Pharmaceutical Sciences Division, University of Wisconsin-Madison School of Pharmacy, Madison, WI 53705, USA.
Adv Drug Deliv Rev. 2012 May 15;64(7):614-28. doi: 10.1016/j.addr.2011.11.002. Epub 2011 Nov 15.
Treatment of central nervous system (CNS) diseases is very difficult due to the blood-brain barrier's (BBB) ability to severely restrict entry of all but small, non-polar compounds. Intranasal administration is a non-invasive method of drug delivery which may bypass the BBB to allow therapeutic substances direct access to the CNS. Intranasal delivery of large molecular weight biologics such as proteins, gene vectors, and stem cells is a potentially useful strategy to treat a variety of diseases/disorders of the CNS including stroke, Parkinson's disease, multiple sclerosis, Alzheimer's disease, epilepsy, and psychiatric disorders. Here we give an overview of relevant nasal anatomy and physiology and discuss the pathways and mechanisms likely involved in drug transport from the nasal epithelium to the CNS. Finally we review both pre-clinical and clinical studies involving intranasal delivery of biologics to the CNS.
由于血脑屏障(BBB)能够严重限制除了小的、非极性化合物之外的所有物质进入中枢神经系统,因此中枢神经系统(CNS)疾病的治疗非常困难。鼻腔给药是一种非侵入性的药物递送方法,它可以绕过 BBB,使治疗物质直接进入 CNS。鼻腔内递增大分子量的生物制剂,如蛋白质、基因载体和干细胞,是治疗多种中枢神经系统疾病/障碍的一种有前途的策略,包括中风、帕金森病、多发性硬化症、阿尔茨海默病、癫痫和精神疾病。在这里,我们概述了相关的鼻腔解剖学和生理学,并讨论了药物从鼻腔上皮到 CNS 的转运途径和机制。最后,我们回顾了涉及生物制剂经鼻腔递送到 CNS 的临床前和临床研究。