Murad Research Center for Modernized Chinese Medicine, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Shanghai Innovation Center of TCM Health Service, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
School of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530001, China.
Int J Pharm. 2019 Apr 5;560:282-293. doi: 10.1016/j.ijpharm.2019.02.012. Epub 2019 Feb 14.
Since the application of chitosan magnetic cationic microspheres in brain drug delivery by Gallo in 1993, chitosan has been extensively studied in brain drug delivery. As the only natural alkaline polysaccharide with good biocompatibility and biodegradability, chitosan prepared nanoparticles which use chitosan as carrier material to encapsulate drug have been proved with advantages of protecting from enzyme degradation, control release and improved bioavailability. Besides, chitosan can enhance drug permeability across the blood-brain barrier by affecting the tight junction. And with positive charge on the surface, chitosan nanoparticles can absorb on the negatively charged cell membrane, thus increase its residence time on the nasal mucosa and benefit of the delivery of drugs from the nasal cavity to the brain. All these properties made chitosan nanoparticles especially suitable for brain delivery. What's more, the free amino groups on the surface of chitosan nanoparticles allow specific chemical modification to form a wide range of chitosan derivatives. Surface modification of the nanoparticles with tumor targeting peptides like chlorotoxin and transferrin, can further improve the targeting property to brain tumor. This article gives a comprehensive review on the advantages and recent progresses in the treatment of brain disease by chitosan nanoparticles.
自 1993 年 Gallo 将壳聚糖磁性阳离子微球应用于脑部药物输送以来，壳聚糖在脑部药物输送中的应用得到了广泛研究。壳聚糖作为唯一具有良好生物相容性和可生物降解性的天然碱性多糖，其制备的纳米粒以壳聚糖为载体材料包载药物，具有保护药物免受酶降解、控制释放和提高生物利用度的优点。此外，壳聚糖可以通过影响紧密连接来增强药物穿过血脑屏障的通透性。并且由于表面带正电荷，壳聚糖纳米粒可以吸附在带负电荷的细胞膜上，从而增加其在鼻黏膜上的停留时间，有利于药物从鼻腔输送到大脑。所有这些特性使得壳聚糖纳米粒特别适合脑部给药。更重要的是，壳聚糖纳米粒表面的游离氨基允许进行特定的化学修饰，形成广泛的壳聚糖衍生物。用肿瘤靶向肽如氯毒素和转铁蛋白对纳米粒进行表面修饰，可以进一步提高对脑肿瘤的靶向性。本文对壳聚糖纳米粒在脑部疾病治疗方面的优势和最新进展进行了全面综述。
