尼莫地平是治疗脑缺血疾病常用的药物,其脑内靶向递送不仅可提高脑内的药物浓度,也可降低外周组织的药物浓度并减轻相应的不良反应。本文综述了尼莫地平脑内靶向递送相关的制剂类型和给药途径的研究进展,并对其优缺点进行了评述。相对于普通溶液剂,混合胶束、微乳、纳米粒、脂质体等新型制剂可实现尼莫地平向脑内的高效递送;鼻腔给药和鞘内注射也有利于药物进入脑内。此外,展望了新型P-糖蛋白抑制剂的开发以及多晶型药物的晶型差异在药物脑靶向递送的应用前景。 Nimodipine is a commonly used drug for the treatment of cerebral ischemia. Targeted delivery in the brain can not only increase the concentration of drugs in the brain, but also reduce the drug concentration in peripheral tissues and reduce the corresponding adverse reactions. This review summarizes the progress in the formulation of nimodipine-based targeted delivery and its route of administration, and reviews its advantages and disadvantages. Compared with common solutions, new formulations such as mixed micelles, microemulsions, nanoparticles, and liposomes can deliver nimodipine to the brain efficiently. Nasal and intrathecal injections also facilitate drug entry into the brain. In addition, the prospect of the development of new P-glycoprotein inhibitors and the polymorphic polymorphism of polymorphic drugs in drug brain targeting delivery are prospected.