血脑屏障作为中枢神经系统内维持内环境稳态的重要生理结构，其高度选择性的通透特性在保护中枢神经系统免受有害物质侵袭的同时，亦成为脑部药物递送的重大障碍。大部分化学药物由于分子结构、理化性质等因素，难以透过血脑屏障抵达脑部病灶靶点，致使神经系统疾病的临床治疗面临诸多挑战。传统中医药实践中，常运用石菖蒲、冰片、麝香等具有芳香开窍功效的中药，借助其“引药上行”之特性防治脑部疾病。现代研究表明，中药精油挥发性成分可对血脑屏障通透性进行精准调节，进而提升药物在脑内的分布浓度。精油作为关键活性组分，因其良好的脂溶性以及小分子结构特征，在透血脑屏障方面展现出明显优势。基于中医“芳香开窍”理论，系统梳理并归纳了中药精油及其挥发性成分调节血脑屏障通透性的研究进展，揭示了其调节P-糖蛋白、紧密连接蛋白，如封闭蛋白-5（Claudin-5）、闭合蛋白（Occludin）、闭锁小带蛋白1（zonula occluden-1，ZO-1）及氧化应激反应的作用机制，以期为脑靶向药物递送提供新策略。

The blood brain barrier (BBB), as an important physiological structure in the central nervous system (CNS) to maintain the homeostasis of the internal environment, has highly selective permeability properties that protect the CNS from harmful substances, but at the same time, it is also a major obstacle to drug delivery in the brain. Due to the molecular structure, physical and chemical properties of most chemical drugs, it is difficult for them to cross the BBB to reach the target of brain lesions, resulting in many challenges in the clinical treatment of neurological diseases. In the practice of traditional Chinese medicine (TCM), TCMs such as Shichangpu (Acori Tatarinowii Rhizoma), Bingpian (Borneolum Syntheticum) and Shexiang (Moschus), which have the effect of opening the orifices with aroma, are often used to prevent and treat cerebral diseases with the help of their characteristic of “guiding the medicine upward”. Modern research has shown that the volatile components of essential oils can accurately regulate the permeability of the BBB, thus enhancing the distribution of drugs in the brain. Essential oils, as key active components, show obvious advantages in BBB permeability due to their good lipid solubility and small molecule structure. Based on the theory of “aromatic opening of the orifices” in TCM, this paper systematically reviewed and summarized the research progress of essential oils and their volatile components in regulating the permeability of the BBB and investigated the mechanisms of their regulation of P-glycoprotein, tight junction proteins, such as Claudin-5, Occludin, zonula occluden-1 (ZO-1) and oxidative stress responses, with a view to providing new strategies for brain-targeted drug delivery.

R285

海南省重点研发项目（ZDYF2025SHFZ055）；国家自然科学基金资助项目（82404878）；江西省自然科学基金资助项目（20242BAB20456）；江西省“赣鄱英才”创新领军人才项目（S2024LQCQ0477）；江西省中医药标委会标准化项目（2024A023，2023A16）；江西中医药大学博士科研启动基金项目（2024BSZR016）；江西中医药大学2024年中药科研实践创新训练项目（24KYCX-YB022）