Laboratory of Experimental Neurosurgery and Neuroanatomy, KU Leuven, Leuven 3000, Belgium.
Cancers (Basel). 2013 Aug 14;5(3):1020-48. doi: 10.3390/cancers5031020.
Despite recent advances in tumor imaging and chemoradiotherapy, the median overall survival of patients diagnosed with glioblastoma multiforme does not exceed 15 months. Infiltration of glioma cells into the brain parenchyma, and the blood-brain barrier are important hurdles to further increase the efficacy of classic therapeutic tools. Local administration methods of therapeutic agents, such as convection enhanced delivery and intracerebral injections, are often associated with adverse events. The intranasal pathway has been proposed as a non-invasive alternative route to deliver therapeutics to the brain. This route will bypass the blood-brain barrier and limit systemic side effects. Upon presentation at the nasal cavity, pharmacological agents reach the brain via the olfactory and trigeminal nerves. Recently, formulations have been developed to further enhance this nose-to-brain transport, mainly with the use of nanoparticles. In this review, the focus will be on formulations of pharmacological agents, which increase the nasal permeation of hydrophilic agents to the brain, improve delivery at a constant and slow release rate, protect therapeutics from degradation along the pathway, increase mucoadhesion, and facilitate overall nasal transport. A mounting body of evidence is accumulating that the underexplored intranasal delivery route might represent a major breakthrough to combat glioblastoma.
尽管肿瘤成像和放化疗技术最近取得了进展,但多形性胶质母细胞瘤患者的中位总生存期仍未超过 15 个月。胶质瘤细胞浸润脑实质和血脑屏障是进一步提高经典治疗工具疗效的重要障碍。治疗药物的局部给药方法,如对流增强输送和脑内注射,常伴有不良反应。鼻内途径已被提议作为一种非侵入性替代途径,将治疗药物递送到大脑。该途径将绕过血脑屏障并限制全身副作用。药物在鼻腔呈现时,通过嗅觉和三叉神经到达大脑。最近,已经开发出制剂来进一步增强这种鼻脑转运,主要是使用纳米颗粒。在这篇综述中,重点将放在增加亲水性药物经鼻渗透到大脑的药物制剂上,以恒定和缓慢的释放速率改善药物输送,保护治疗药物在整个途径中免受降解,增加粘膜黏附性,并促进整体鼻内转运。越来越多的证据表明,鼻腔内给药途径可能是对抗胶质母细胞瘤的重大突破。