Endogenous Oleoylethanolamide Crystals Loaded Lipid Nanoparticles with Enhanced Hydrophobic Drug Loading Capacity for Efficient Stroke Therapy

Wu, Shichao; Liao, Di; Li, Xi; Liu, Zeyu; Zhang, Lin; Mo, Fong Ming; Hu, Shuo; Xia, Jian; Yang, Xiangrui

doi:10.2147/ijn.s344318

Cited by 11 publications

(7 citation statements)

References 52 publications

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“…Wu et al reported a novel preparation method for efficiently loading hydrophobic drugs (endogenous high hydrophobic molecular oil ethanolamide with significant neuroprotective effects) to liposome for stroke treatment (Wu et al, 2021). The effective retention of oleoylethanolamide (OEA) in liposome could significantly enhance neuroprotective effects.…”

Section: Liposomementioning

confidence: 99%

“…The effective retention of oleoylethanolamide (OEA) in liposome could significantly enhance neuroprotective effects. Liposome could significantly improve the survival rate, behavior score, cerebral infarction volume, edema degree and spatial learning and memory ability of MCAO model rats (Wu et al, 2021). Resveratrol (NR), found in grapes and red wine, has good antioxidant and anti-inflammatory properties (Malaguarnera, 2019).…”

Section: Liposomementioning

confidence: 99%

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Advances in the research of nano delivery systems in ischemic stroke

Wang²,

Jin³

et al. 2022

Front. Bioeng. Biotechnol.

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Ischemic stroke is the most common type of cerebrovascular disease with high disability rate and mortality. The blood-brain barrier (BBB) protects the homeostasis of the brain’s microenvironment and impedes the penetration of 98% of drugs. Therefore, effective treatment requires the better drug transport across membranes and increased drug distribution. Nanoparticles are a good choice for drugs to cross BBB. The main pathways of nano delivery systems through BBB include passive diffusion, adsorption-mediated endocytosis, receptor-mediated transport, carrier-mediated transport, etc. At present, the materials used in brain-targeted delivery can be divided into natural polymer, synthetic polymers, inorganic materials and phospholipid. In this review, we first introduced several ways of nano delivery systems crossing the BBB, and then summarized their applications in ischemic stroke. Based on their potential and challenges in the treatment of ischemic stroke, new ideas and prospects are proposed for designing feasible and effective nano delivery systems.

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Section: Liposomementioning

confidence: 99%

Section: Liposomementioning

confidence: 99%

Advances in the research of nano delivery systems in ischemic stroke

Wang²,

Jin³

et al. 2022

Front. Bioeng. Biotechnol.

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“…The DLS result indicated that the OEA Liposomes possessed a hydrodynamic size of 97.6 ± 4.8 nm and a PDI of 0.193 ( Figure 2A ). Since the retention of highly hydrophobic drugs in liposomes was always problematic ( Zhigaltsev et al, 2010 ; Wu et al, 2021 ), the drug loading and loading efficiency of highly hydrophobic OEA was relatively low. The drug loading of OEA in the liposomes was 3.32% ± 0.46%.…”

Section: Resultsmentioning

confidence: 99%

OEA loaded liposomes with the neuroprotective effect for stroke therapy

Yang

2022

Front. Chem.

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With high mortality, stroke has become a serious threat to human health. Nevertheless, the strategy for stroke therapy is quite limited in the clinic till now. In this research, we prepared a novel neuroprotective nanoformulation (OEA Liposomes) via encapsulating endogenous N-oleoylethanolamine (OEA) in liposomes for intravenous administration. The formulation largely increased the solubility and bioavailability of OEA. Then the following systematic experiments stated the excellent neuroprotective effect of OEA Liposomes in vivo. The survival rate of the nanodrug group was largely increased to 75%, while that of the Middle Cerebral Artery Occlusion (MCAO) group was only 41.7%. And the severe neurological functional deficit of the MCAO rats was also significantly improved. What’s more, the OEA Liposomes could inhibit the apoptosis of neurons and the inflammation of reperfusion to a very slight level, indicating their outstanding neuroprotective effect. These results indicated that the OEA Liposomes have a great potential for clinic anti-stroke application.

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“…As a result, encapsulating OEA in a nanoparticulate structure like cubosomes, which may be utilized to target the BBB, protects it from hydrolysis and allows therapeutic amounts to reach the brain [ 36 ]. Another study by Wu et al showed that the survival rate, behavioral score, cerebral infarct volume, edema degree, spatial learning, and memory capacity of stroke-model rats could all be improved greatly using endogenous OEA crystals loaded lipid nanoparticles [ 37 ]. Further studies should be done in order to find the most effective format for OEA administration.…”

Section: Discussionmentioning

confidence: 99%

The Effect of Oleoylethanolamide (OEA) Add-On Treatment on Inflammatory, Oxidative Stress, Lipid, and Biochemical Parameters in the Acute Ischemic Stroke Patients: Randomized Double-Blind Placebo-Controlled Study

Sabahi

Ahmadi

Kazemi

et al. 2022

Oxidative Medicine and Cellular Longevity

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Background and Objective. There is a growing body of evidence for the efficacy of oleoylethanolamide (OEA) in patients with inflammatory disorders. The present randomized double-blind placebo-controlled study is aimed at evaluating the efficacy of OEA add-on treatment in patients with acute ischemic stroke (AIS). Methods. Sixty patients with a mean age of 68.60 ± 2.10 comprising 29 females (48.33%), who were admitted to an academic tertiary care facility within the first 12 hours poststroke symptoms onset or last known well (LKW), in case symptom onset time is not clear, were included in this study. AIS was confirmed based on a noncontrast head CT scan and also neurological symptoms. Patients were randomly and blindly assigned to OEA of 300 mg/day ( n = 20 ) or 600 mg/day ( n = 20 ) or placebo ( n = 20 ) in addition to the standard AIS treatment for three days. A blood sample was drawn at 12 hours from symptoms onset or LKW as the baseline followed by the second blood sample at 72 hours post symptoms onset or LKW. Blood samples were assessed for inflammatory and biochemical parameters, oxidative stress (OS) biomarkers, and lipid profile. Results. Compared to the baseline, there is a significant reduction in the urea, creatinine, triglyceride, high-density lipoprotein, cholesterol, alanine transaminase, total antioxidant capacity, malondialdehyde (MDA), total thiol groups (TTG), interleukin-6 (IL-6), and C-reactive protein levels on the follow-up blood testing in the OEA (300 mg/day) group. In patients receiving OEA (600 mg/day) treatment, there was only a significant reduction in the MDA level comparing baseline with follow-up blood testing. Also, the between-group analysis revealed a statistically significant difference between patients receiving OEA (300 mg/day) and placebo in terms of IL-6 and TTG level reduction when comparing them between baseline and follow-up blood testing. Conclusion. OEA in moderate dosage, 300 mg/day, add-on to the standard stroke treatment improves short-term inflammatory, OS, lipid, and biochemical parameters in patients with AIS. This effect might lead to a better long-term neurological prognosis.

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Endogenous Oleoylethanolamide Crystals Loaded Lipid Nanoparticles with Enhanced Hydrophobic Drug Loading Capacity for Efficient Stroke Therapy

Cited by 11 publications

References 52 publications

Advances in the research of nano delivery systems in ischemic stroke

Advances in the research of nano delivery systems in ischemic stroke

OEA loaded liposomes with the neuroprotective effect for stroke therapy

The Effect of Oleoylethanolamide (OEA) Add-On Treatment on Inflammatory, Oxidative Stress, Lipid, and Biochemical Parameters in the Acute Ischemic Stroke Patients: Randomized Double-Blind Placebo-Controlled Study

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