A multimodal Pepstatin A peptide-based nanoagent for the molecular imaging of P-glycoprotein in the brains of epilepsy rats

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• 作者：Xiangrong Yu^a ; ¹ ; Jianhong Wang^c ; ¹ ; Jiansheng Liu^c ; ¹ ; Shun Shen^b ; Zhonglian Cao^d ; Jiawei Pan^a ; Shuyi Zhou^a ; Zhiqing Pang^b ; ^{zqpang@fudan.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; Daoying Geng^a ; ^{daoyinggeng@163.com" class="auth_mail" title="E-mail the corresponding author} ; Jun Zhang^a ; ^{zj810828@163.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：P-glycoprotein ; Epilepsy ; Multimodal nanoagent ; Magnetic resonance imaging ; Optical imaging
• 刊名：Biomaterials
• 出版年：2016
• 出版时间：January 2016
• 年：2016
• 卷：76
• 期：Complete
• 页码：173-186
• 全文大小：3997 K

文摘

Regional overexpression of the multidrug transporter P-glycoprotein (P-gp) in epileptic brain tissues may lower antiepileptic drugs concentrations at the target site and contribute to pharmacoresistance in refractory epilepsy. However, few techniques are available to quantitate the level of P-gp expression noninvasively in vivo. In this study, we developed a nanoagent by conjugating superparamagnetic iron oxide nanoparticles with a near infrared probe and the targeting element Pepstatin A, a peptide with specific affinity for P-gp. In a rat model of epilepsy, the nanoagent was readily and selectively accumulated within epileptogenic cerebral regions, which were detectable by both magnetic resonance imaging and optical imaging modalities. This P-gp-targeted nanoagent could be used not only in the molecular imaging of P-gp expression changes in seizure-induced regional, understanding the mechanisms of P-gp disorders, and the prediction of refractory epilepsy, but also in targeted therapies with P-gp modulators.