基于硬脂酸的、系统性设计的口服脂质纳米粒用于增强富马酸二甲酯的脑递药。
Stearic acid based, systematically designed oral lipid nanoparticles for enhanced brain delivery of dimethyl fumarate.
机构信息
Department of Pharmacy, School of Chemical Sciences & Pharmacy, Central University of Rajasthan, Bandar Sindri, Distt. Ajmer, Rajasthan 305817, India.
Division of Pharmaceutics, UGC-Centre of Advanced Study, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India.
出版信息
Nanomedicine (Lond). 2017 Dec;12(23):2607-2621. doi: 10.2217/nnm-2017-0082. Epub 2017 Nov 2.
AIM
Dimethyl fumarate is a frequent prescription for the management of numerous neurological disorders. Despite immense promises, DMF is associated with various problems such as multiple dosing (2-3 oral doses daily) and lower brain permeability. Our aim was to enhance the oral bioavailability and increase the brain concentrations of dimethyl fumarate.
METHODS
Solid lipid nanoparticles were systematically formulated by optimizing the composition based on the desired attributes viz. particle size, entrapment efficiency and amount of drug released in 6 h. Results & conclusion: The developed system offered nanometric particle size with entrapment efficiency > 90%. Enhanced Caco-2 cells cellular uptake by optimized solid lipid nanoparticless with superior pharmacokinetic and higher brain biodistribution were observed.
目的
富马酸二甲酯是治疗多种神经紊乱的常用药物。尽管有巨大的应用前景，但富马酸二甲酯与多种问题相关，如多次给药（每日 2-3 次口服）和较低的脑穿透性。我们的目的是提高富马酸二甲酯的口服生物利用度并增加其在脑内的浓度。
方法
通过优化基于所需特性（如粒径、包封效率和 6 小时内释放的药物量）的组成，系统地制备了固体脂质纳米粒。
结果与结论
所开发的系统提供了纳米级粒径，包封效率>90%。与优化的固体脂质纳米粒相比，Caco-2 细胞摄取能力增强，药代动力学性能更优，脑内分布更高。
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