Fernandes Filipe, Dias-Teixeira Mónica, Delerue-Matos Cristina, Grosso Clara
REQUIMTE/LAQV, Instituto Superior de Engenharia do Instituto Politécnico do Porto, Rua Dr. António Bernardino de Almeida, 431, 4249-015 Porto, Portugal.
NICiTeS-Núcleo de Investigação em Ciências e Tecnologias da Saúde, Escola Superior de Saúde Ribeiro Sanches, 1649-028 Lisbon, Portugal.
Nanomaterials (Basel). 2021 Feb 24;11(3):563. doi: 10.3390/nano11030563.
The biggest obstacle to the treatment of diseases that affect the central nervous system (CNS) is the passage of drugs across the blood-brain barrier (BBB), a physical barrier that regulates the entry of substances into the brain and ensures the homeostasis of the CNS. This review summarizes current research on lipid-based nanoparticles for the nanoencapsulation of neuroprotective compounds. A survey of studies on nanoemulsions (NEs), nanoliposomes/nanophytosomes and solid lipid nanoparticles (SLNs)/nanostructured lipid carriers (NLCs) was carried out and is discussed herein, with particular emphasis upon their unique characteristics, the most important parameters influencing the formulation of each one, and examples of neuroprotective compounds/extracts nanoencapsulated using these nanoparticles. Gastrointestinal absorption is also discussed, as it may pose some obstacles for the absorption of free and nanoencapsulated neuroprotective compounds into the bloodstream, consequently hampering drug concentration in the brain. The transport mechanisms through which compounds or nanoparticles may cross BBB into the brain parenchyma, and the potential to increase drug bioavailability, are also discussed. Additionally, factors contributing to BBB disruption and neurodegeneration are described. Finally, the advantages of, and obstacles to, conventional and unconventional routes of administration to deliver nanoencapsulated neuroprotective drugs to the brain are also discussed, taking into account the avoidance of first-pass metabolism, onset of action, ability to bypass the BBB and concentration of the drug in the brain.
影响中枢神经系统（CNS）疾病治疗的最大障碍是药物穿越血脑屏障（BBB），血脑屏障是一种物理屏障，可调节物质进入大脑并确保中枢神经系统的内环境稳定。本综述总结了基于脂质的纳米颗粒用于神经保护化合物纳米包封的当前研究。对纳米乳液（NEs）、纳米脂质体/纳米植物脂质体和固体脂质纳米颗粒（SLNs）/纳米结构脂质载体（NLCs）的研究进行了调查并在此讨论，特别强调了它们的独特特性、影响每种制剂的最重要参数，以及使用这些纳米颗粒纳米包封的神经保护化合物/提取物的实例。还讨论了胃肠道吸收，因为它可能对游离和纳米包封的神经保护化合物吸收进入血液构成一些障碍，从而阻碍药物在大脑中的浓度。还讨论了化合物或纳米颗粒穿越血脑屏障进入脑实质的转运机制以及提高药物生物利用度的潜力。此外，还描述了导致血脑屏障破坏和神经退行性变的因素。最后，还讨论了将纳米包封的神经保护药物输送到大脑的传统和非常规给药途径的优点和障碍，同时考虑到避免首过代谢、起效、绕过血脑屏障的能力以及药物在大脑中的浓度。
