中药靶向递药入脑策略的研究进展

血脑屏障是中枢神经系统的一层特殊屏障，调节中枢神经系统稳态，允许正常的神经元功能，保护中枢神经系统免遭毒素、病原体和炎症的侵害。然而，脑毛细血管内皮细胞紧密连接的特性在保护的同时也极大程度限制了药物分子向内的递送效果。近年来，纳米制剂在中药靶向递药领域被广泛应用，较大的系统结构受制于血脑屏障导致疗效并不理想。基于血脑屏障上各种内源性受体及转运蛋白的发现，以及血脑屏障表面荷负电的生理特征，构建安全高效的靶向递药系统，从而设计受体介导、载体介导及吸附介导的转运途径实现血脑屏障的跨越，使药物制剂富集于脑部病变组织，有效提高疾病的治疗效果。受芳香中药“通关开窍”的传统功效启发，阐述其调节血脑屏障通透性的机制，并将这一功效与新兴纳米制剂结合，发挥中药特色进而实现制剂透过血脑屏障入脑释药。

Targeted Drug Delivery Strategy of Chinese Medicine into Brain: A Review

The blood-brain barrier is a special barrier of the central nervous system, which regulates the homeostasis of the central nervous system, allows normal neuronal function, and protects the central nervous system from toxins, pathogens, and inflammation. However, the tight junction of brain capillary endothelial cells greatly limits the inward delivery effect of drug molecules while protecting it. In recent years, nano-preparations have been widely used in the field of targeted drug delivery of Chinese medicine, but the curative effect is not ideal because their large system structure is restricted by the blood-brain barrier. Based on the discovery of various endogenous receptors and transporters on the blood-brain barrier and the physiological characteristics of negative charge on the surface of the blood-brain barrier, a safe and efficient targeted drug delivery system was constructed. Therefore, receptor-mediated, carrier-mediated, and adsorption-mediated transport pathways were designed to achieve the leapfrogging of the blood-brain barrier, so that drug preparations were enriched in brain lesions, thus effectively improving the therapeutic effect of the disease. Inspired by the traditional efficacy of aromatic Chinese medicine in "clearance and opening", this paper expounded its mechanism of regulating the permeability of blood-brain barrier and combined this effect with new nano-preparations to give full play to the characteristics of Chinese medicine, thereby releasing drugs into the brain through the blood-brain barrier.