Nose-to-Brain Delivery of Therapeutic Peptides as Nasal Aerosols.
Nose-to-Brain Delivery of Therapeutic Peptides as Nasal Aerosols.
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DOI：
10.3390/pharmaceutics14091870
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发表时间：
2022-09-05
期刊：
影响因子：
5.4
通讯作者：
Mansour HM
中科院分区：
文献类型：
--
作者：
Alabsi W;Eedara BB;Encinas-Basurto D;Polt R;Mansour HM
中枢神经系统（CNS）疾病，例如精神疾病、神经退行性疾病、慢性疼痛、中风、脑肿瘤、脊髓损伤和许多其他中枢神经系统疾病，将从特异性和有效的肽药物及其低固有毒性中受益匪浅。将肽递送至脑是具有挑战性的，这是由于它们的低代谢稳定性，这降低了它们的作用持续时间，血脑屏障（BBB）的渗透性差，以及它们与口服给药的不相容性，通常导致需要肠胃外给药。这些挑战限制了肽的临床应用，并解释了对肽给药的替代途径的兴趣，特别是鼻-脑（N-to-B）递送，其允许蛋白质和肽药物非侵入性地到达大脑。N-至B递送可以是快速靶向CNS、绕过BB B和最小化全身暴露的方便方法;嗅觉和三叉神经提供了通向大脑和外部环境的独特途径。这篇综述强调了药物的鼻内递送，重点是肽递送，说明了各种临床应用，鼻内递送装置，以及这种方法的范围和局限性。
Central nervous system (CNS) disorders, such as psychiatric disorders, neurodegeneration, chronic pain, stroke, brain tumor, spinal cord injury, and many other CNS diseases, would hugely benefit from specific and potent peptide pharmaceuticals and their low inherent toxicity. The delivery of peptides to the brain is challenging due to their low metabolic stability, which decreases their duration of action, poor penetration of the blood-brain barrier (BBB), and their incompatibility with oral administration, typically resulting in the need for parenteral administration. These challenges limit peptides’ clinical application and explain the interest in alternative routes of peptide administration, particularly nose-to-brain (N-to-B) delivery, which allows protein and peptide drugs to reach the brain noninvasively. N-to-B delivery can be a convenient method for rapidly targeting the CNS, bypassing the BBB, and minimizing systemic exposure; the olfactory and trigeminal nerves provide a unique pathway to the brain and the external environment. This review highlights the intranasal delivery of drugs, focusing on peptide delivery, illustrating various clinical applications, nasal delivery devices, and the scope and limitations of this approach.
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