Angiopep-Conjugated Electro-Responsive Hydrogel Nanoparticles: Therapeutic Potential for Epilepsy
Angiopep-Conjugated Electro-Responsive Hydrogel Nanoparticles: Therapeutic Potential for Epilepsy
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Angiopep 共轭电响应水凝胶纳米颗粒：治疗癫痫的潜力
DOI：
10.1002/anie.201403846
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发表时间：
2014-11-10
影响因子：
16.6
通讯作者：
Chen, Zhong
中科院分区：
文献类型：
--
作者：
Ying, Xiaoying;Wang, Yi;Chen, Zhong
安全有效的癫痫治疗需要一种能够穿透血脑屏障并随后快速释放抗癫痫药物以及时抑制神经元放电的药物递送系统。我们已经开发了电响应水凝胶纳米粒子（ERHNPs）修饰血管肽-2（ANG），以促进抗癫痫药物苯妥英钠的输送。所得ANG-ERHNP的平均直径为（102.3 +/-16.8）nm，并且在粒径和体外药物释放方面是电敏感的。ANG-ERHNPs具有易于穿透血脑屏障的特点，在中枢系统中分布较多。采用杏仁核点燃模型观察其抗癫痫作用。结果表明，ANG-ERHNPs能够将抗癫痫药物转运到大脑中，并在脑电图癫痫样异常下释放它们，从而大大提高了临床使用的现有药物的治疗指数。
A safe and effective therapy for epilepsy requires a drug delivery system that can penetrate the blood-brain barrier and subsequently release antiepileptic drugs rapidly to suppress neuronal discharges in a timely manner. We have developed electro-responsive hydrogel nanoparticles (ERHNPs) modified with angiopep-2 (ANG) to facilitate the delivery of the antiepileptic drug phenytoin sodium. The resulting ANG-ERHNPs had an average diameter of (102.3 +/- 16.8)nm and were electro-sensitive with regard to particle size and drug release invitro. ANG-ERHNPs have the characteristics of penetrate the BBB easily, resulting in a higher distribution in the central system. The improved antiepileptic effects were investigated with the amygdala kindling model. The results demonstrate that the ANG-ERHNPs were able to transport antiepileptic drugs into the brain and release them under electroencephalograph epileptiform abnormalities to greatly improve the therapeutic index of existing drugs in clinical use.