Department of Chemical Engineering, National Chung Cheng University, Chia-Yi, Taiwan, Republic of China.
J Drug Target. 2010 Jul;18(6):447-56. doi: 10.3109/10611860903494245.
This study investigates the electromagnetic field (EMF)-regulated transport of cationic solid lipid nanoparticles (CSLNs) across human brain-microvascular endothelial cells (HBMECs). The positive charge of CSLNs was from dioctadecyldimethyl ammonium bromide and stearylamine, and radiofrequency EMF was applied to HBMECs for promoting uptake of CSLNs. Immunochemical staining revealed that the expression of clathrin on the membrane of HBMECs enhanced during vesicular endocytosis of CSLNs. However, CSLNs and EMF slightly affected the expression of P-glycoprotein on the membrane of HBMECs. An exposure to EMF yielded negligible increase in the permeability of free saquinavir (SQV) across the HBMEC monolayer. Nevertheless, the permeability of SQV across the HBMEC monolayer increased about 17-fold when SQV was entrapped in CSLNs. Moreover, the permeability of SQV across the HBMEC monolayer increased about 22-fold by applying the CSLN encapsulation and EMF exposure. CSLNs and EMF could produce synergistic effect on improving the brain-targeting delivery.
本研究探讨了电磁场(EMF)调控阳离子固体脂质纳米粒(CSLN)跨人脑微血管内皮细胞(HBMEC)的转运。CSLN 的正电荷来自双十八烷基二甲基溴化铵和硬脂胺,射频 EMF 被应用于 HBMEC 以促进 CSLN 的摄取。免疫化学染色显示,在 CSLN 的囊泡内吞过程中,HBMEC 膜上网格蛋白的表达增强。然而,CSLN 和 EMF 对 HBMEC 膜上 P-糖蛋白的表达影响不大。EMF 的暴露对游离沙奎那韦(SQV)穿过 HBMEC 单层的通透性仅有微小的增加。然而,当 SQV 被包封在 CSLN 中时,SQV 穿过 HBMEC 单层的通透性增加了约 17 倍。此外,通过应用 CSLN 包封和 EMF 暴露,SQV 穿过 HBMEC 单层的通透性增加了约 22 倍。CSLN 和 EMF 可以产生协同作用,改善脑靶向递送。