Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, West China School of Pharmacy, Sichuan University, Chengdu, P. R. China.
School of Food and Biological Engineering, Chengdu University, Chengdu, P. R. China.
Expert Opin Drug Deliv. 2023 Jul-Dec;20(12):1713-1730. doi: 10.1080/17425247.2023.2245332. Epub 2023 Aug 10.
A major challenge in treating central nervous system (CNS) disorders is to achieve adequate drug delivery across the blood-brain barrier (BBB). Receptor-mediated nanodrug delivery as a Trojan horse strategy has become an exciting approach. However, these nanodrugs do not accumulate significantly in the brain parenchyma, which greatly limits the therapeutic effect of drugs. Amplifying the efficiency of receptor-mediated nanodrug delivery across the BBB becomes the holy grail in the treatment of CNS disorders.
In this review, we tend to establish links between dynamic BBB and receptor-mediated nanodrug delivery, starting with the delivery processes across the BBB, describing factors affecting nanodrug delivery efficiency, and summarizing potential strategies that may amplify delivery efficiency.
Receptor-mediated nanodrug delivery is a common approach to significantly enhance the efficiency of brain-targeting delivery. As BBB is constantly undergoing changes, it is essential to investigate the impact of diseases on the effectiveness of brain-targeting nanodrug delivery. More critically, there are several barriers to achieving brain-targeting nanodrug delivery in the five stages of receptor-mediated transcytosis (RMT), and the impacts can be conflicting, requiring intricate balance. Further studies are also needed to investigate the material toxicity of nanodrugs to address the issue of clinical translation.
治疗中枢神经系统（CNS）疾病的主要挑战是实现药物在血脑屏障（BBB）中的充分传递。受体介导的纳米药物递送作为一种特洛伊木马策略已成为一种令人兴奋的方法。然而，这些纳米药物在脑实质中的积累并不显著，这极大地限制了药物的治疗效果。提高受体介导的纳米药物穿过 BBB 的传递效率成为治疗 CNS 疾病的圣杯。
在这篇综述中，我们倾向于在动态 BBB 和受体介导的纳米药物传递之间建立联系，从 BBB 的传递过程开始，描述影响纳米药物传递效率的因素，并总结可能放大传递效率的潜在策略。
受体介导的纳米药物传递是显著提高脑靶向递送效率的常用方法。由于 BBB 不断发生变化，因此研究疾病对脑靶向纳米药物传递效率的影响至关重要。更关键的是，受体介导的胞吞作用（RMT）的五个阶段中存在几种实现脑靶向纳米药物传递的障碍，其影响可能相互矛盾，需要精细的平衡。还需要进一步的研究来研究纳米药物的材料毒性，以解决临床转化的问题。
