Tiwari Sandip B, Amiji Mansoor M
Department of Pharmaceutical Sciences, School of Pharmacy, Northeastern University, Boston, MA 02115, USA.
Curr Drug Deliv. 2006 Apr;3(2):219-32. doi: 10.2174/156720106776359230.
Drug delivery to the central nervous system (CNS) is one of the most challenging fields of research and development for pharmaceutical and biotechnology products. A number of hydrophilic therapeutic agents, such as antibiotics, anticancer agents, or newly developed neuropeptides do not cross the blood brain barrier (BBB) after systemic administration. The BBB is formed by the tight junctions at the brain capillary endothelial cells, which strictly control drug transfer from blood to brain. Drug modification, osmotic opening of cerebral capillary endothelium, and alternative routes for administration (e.g., intracerebral delivery) have been successfully used to enhance drug transport to the CNS. The use of nanocarriers, such as liposomes and solid polymeric or lipid nanoparticles may be advantageous over the current strategies. These nanocarriers can not only mask the BBB limiting characteristics of the therapeutic drug molecule, but may also protect the drug from chemical/enzymatic degradation, and additionally provide the opportunity for sustained release characteristics. Reduction of toxicity to peripheral organs can also be achieved with these nanocarriers. This review article discusses the various barriers for drug delivery to the CNS and reviews the current state of nanocarriers for enhancing drug transport into the CNS.
药物递送至中枢神经系统（CNS）是制药和生物技术产品研发中最具挑战性的研究领域之一。许多亲水性治疗剂，如抗生素、抗癌剂或新开发的神经肽，全身给药后无法穿过血脑屏障（BBB）。血脑屏障由脑毛细血管内皮细胞的紧密连接形成，严格控制药物从血液向脑内的转运。药物修饰、脑毛细血管内皮的渗透开放以及其他给药途径（如脑内给药）已成功用于增强药物向中枢神经系统的转运。使用纳米载体，如脂质体和固体聚合物或脂质纳米颗粒，可能比当前策略更具优势。这些纳米载体不仅可以掩盖治疗药物分子的血脑屏障限制特性，还可以保护药物免受化学/酶降解，此外还提供了实现缓释特性的机会。使用这些纳米载体还可以降低对外周器官的毒性。本文综述了药物递送至中枢神经系统的各种屏障，并回顾了用于增强药物向中枢神经系统转运的纳米载体的现状。
