Liu Ziyao, Xiang Shijun, Chen Bei, Li Jian, Zhu Dingcheng, Xu Hongjuan, Hu Shuo
Department of Nuclear Medicine, Xiangya Hospital, Central South University, Changsha, 410008, China.
Key Laboratory of Biological Nanotechnology of National Health Commission, Xiangya Hospital, Central South University, Changsha, 410008, China.
Adv Sci (Weinh). 2024 Dec;11(46):e2404717. doi: 10.1002/advs.202404717. Epub 2024 Oct 21.
Parkinson's disease (PD) is characterized by dopamine (DA) neuron loss and neuroinflammation. This study develops carrier-free nanocapsules (NCs) for targeted delivery of DA and catalase (CAT) to the PD brain, addressing both DA depletion and neuroinflammation simultaneously. The NCs are engineered by DA and 4-formylphenylboronic acid co-loading with cRGD-modified CAT (CAT-cRGD) and surface-modifying with Angiopep-2 (Ang). Ang targets the blood-brain barrier (BBB), enhancing brain delivery, while cRGD targets upregulated integrin receptors in the PD-affected BBB. The NCs showed a 1.4-fold increase in parkinsonian brain targeting efficiency compared to normal mice. In PD mice models, NCs demonstrated a stable increase in learning and memory, enhanced locomotor activity, and improved motor coordination. DA supplementation significantly enhanced dopaminergic signaling, increasing DA levels 1.8- and 3.5-fold in the striatum and substantia nigra, respectively. Additionally, delivered CAT effectively reduced neuroinflammation by mitigating endoplasmic reticulum stress, slowing disease progression, and protecting DA from oxidation. This innovative approach using PD-targeted NCs represents a synergistic strategy for PD treatment, combining symptomatic relief with disease progression intervention.
帕金森病(PD)的特征是多巴胺(DA)神经元丧失和神经炎症。本研究开发了无载体纳米胶囊(NCs),用于将DA和过氧化氢酶(CAT)靶向递送至帕金森病大脑,同时解决DA耗竭和神经炎症问题。通过将DA与4-甲酰基苯硼酸共同负载cRGD修饰的CAT(CAT-cRGD)并使用血管生成素-2(Ang)进行表面修饰来构建NCs。Ang靶向血脑屏障(BBB),增强脑部递送,而cRGD靶向帕金森病影响的BBB中上调的整合素受体。与正常小鼠相比,NCs在帕金森病大脑中的靶向效率提高了1.4倍。在帕金森病小鼠模型中,NCs显示出学习和记忆的稳定增加、运动活性增强以及运动协调性改善。补充DA显著增强了多巴胺能信号传导,使纹状体和黑质中的DA水平分别增加了1.8倍和3.5倍。此外,递送的CAT通过减轻内质网应激、减缓疾病进展以及保护DA免受氧化,有效减轻了神经炎症。这种使用靶向帕金森病的NCs的创新方法代表了一种帕金森病治疗的协同策略,将症状缓解与疾病进展干预相结合。