Dopamine is unable to access the central nervous system through the bloodstream. Only its precursor can do so, and with an effectiveness below 100% of the dose administered, as it is metabolized before crossing the blood-brain barrier. In this study, we describe a new solid lipid nanocarrier system designed and developed for dopamine. The nanoparticles were prepared by the melt-emulsification method and then coated with chitosan. The nanocarriers developed had a droplet size of about 250 nm, a polydispersity index of 0.2, a positive surface charge (+30 mV), and a percentage encapsulation efficiency of 36.3 ± 5.4. Transmission and scanning electron microscopy verified uniformity of particle size with spherical morphology. Various types of tests were performed to confirm that the nanoparticles designed are suitable for carrying dopamine through the blood-brain barrier. In vitro tests demonstrated the ability of these nanocarriers to pass through endothelial cell monolayers without affecting their integrity. This study shows that the formulation of dopamine in chitosan-coated solid lipid nanoparticles is a potentially viable formulation strategy to achieve the bioavailability of the drug for the treatment of Parkinson's disease in the central nervous system.

中文翻译：

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负载多巴胺的壳聚糖包被的固体脂质纳米粒子作为中枢神经系统的纳米载体

多巴胺无法通过血流进入中枢神经系统。只有其前体才能做到这一点，并且其有效性低于所施用剂量的 100%，因为它在穿过血脑屏障之前就被代谢了。在这项研究中，我们描述了一种为多巴胺设计和开发的新型固体脂质纳米载体系统。采用熔融乳化法制备纳米粒子，然后用壳聚糖包覆纳米粒子。所开发的纳米载体的液滴尺寸约为250 nm，多分散指数为0.2，表面电荷为正（+30 mV），封装效率百分比为36.3 ± 5.4。透射和扫描电子显微镜验证了颗粒尺寸的均匀性和球形形态。进行了各种类型的测试，以确认设计的纳米颗粒适合携带多巴胺穿过血脑屏障。体外测试证明了这些纳米载体能够穿过内皮细胞单层而不影响其完整性。这项研究表明，在壳聚糖包被的固体脂质纳米颗粒中配制多巴胺是一种潜在可行的制剂策略，可实现药物的生物利用度，用于治疗中枢神经系统的帕金森病。