Caprifico Anna E, Foot Peter J S, Polycarpou Elena, Calabrese Gianpiero
School of Life Sciences, Pharmacy and Chemistry, Kingston University London, Penrhyn Road, Kingston upon Thames KT1 2EE, UK.
Pharmaceutics. 2020 Oct 23;12(11):1013. doi: 10.3390/pharmaceutics12111013.
The major impediment to the delivery of therapeutics to the brain is the presence of the blood-brain barrier (BBB). The BBB allows for the entrance of essential nutrients while excluding harmful substances, including most therapeutic agents; hence, brain disorders, especially tumours, are very difficult to treat. Chitosan is a well-researched polymer that offers advantageous biological and chemical properties, such as mucoadhesion and the ease of functionalisation. Chitosan-based nanocarriers (CsNCs) establish ionic interactions with the endothelial cells, facilitating the crossing of drugs through the BBB by adsorptive mediated transcytosis. This process is further enhanced by modifications of the structure of chitosan, owing to the presence of reactive amino and hydroxyl groups. Finally, by permanently binding ligands or molecules, such as antibodies or lipids, CsNCs have showed a boosted passage through the BBB, in both in vivo and in vitro studies which will be discussed in this review.
将治疗药物输送到大脑的主要障碍是血脑屏障(BBB)的存在。血脑屏障允许必需营养物质进入,同时排除有害物质,包括大多数治疗药物;因此,脑部疾病,尤其是肿瘤,很难治疗。壳聚糖是一种经过充分研究的聚合物,具有有利的生物学和化学性质,如粘膜粘附性和易于功能化。基于壳聚糖的纳米载体(CsNCs)与内皮细胞建立离子相互作用,通过吸附介导的转胞吞作用促进药物穿过血脑屏障。由于存在反应性氨基和羟基,壳聚糖结构的修饰进一步增强了这一过程。最后,通过永久结合配体或分子,如抗体或脂质,CsNCs在体内和体外研究中均显示出通过血脑屏障的能力增强,本文将对此进行讨论。