % entrapment efficiency (% EE), and in-vitro drug release in order to screen for the optimized formulations. The selected formulation was evaluated for possible ingredients interactions using Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction, and their morphology using Transmission electron microscopy (TEM). Ex-vivo study on rabbit intestine was conducted to evaluate the permeation behavior. The selected formulation proved superior to pure aqueous Eplerenone suspension. As for Eplerenone modified nanostructured lipid carrier for ocular delivery in CSCR treatment, they were fabricated by emulsification solvent evaporation technique followed by simple modification (coating) with coating polymers under magnetic stirring. Modified carriers were characterized in (PS), polydispersity index (PDI), zeta potential (ZP), % entrapment efficiency (% EE), and viscosity measurement. The selected nano-systems were further evaluated for their in-vitro release, in-vitro irritation using hen’s egg test on chorioallantoic membrane, mucoadhesion, pH, refractive index, and TEM. Future in-vivo studies was conducted with the purpose of considering the in-vivo corneal irritation on laboratory animals through Draize test and histopathological examination, and for screening the transcorneal permeation by confocal laser microscopy. The final conclusions represent a direct approach for Eplerenone ocular delivery and replace the necessity of oral use |