Experimental Centre, Shandong University of Traditional Chinese Medicine, Jinan 250355, P. R. China.
College of Intelligence and Information Engineering, Shandong University of Traditional Chinese Medicine, Jinan 250355, P. R. China.
Mol Pharm. 2024 Oct 7;21(10):4786-4803. doi: 10.1021/acs.molpharmaceut.4c00447. Epub 2024 Sep 4.
Recently, the incidence of brain diseases, such as central nervous system degenerative diseases, brain tumors, and cerebrovascular diseases, has increased. However, the blood-brain barrier (BBB) limits the effective delivery of drugs to brain disease areas. Therefore, the mainstream direction of new drug development for these diseases is to engineer drugs that can better cross the BBB to exert their effects in the brain. This paper reviews the research progress and application of the main trans-BBB drug delivery strategies (receptor/transporter-mediated BBB crossing, focused ultrasound to open the BBB, adenosine agonist reversible opening of the BBB, aromatic resuscitation, transnasal administration, cell-mediated trans-BBB crossing, and viral vector system-mediated brain drug delivery). Meanwhile, the potential applications, advantages, and disadvantages of these strategies for crossing the BBB are analyzed. Finally, the future development prospects of strategies for crossing the BBB are also discussed. These strategies have potential value for treating brain diseases.
近年来，中枢神经系统退行性疾病、脑肿瘤和脑血管疾病等脑部疾病的发病率不断上升。然而，血脑屏障（BBB）限制了药物有效递送到脑部疾病区域。因此，针对这些疾病的新药研发主流方向是设计能够更好地穿越 BBB 的药物，以在大脑中发挥作用。本文综述了主要的跨 BBB 药物递送策略（受体/转运体介导的 BBB 穿越、聚焦超声打开 BBB、腺苷激动剂可逆性打开 BBB、芳香复苏、经鼻给药、细胞介导的跨 BBB 穿越和病毒载体系统介导的脑内药物递送）的研究进展和应用。同时，分析了这些 BBB 穿越策略的潜在应用、优势和劣势。最后，还讨论了 BBB 穿越策略的未来发展前景。这些策略对于治疗脑部疾病具有潜在的应用价值。
