尼莫地平脑内靶向递送的研究进展

Research Progress of Brain Targeting Delivery of Nimodipine

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 treatment of the cerebral ischemia diseases. Brain targeting delivery of nimodipine can not only increase the intracephalic drug concentration, but also reduce the peripheral drug concentration and the related side effects. This paper focuses on reviewing the novel dosage forms and drug delivery routes which are related to the brain targeting delivery of nimodipine. Compared with solution, a traditional dosage form, novel dosage forms such as mixed micelles, microemulsions, nanoparticles and liposomes can improve the brain targeting delivery of nimodipine. Meanwhile, intranasal administration and intrathecal injection of nimodipine also facilitate its brain targeting delivery. In addition, some comments on strategy for the future development of the brain targeting drug delivery system are introduced by the use of novel P-glycoprotein inhibitors and careful selection of crystal forms for polymorphic drugs.