Eplerenone nanoemulsions for treatment of hypertension. Part II: Physical stability assessment and in vivo study

Özdemir, Samet; Çelik, Burak; Sümer, Engin; Acar, Ebru Türköz; Üner, Melike

doi:10.1016/j.jddst.2018.03.014

Cited by 18 publications

(8 citation statements)

References 30 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Blood samples were added to heparinized tubes and were instantly centrifuged at 7000 rpm for 10 min. Plasma was isolated and preserved at −80 °C till further analysis (Özdemir et al., 2018 ).…”

Section: Methodsmentioning

confidence: 99%

Eplerenone nanocrystals engineered by controlled crystallization for enhanced oral bioavailability

et al. 2021

View full text Add to dashboard Cite

Section: Methodsmentioning

confidence: 99%

Eplerenone nanocrystals engineered by controlled crystallization for enhanced oral bioavailability

et al. 2021

View full text Add to dashboard Cite

“…This biphasic release pattern is beneficial therapeutically, where a rapid response of action beside a maintenance in heart attack syndrome can be achieved 66 . Furthermore, Özdemir et al, 67 evaluated the prepared EPL‐loaded NEs for subcutaneous administration and reported improved bioavailability compared to the traditional oral administration and even the subcutaneous administration of EPL solution. The subcutaneously administered NEs showed 2.97‐fold higher C max , and 2.05‐fold higher AUC 0 → ∞ 2.97 than that of EPL oral solution.…”

Section: Literature Surveymentioning

confidence: 99%

“…NE liquisolids combine the advantages of NE (higher drug solubility, protection from liver metabolism) 68 with the advantages of liquisolids (presentation of NE in form of dry highly flowable compressible powder with high drug release at the absorption site and hence enhanced bioavailability). Khames 62 prepared EPL-loaded NE liquisolids by simple manual mixing of EPL-loaded NEs (prepared by the titration spontaneous emulsification method) with Avicel/nano-sized silicone dioxide as a carrier mixture.…”

Section: Eplerenone In Ne Liquisolidsmentioning

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

View full text Add to dashboard Cite

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.

show abstract

“…Previous studies succeeded to improve its oral bioavailability and biodistribution through the formulation of EPL nano-emulsion and EPL solid dispersion (Almeida et al. 2011 ; Kendre & Chaudhari, 2017 ; Haghighi et al., 2018 ; Özdemir et al., 2018a ). EPL oral bioadhesive pellets succeeded to improve EPL solubility and hence the bioavailability (Kendre & Chaudhari, 2017 ).…”

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

View full text Add to dashboard Cite

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.

show abstract

Eplerenone nanoemulsions for treatment of hypertension. Part II: Physical stability assessment and in vivo study

Cited by 18 publications

References 30 publications

Eplerenone nanocrystals engineered by controlled crystallization for enhanced oral bioavailability

Eplerenone nanocrystals engineered by controlled crystallization for enhanced oral bioavailability

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

Contact Info

Product

Resources

About