LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, 4050-313, Porto, Portugal; CQM, Centro de Química da Madeira, Universidade da Madeira, Campus da Penteada, 9020-105 Funchal, Portugal.
LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, 4050-313, Porto, Portugal.
J Biotechnol. 2021 Apr 10;331:108-117. doi: 10.1016/j.jbiotec.2021.03.010. Epub 2021 Mar 13.
Curcumin is an anti-inflammatory and antioxidant compound with potent neuroprotective activity. Due to its poor water solubility, low bioavailability, rapid elimination and the challenges for crossing and transposing the blood-brain barrier (BBB), solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) loaded with curcumin were successfully produced and functionalized with transferrin, in order to mediate the transport of these particles through the BBB endothelium to the brain. The nanosystems revealed Z-averages under 200 nm, polydispersity index below 0.2 and zeta potential around -30 mV. Curcumin encapsulation around 65 % for SLNs and 80 % for NLCs was accomplished, while the functionalized nanoparticles presented a value around 70-75 %. A stability study revealed these characteristics remained unchanged for at least 3 months. hCMEC/D3 cells viability was firstly analysed by MTT and LDH assays, respectively, and a concentration of 10 μM of curcumin-loaded nanoparticles were then selected for the subsequent permeability assay. The permeability study was conducted using transwell devices with hCMEC/D3 cells monolayers and a 1.5-fold higher permeation of curcumin through the BBB was verified. Both SLNs and NLCs are promising for curcumin brain delivery, protecting the incorporated curcumin and targeting to the brain by the addition of transferrin to the nanoparticles surface.
姜黄素是一种具有抗炎和抗氧化活性的化合物，具有很强的神经保护作用。由于其水溶性差、生物利用度低、消除速度快以及穿越血脑屏障（BBB）的挑战，负载姜黄素的固体脂质纳米粒（SLNs）和纳米结构化脂质载体（NLCs）已成功制备并通过转铁蛋白功能化，以介导这些颗粒通过 BBB 内皮细胞向大脑的转运。纳米系统的 Z 均粒径小于 200nm，多分散指数低于 0.2，zeta 电位约为-30mV。实现了姜黄素包封率为 SLNs 约 65%和 NLCs 约 80%，而功能化纳米粒的包封率约为 70-75%。稳定性研究表明，这些特性至少在 3 个月内保持不变。首先通过 MTT 和 LDH 测定分析 hCMEC/D3 细胞活力，然后选择 10μM 载姜黄素纳米粒进行随后的渗透性测定。通过 hCMEC/D3 细胞单层的 Transwell 装置进行渗透性研究，证实姜黄素通过 BBB 的渗透增加了 1.5 倍。SLNs 和 NLCs 都可用于姜黄素的脑递送，通过在纳米粒表面添加转铁蛋白来保护所包含的姜黄素并靶向大脑。
