Neurological disorders are undoubtedly among the most alarming diseases humans might face. In treatment of neurological disorders, the blood‐brain barrier (BBB) is a challenging obstacle preventing drug penetration into the brain. Advances in dendrimer chemistry for central nervous system (CNS) treatments are presented here. A poly(amido)amine (PAMAM) dendrimer bioconjugate with a streptavidin adapter for the attachment of dendrons or any biotinylated drug is constructed. In vitro studies on porcine or murine models and in vivo mouse studies are performed and reveal the permeation of dendronized streptavidin (DSA) into the CNS. The bioconjugate is taken up mainly by the caveolae pathway and transported across the BBB via transcytosis escaping from lysosomes. After transcytosis DSA are delivered to astrocytes and neurons. Furthermore, DSA offer high biocompatibility in vitro and in vivo. In summary, a new strategy for implementing therapeutic PAMAM function as well as drug delivery in neuropathology is presented here.

中文翻译：

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多功能树状大分子蛋白生物缀合物的脑部传递。

神经系统疾病无疑是人类可能面临的最令人震惊的疾病。在治疗神经系统疾病时，血脑屏障（BBB）是阻止药物渗透到大脑的具有挑战性的障碍。本文介绍了用于中枢神经系统（CNS）治疗的树枝状大分子化学的进展。构建了具有链霉亲和素衔接子的聚（酰胺基）胺（PAMAM）树状聚合物生物缀合物，用于连接树突或任何生物素化的药物。进行了关于猪或鼠模型的体外研究以及体内小鼠研究，它们揭示了树突化链霉亲和素（DSA）渗透到中枢神经系统中。生物共轭物主要由小窝途径吸收，并通过从溶酶体逃逸的转胞吞作用穿过血脑屏障。转胞吞后，DSA被递送至星形胶质细胞和神经元。此外，DSA在体外和体内均具有高生物相容性。总之，这里介绍了在神经病理学中实现治疗性PAMAM功能以及药物递送的新策略。