Eplerenone, a new treatment for an old problem: Retinitis pigmentosa with recalcitrant macular edema

Polo, R. Campos; Sánchez, C. Rubio; Guisado, D.M. García; Luque, M.

doi:10.1016/j.oftale.2017.05.012

Cited by 3 publications

(4 citation statements)

References 9 publications

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“…In this review, only studies or cases relating CSCR patients with EPL were highlighted (Figure 1 represents the count of the research articles for EPL studies in CSCR in 2013–2020). Numerous case reports and studies reported enhancement in the visual acuity and decrease/resolution of subretinal fluid level 45 (studies results are summarized in Table 2). A dose of 25–50 mg/d of oral EPL has been found to be efficient and tolerant for chronic CSCR management.…”

Section: Literature Surveymentioning

confidence: 99%

“…EPL achieves its antihypertensive and cardioprotective effect through binding to mineralocorticoid receptors and blocking the aldosterone binding, 42 resulting in increase in plasma renin and serum aldosterone with inhibition of the negative regulatory feedback of aldosterone on the renin secretion. In treatment of CSCR, EPL has the ability to act at the neuroretinal cells 35 modifying the physio‐pathological processes, such as vasoproliferative and inflammatory processes, inducing increased vascular permeability 43 upon stimulation of renin–angiotensin–aldosterone system at the ocular level 44,45 . Hyperkalaemia is the main side effect observed with treatment with EPL, so therapeutic dosage adjustment should be based on serum potassium levels 46 .…”

Section: Pharmacological Aspects Of Eplerenonementioning

confidence: 99%

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Eplerenone repurposing in management of chorioretinopathy: Mechanism, nanomedicine‐based delivery applications and future trends

Abdelhakeem

El-Nabarawi

Shamma

2022

Brit J Clinical Pharma

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Chronic central serous chorioretinopathy (CSCR) is an ocular threatening disease, a common cause of central vision loss, affecting the posterior pole of the eye.Eplerenone (EPL) is a selective mineralocorticoid receptor antagonist that is primarily used to treat hypertension. Recently, it has shown many benefits in modifying the physio-pathological processes occurring upon stimulation of renin-angiotensinaldosterone system at the ocular level. In CSCR treatment, several clinical studies and case reports prove the efficacy and safety of EPL. However, setbacks for such studies include a relatively small number of participants and short follow-up periods. This review article is intended to describe theories about the nature and classification of CSCR and recapitulate EPL therapeutic benefits as selective mineralocorticoid receptor antagonist in the treatment of CSCR. Furthermore, we survey the literature on clinical studies discussing the results of use of EPL in treatment of CSCR. In addition, EPL therapeutic formulations that have been developed are described, and future potential delivery systems will be suggested.

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Section: Literature Surveymentioning

confidence: 99%

Section: Pharmacological Aspects Of Eplerenonementioning

confidence: 99%

Eplerenone repurposing in management of chorioretinopathy: Mechanism, nanomedicine‐based delivery applications and future trends

Abdelhakeem

El-Nabarawi

Shamma

2022

Brit J Clinical Pharma

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“…EPL is analogues to the commonly used diuretic spironolactone, with an increased mineralocorticoid receptor selectivity and higher affinity (Cook et al., 2003 ; Yang and Eliott, 2017 ). It has the ability to act at neuroretinal cell types (Zhao et al., 2010 ) modifying the above-mentioned physiopathological processes (Yang and Eliott, 2017 ; Campos Polo et al., 2018 ; Chatziralli et al., 2018 ).…”

Section: Introductionmentioning

confidence: 99%

Lipid-based nano-formulation platform for eplerenone oral delivery as a potential treatment of chronic central serous chorioretinopathy: in-vitro optimization and ex-vivo assessment

2021

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Purpose Eplerenone (EPL) is a selective mineralocorticoid receptor antagonist used for treatment of chronic central serous chorioretinopathy which characterized by accumulation of subretinal fluid causing a localized area of retinal detachment. unfortunately, EPL suffers from poor oral bioavailability due to poor aqueous solubility in addition to high hepatic first pass metabolism. Method Aiming to improve its oral bioavailability, EPL-loaded nanostructured lipid carriers (NLCs) were prepared by the emulsification solvent evaporation method and in-vitro evaluated for particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (EE%). A D-optimal design was used for study the effect of liquid lipid to solid lipid ratio, surfactant type and percentage on PS, PDI, EE%, and for data optimization. The optimized EPL-loaded NLCs system was further evaluated using in-vitro drug release and ex-vivo permeation studies through rabbit intestine in comparison to EPL aqueous suspension. The physicochemical properties of the drug in the optimized system were further examined using FT-IR and X-ray diffraction studies. Results The resultant NLCs showed small PS (100.85–346.60 nm), homogenous distribution (0.173–0.624), negatively charged particles (ZP −20.20 to −36.75 mV), in addition to EE% (34.31–70.64%). The optimized EPL-loaded NLCs system with a desirability value of 0.905 was suggested through the Design expert ® software, containing liquid to solid lipid ratio (2:1) in presence of 0.43%w/v Pluronic ® F127 as a surfactant. The optimized EPL-loaded NLCs system showed a PS of 134 nm and PDI of 0.31, in addition to high EE% (76 ± 6.56%w/w), and ZP (-32.37 mV). The ex-vivo permeation study showed two-fold higher drug permeation through rabbit intestine compared to that from the aqueous drug suspension after 24 h, confirming the ability of optimized EPL-loaded NLCs system as successful oral targeting delivery carrier. Conclusion Our results pave the way for a new oral nanotherapeutic approach toward CSCR treatment. In-vivo study is currently under investigation.

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“…8 Epl has the ability to act on neuroretinal cell types, 9 modifying the a forementioned physiopathological processes. [10][11][12] Topical formulations to treat intraocular diseases face obstacles, limiting their delivery, including precorneal loss factors (eg, tear dynamics, transient residence time in the cul-de-sac, and relative impermeability of the corneal epithelial membrane), resulting in poor bioavailability. 13 In addition, the residence time of the drug on the corneal surface and drug penetration across the cornea still needs to be increased.…”

Section: Introductionmentioning

confidence: 99%

Effective Ocular Delivery of Eplerenone Using Nanoengineered Lipid Carriers in Rabbit Model

Abdelhakeem¹,

El-Nabarawi²,

Shamma³

2021

IJN

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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: 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 1 ×4 1 full factorial design was used to evaluate the effect of the surface modification on the properties of the prepared systems. Selected optimal Epl-loaded MNLCs were further evaluated for in vitro drug release, morphology, pH, rheological properties, corneal mucoadhesion, irritation, and penetration. 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: Overall, the results confirmed the potential of Epl-loaded MNLCs as a direct approach for Epl ocular delivery.

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Eplerenone, a new treatment for an old problem: Retinitis pigmentosa with recalcitrant macular edema

Cited by 3 publications

References 9 publications

Eplerenone repurposing in management of chorioretinopathy: Mechanism, nanomedicine‐based delivery applications and future trends

Eplerenone repurposing in management of chorioretinopathy: Mechanism, nanomedicine‐based delivery applications and future trends

Lipid-based nano-formulation platform for eplerenone oral delivery as a potential treatment of chronic central serous chorioretinopathy: in-vitro optimization and ex-vivo assessment

Effective Ocular Delivery of Eplerenone Using Nanoengineered Lipid Carriers in Rabbit Model

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