Student Research Committee, Babol University of Medical Sciences , Babol, Iran.
Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences , Babol, Iran.
Int J Nanomedicine. 2019 Aug 13;14:6481-6495. doi: 10.2147/IJN.S218317. eCollection 2019.
Despite the numerous pharmacological activities of quercetin, its biomedical application has been hampered, because of poor water solubility and low oral bioavailability. In the present study, we fabricated a novel form of quercetin-conjugated FeO-β-cyclodextrin (βCD) nanoparticles (NPs), and the effect of these prepared NPs was evaluated in a chronic model of epilepsy.
Quercetin-loaded NPs were prepared using an iron oxide core coated with βCD and pluronic F68 polymer. The chronic model of epilepsy was developed by intraperitoneal injection of pentylenetetrazole (PTZ) at dose of 36.5 mg/kg every second day. Quercetin or its nanoformulation at doses of 25 or 50 mg/kg were administered intraperitoneally 10 days before PTZ injections and their applications continued 1 hour before each PTZ injection. Immunostaining was performed to evaluate the neuronal density and astrocyte activation of hippocampi.
Our data showed successful fabrication of quercetin onto FeO-βCD NPs. In comparison to free quercetin, quercetin NPs markedly reduced seizure behavior, neuronal loss, and astrocyte activation in a PTZ-induced kindling model.
Overall, quercetin-FeO-βCD NPs might be regarded as an ideal therapeutic approach in epilepsy disorder.
尽管槲皮素具有众多的药理学活性，但由于其水溶性差和口服生物利用度低，其在生物医学中的应用受到了阻碍。在本研究中，我们制备了一种新型的槲皮素偶联 FeO-β-环糊精（βCD）纳米粒子（NPs），并评估了这些制备的 NPs 在慢性癫痫模型中的作用。
采用氧化亚铁核包裹βCD 和泊洛沙姆 F68 聚合物的方法制备载槲皮素 NPs。采用腹腔注射戊四氮（PTZ）（剂量为 36.5mg/kg），每隔两天注射一次的方法建立慢性癫痫模型。在 PTZ 注射前 10 天，以 25 或 50mg/kg 的剂量经腹腔给予槲皮素或其纳米制剂，并在每次 PTZ 注射前 1 小时继续给药。免疫染色用于评估海马神经元密度和星形胶质细胞激活。
我们的数据表明成功地将槲皮素偶联到了 FeO-βCD NPs 上。与游离槲皮素相比，槲皮素 NPs 明显减少了 PTZ 诱导的点燃模型中的癫痫发作行为、神经元丢失和星形胶质细胞激活。
总的来说，槲皮素-FeO-βCD NPs 可能被视为癫痫疾病的一种理想治疗方法。
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