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由于脑毛细血管结构特殊,其内皮细胞紧密相连形成血-脑屏障(BBB),从而限制了某些物质在血管与脑实质之间自由交往,如水溶性药物,电解质与蛋白质等就难以进入脑内,因此对颅内一些疾患如肿瘤、炎症与某种先天性酶缺乏病的治疗就受其影响。多年来,一些学者为克服这一缺陷,提高药物向中枢神经系统(CNS)传递,已作了大量研究,如采用能透过脑毛细管的脂溶性药物,但目前对脑瘤治疗有效的药物多为水溶性,如氨甲喋呤(MTX)在脑脊液(CSF)与血清之浓度比值仅为0.02,不能达到治疗目的。此外,用系统大剂量抗癌药,然后以四氢叶酸解救,试图提高脑内药物浓度,曾用
Due to the special structure of brain capillaries, their endothelial cells are closely connected to form the blood-brain barrier (BBB), which limits the free interaction between certain substances in the blood vessels and brain parenchyma. For example, water-soluble drugs, electrolytes, and proteins are difficult to enter the brain. Therefore, the treatment of some diseases in the brain such as tumors, inflammation, and certain innate enzyme deficiency diseases is affected. Over the years, some scholars have done a lot of research to overcome this deficiency and improve the delivery of drugs to the central nervous system (CNS). For example, lipid-soluble drugs that penetrate the brain’s capillaries are available, but many drugs that are currently effective in the treatment of brain tumors For water-soluble, such as methotrexate (MTX) in the ratio of the concentration of cerebrospinal fluid (CSF) and serum is only 0.02, can not achieve therapeutic purposes. In addition, he used large-scale systemic anticancer drugs and then rescued with tetrahydrofolic acid to try to increase the concentration of drugs in the brain.