Investigation of supersaturation and in vitro permeation of the poorly water soluble drug ezetimibe

Alhayali, Amani; Selo, Mohammed Ali; Ehrhardt, Carsten; Velaga, Sitaram P.

doi:10.1016/j.ejps.2018.01.047

Cited by 17 publications

(4 citation statements)

References 26 publications

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“…This demonstrate the insignificant difference in the elimination rate constant and half-life between ezetimibe suspension and NP formulation with a slight deviation towards NP formulation. Because of higher lipophilicity of ezetimibe and so its permeability to membranes [ 53 ].…”

Section: Disscusionmentioning

confidence: 99%

Development and assessment of nano drug delivery systems for combined delivery of rosuvastatin and ezetimibe

Metwally,

El-Zawahry,

Ali

et al. 2024

Korean J Physiol Pharmacol

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Worldwide, cardiovascular disease is the main cause of death, which accordingly increased by hyperlipidemia. Hyperlipidemia therapy can include lifestyle changes and medications to control cholesterol levels. Statins are the medications of the first choice for dealing with lipid abnormalities. Rosuvastatin founds to control high lipid levels by hindering liver production of cholesterol and to achieve the targeted levels of low-density lipoprotein cholesterol, another lipid lowering agents named ezetimibe may be used as an added therapy. Both rosuvastatin and ezetimibe have low bioavailability which will stand as barrier to decrease cholesterol levels, because of such depictions, formulations of this combined therapy in nanotechnology will be of a great assistance. Our study demonstrated preparations of nanoparticles of this combined therapy, showing their physical characterizations, and examined their behavior in laboratory conditions and vivo habitation. The mean particle size was uniform, polydispersity index and zeta potential of formulations were found to be in the ranges of (0.181–0.72) and (–13.4 to –6.24), respectively. Acceptable limits of entrapment efficiency were affirmed with appearance of spherical and uniform nanoparticles. In vitro testing showed a sustained release of drug exceeded 90% over 24 h. In vivo study revealed an enhanced dissolution and bioavailability from loaded nanoparticles, which was evidenced by calculated pharmacokinetic parameters using triton for hyperlipidemia induction. Stability studies were performed and assured that the formulations are kept the same up to one month. Therefore, nano formulations is a suitable transporter for combined therapy of rosuvastatin and ezetimibe with improvement in their dissolution and bioavailability.

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Section: Disscusionmentioning

confidence: 99%

Development and assessment of nano drug delivery systems for combined delivery of rosuvastatin and ezetimibe

Metwally,

El-Zawahry,

Ali

et al. 2024

Korean J Physiol Pharmacol

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“…Since ezetimibe is a lipophilic agent, it is permeable to membranes [ 39 ]. In our experiments, ezetimibe induces mitochondrial swelling and membrane potential dissipation.…”

Section: Resultsmentioning

confidence: 99%

Studies of the Formation and Stability of Ezetimibe-Cyclodextrin Inclusion Complexes

Biernacka

Ilyich

Заводник

et al. 2021

IJMS

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In the presented studies, the interactions between ezetimibe (EZE) and selected cyclodextrins were investigated. α-Cyclodextrin (αCD), β-cyclodextrin (βCD) and its modified derivatives, hydroxypropyl-β-cyclodextrin (HPβCD) and sulfobutylether-β-cyclodextrin (SBEβCD), were selected for the research. Measurements were carried out using calorimetric and spectroscopic methods. Additionally, the Hirshfeld surface and biochemical analysis were achieved. As a result of the study, the inclusion complexes with 1:1 stoichiometry were obtained. The most stable are the complexes of β-cyclodextrin and its derivatives. The comparison of βCD with its derivatives shows that the modifications have an affect on the formation of more durable and stable complexes.

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“…Although ezetimbe is well-tolerated, it is however not first-line therapy, due to a lower efficiency compared to the commonly used statins. Ezetimibe is membrane permeable (Alhayali et al, 2018), orally bioavailable, and plasma concentrations reach a maximum approx. 2 hours after intake.…”

Section: Novel Micups For Preclinical and Clinical Testingmentioning

confidence: 99%

“…A possible explanation could be differences in tissue-specific mitochondrial Ca 2+ uniporter activity (Fieni et al, 2012), mitochondrial Ca 2+ uptake pathway composition (Patron et al, 2019;Raffaello et al, 2013), or physiological adaption (Lambert et al, 2019) well tolerated, it is however not first-line therapy, due to a lower efficiency compared to the commonly used statins. Ezetimibe is membrane permeable (Alhayali et al, 2018) and orally bioavailable, and plasma concentrations reach a maximum approximately 2 h after intake. It is enterohepatically metabolized (Kosoglou et al, 2005).…”

Section: Mitochondrial Ca 2+ Uptake Enhancer Screenmentioning

confidence: 99%

Approved drugs ezetimibe and disulfiram enhance mitochondrial Ca²⁺ uptake and suppress cardiac arrhythmogenesis

Sander¹,

Feng

Schweitzer³

et al. 2021

British J Pharmacology

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Investigation of supersaturation and in vitro permeation of the poorly water soluble drug ezetimibe

Cited by 17 publications

References 26 publications

Development and assessment of nano drug delivery systems for combined delivery of rosuvastatin and ezetimibe

Development and assessment of nano drug delivery systems for combined delivery of rosuvastatin and ezetimibe

Studies of the Formation and Stability of Ezetimibe-Cyclodextrin Inclusion Complexes

Approved drugs ezetimibe and disulfiram enhance mitochondrial Ca²⁺ uptake and suppress cardiac arrhythmogenesis

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Investigation of supersaturation and in vitro permeation of the poorly water soluble drug ezetimibe

Cited by 17 publications

References 26 publications

Development and assessment of nano drug delivery systems for combined delivery of rosuvastatin and ezetimibe

Development and assessment of nano drug delivery systems for combined delivery of rosuvastatin and ezetimibe

Studies of the Formation and Stability of Ezetimibe-Cyclodextrin Inclusion Complexes

Approved drugs ezetimibe and disulfiram enhance mitochondrial Ca2+ uptake and suppress cardiac arrhythmogenesis

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Approved drugs ezetimibe and disulfiram enhance mitochondrial Ca²⁺ uptake and suppress cardiac arrhythmogenesis