Faculty of Information Technology and Bionics, Pázmány Péter Catholic University, Práter u. 50A, H-1083 Budapest, Hungary.
Faculty of Information Technology and Bionics, Pázmány Péter Catholic University, Práter u. 50A, H-1083 Budapest, Hungary.
Brain Res Bull. 2018 Oct;143:155-170. doi: 10.1016/j.brainresbull.2018.10.009. Epub 2018 Oct 25.
The acute or chronic drug treatments for different neurodegenerative and psychiatric disorders are challenging from several aspects. The low bioavailability and limited brain exposure of oral drugs, the rapid metabolism, elimination, the unwanted side effects and also the high dose to be added mean both inconvenience for the patients and high costs for the patients, their family and the society. The reason of low brain penetration of the compounds is that they have to overcome the blood-brain barrier which protects the brain against xenobiotics. Intranasal drug administration is one of the promising options to bypass blood-brain barrier, to reduce the systemic adverse effects of the drugs and to lower the doses to be administered. Furthermore, the drugs administered using nasal route have usually higher bioavailability, less side effects and result in higher brain exposure at similar dosage than the oral drugs. In this review the focus is on giving an overview on the anatomical and cellular structure of nasal cavity and absorption surface. It presents some possibilities to enhance the drug penetration through the nasal barrier and summarizes some in vitro, ex vivo and in vivo technologies to test the drug delivery across the nasal epithelium into the brain. Finally, the authors give a critical evaluation of the nasal route of administration showing its main advantages and limitations of this delivery route for CNS drug targeting.
治疗各种神经退行性和精神疾病的急性或慢性药物治疗在多个方面都具有挑战性。口服药物的生物利用度低、脑内暴露量有限、代谢和消除迅速、产生不必要的副作用，以及需要增加高剂量，这对患者和患者、他们的家庭和社会来说都意味着不便和高成本。化合物脑穿透率低的原因是它们必须克服血脑屏障，血脑屏障可防止大脑接触外来物质。鼻腔内给药是绕过血脑屏障、减少药物全身不良反应并降低所需给药剂量的一种很有前途的选择。此外，通过鼻腔途径给予的药物通常具有更高的生物利用度、更少的副作用，并在相似剂量下导致更高的脑暴露，优于口服药物。本文综述重点概述鼻腔的解剖学和细胞结构以及吸收表面。它提出了一些增强药物穿透鼻屏障的可能性，并总结了一些体外、离体和体内技术，以测试药物经鼻腔上皮进入大脑的递药情况。最后，作者对鼻腔给药途径进行了批判性评估，展示了该给药途径在中枢神经系统药物靶向中的主要优势和局限性。
