Development and optimization of ezetimibe nanoparticles with improved antihyperlipidemic activity

Shukr, Marwa Hassan; Ismail, Soha; Ahmed, Samya Mahmoud

doi:10.1016/j.jddst.2018.12.001

Cited by 25 publications

(25 citation statements)

References 46 publications

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“…Cardiovascular risk evaluation has been found to be valuable in minimizing and controlling various CVDs [1]. Hyperlipidemia is a major risk factor for coronary heart disease.…”

Section: Discussionmentioning

confidence: 99%

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Antihyperlipidemic and Antioxidant Effects of Averrhoa Carambola Extract in High-Fat Diet-Fed Rats

et al. 2019

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The present study explored the antihyperlipidemic potential of a standardized methanolic extract of Averrhoa carambola (A. carambola) leaf (MEACL) in high-fat diet (HFD)-fed rats. The standardized MEACL was orally administered at different doses (250, 500, and 1000 mg/kg) to HFD-induced hyperlipidemic rats for five weeks. Serum lipid profile, body weight changes, body mass index (BMI), daily food intake, relative organ weight, and histology of the liver were evaluated. In addition, the effect of MEACL on HMG-CoA reductase and pancreatic lipase activities as well as hepatic and fecal lipids was demonstrated. MEACL supplementation reduced serum lipids in HFD-fed rats in a dose-dependent manner. Histopathological scores revealed that 1000 mg/kg MEACL restored the damage to liver tissue in hyperlipidemic rats. MEACL decreased the body mass index (BMI), atherogenic index, and hepatic cholesterol and triglycerides and increased fecal cholesterol and bile acids in HFD-fed rats. Also, MEACL ameliorated lipid peroxidation and improved antioxidant defenses in the liver of HFD-fed rats. Furthermore, HMG-CoA reductase and lipase were suppressed by MEACL. In conclusion, this study shows the potential effect of MEACL to ameliorate hyperlipidemia and oxidative stress in HFD-fed rats. It prevented hepatic lipid accumulation and exerted an inhibitory effect on HMG-CoA reductase and lipase.

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“…Cardiovascular risk evaluation has been found to be valuable in minimizing and controlling various CVDs [1]. Hyperlipidemia is a major risk factor for coronary heart disease.…”

Section: Discussionmentioning

confidence: 99%

“…Cardiovascular diseases (CVDs) are responsible for the highest burden of disease globally [1]. They are the leading causes of death, morbidity, and health expenses in developed and developing countries, accounting for around 30% of the annual global mortality and 10% of worldwide health burden [2].…”

Section: Introductionmentioning

confidence: 99%

Antihyperlipidemic and Antioxidant Effects of Averrhoa Carambola Extract in High-Fat Diet-Fed Rats

et al. 2019

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“…Total cholesterol (TC), triglycerides (TG), low-density lipoproteins (LDL-C), very low density lipoproteins (vLDL-C), and high-density lipoproteins (HDL-C) were measured using commercially available diagnostic kits (Crescent diagnostics, Jeddah, Saudi Arabia) adopting the calorimetric method (CLARIOstar ® , BMG LABTECH, SpectraMax ® M5e Microplate Reader). Atherosclerosis risk factor was calculated by computing atherogenic indices (AI) as per the following formula given in literature [32]. Furthermore, the TG/HDL-C ratio was investigated to calculate insulin resistance as reported elsewhere [33].…”

Section: Methodsmentioning

confidence: 99%

Hepatoprotective and Renoprotective Properties of Lovastatin-Loaded Ginger and Garlic Oil Nanoemulsomes: Insights into Serum Biological Parameters

et al. 2019

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Background and Objectives: Dyslipidemia is gaining much attention among healthcare professionals because of its high association with the malfunctioning of a number of normal physiological and metabolic processes in the body. Obesity is directly interconnected with dyslipidemia and is said to be a denouement of hyperlipidemia and, if left untreated, may lead to intense damage to organs that are directly involved in fat metabolism. The objective of this study was to investigate the synergistic antiobesity and anti-hyperlipidemic activities along with hepato- and renoprotective potential of nanoemulsomes (NES) of lovastatin (LTN)-loaded ginger (GR) and garlic (GL) oils. Materials and Methods: LTN nanoemulsomes co-encapsulated with GR oil and GL oil were prepared by a thin hydration technique. Eight-week-old male Wistar rats weighing 200–250 g were induced with hyperlipidemia via a high-fat diet (HFD) comprising 40% beef tallow. Body weight, serum biochemical lipid parameters, and those for liver and kidney functions, serum TC, LDL-C, vLDL-C, HDL-C, TG, atherogenic index (AI), ALT, AFT, ALP, γ-GT, total protein (TP), serum albumin and globulin ratio (A/G), serum creatinine, blood urea nitrogen (BUN) and blood urea, and histopathology of hematoxylin and eosin (H&E) stained liver and kidney sections of all aforementioned groups were examined in the treated animals. Results: Nanoemulsomes of LTN-loaded GR and GL oils provided synergistic effects with LTN, exerted better ameliorative actions in reducing serum TC, LDL-C, vLDL-C, triglycerides, and AI, and improved serum HDL-C levels. Serum ALT, AST, ALP, and γ-GT levels were in the normal range for nanoemulsome groups. H&E stained liver and kidney sections of these animals confirmed better hepatoprotective and renoprotective effects than LTN alone. Serum biochemical parameters for renal functions also claimed to be in the moderate range for nanoemulsome-treated groups. Conclusion: This study demonstrated that nanoemulsomes of LTN-loaded GR and GL oils synergistically provided better antihyperlipidemic, hepatoprotective, and renoprotective effects as compared to LTN alone.

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“…CVDs are the main cause of death in both developed and developing countries, accounting for approximately 30% of annual deaths and 10% of the disease burden worldwide. Consequently, CVDs are associated with significant nursing and healthcare expenditure (Shukr et al 2019). Hyperlipidemia, primarily defined as higher levels low-density lipoprotein (LDL-c)) Joseph et al 2020), as well as oxidative stress, defined as the increased generation of reactive oxygen species in relative to cell antioxidants are two-related mechanisms which contribute significantly to atherosclerosis and major pathways responsible for the development of CVDs (Elahi et al 2009;Li et al 2013;Surya et al Jayathilake et al 2016).…”

Section: Introductionmentioning

confidence: 99%

Antihyperlipidemic and hepatic antioxidant effects of Leek leaf methanol extract in high fat diet-fed rats

et al. 2020

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Hyperlipidemia and oxidative stress are major risk factors for the development of atherosclerosis and cardiovascular disease. This study was designed to investigate the hypolipidemic and hepatic antioxidant potentials of the methanol Leek extract (LE) in a high-fat diet (HFD)-fed rat model. Wistar rats were divided into 6 groups (n = 6/groups) as 1) control fed standard diet, 2) HFD, 3) HFD + (Atorvastatin) (20 mg/kg), and HFD + LE (100, 200, or 300 mg/kg). All treatments were administered by gavage and conducted for 6 weeks, daily. At all tested, but in a dose-independent manner, LE significantly reduced final body weights and food intake and suppressed serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST). Besides, in inhibited serum and hepatic levels of total cholesterol (TC), triglycerides (TGs), and low-density lipoprotein cholesterol (LDL-C) but increased serum and hepatic levels of high-density lipoprotein cholesterol (HDL-C). Concomitantly, LE, at all tested doses increased the activity of superoxidase dismutase (SOD) and glutathione peroxidase (GPx), increased the levels of catalase (CAT) and decreased the levels of malondialdehyde (MDA) in the livers of HFD-fed rats. In conclusion, LE exerts potent hypolipidemic and hepatic antioxidant potentials in HFD-fed rats which highlight its beneficial effects in various metabolic-related disorders.

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Development and optimization of ezetimibe nanoparticles with improved antihyperlipidemic activity

Cited by 25 publications

References 46 publications

Antihyperlipidemic and Antioxidant Effects of Averrhoa Carambola Extract in High-Fat Diet-Fed Rats

Antihyperlipidemic and Antioxidant Effects of Averrhoa Carambola Extract in High-Fat Diet-Fed Rats

Hepatoprotective and Renoprotective Properties of Lovastatin-Loaded Ginger and Garlic Oil Nanoemulsomes: Insights into Serum Biological Parameters

Antihyperlipidemic and hepatic antioxidant effects of Leek leaf methanol extract in high fat diet-fed rats

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