Department of Chemical Engineering, Hacettepe University, Beytepe 06800, Ankara, Turkey.
Department of Chemical Engineering, Hacettepe University, Beytepe 06800, Ankara, Turkey.
Eur J Pharm Biopharm. 2020 Apr;149:45-57. doi: 10.1016/j.ejpb.2020.01.017. Epub 2020 Jan 31.
Lungs are critical organs that are continuously exposed to exogeneous matter. The presence of the mucus layer helps to protect them via its adhesive structure and filtering mechanisms. Mucus also acts as a strong barrier against the drugs and nanocarriers in drug delivery. In this study, solid lipid nanoparticles (SLNs), at different sizes and surface properties, were prepared and their spreading/penetration ability was tested for their use in pulmonary drug delivery. The biophysical interactions of SLNs have been studied via light scattering (LS) and zeta potential analyses by incubating the SLNs in mucin solution and forming a model mucus layer using a Langmuir-Blodgett (LB) trough. In addition, the penetration performance of the particles was evaluated using Franz diffusion cell and rotating diffusion tubes. It was determined that 36% of SLNs can penetrate through a 1.2 ± 0.2-mm-thick mucus layer. Finally, the spreading behavior of the particles on a mucus-mimicking subphase was characterized and enhanced using a catanionic surfactant mixture. Overall, the current study was the first to investigates both the spreading and penetration performance of SLNs. The developed systems offer a drug delivery system that is able to achieve high penetration rates through a thick mucus layer.
肺部是持续暴露于外源性物质的关键器官。黏液层的存在通过其粘性结构和过滤机制有助于保护肺部。黏液还对药物输送中的药物和纳米载体起到强大的屏障作用。在这项研究中，制备了不同大小和表面性质的固体脂质纳米粒（SLN），并测试了它们在肺部药物输送中的铺展/渗透能力。通过在黏液溶液中孵育 SLN 并使用 Langmuir-Blodgett (LB) 槽形成模型黏液层，通过光散射 (LS) 和 ζ 电位分析研究了 SLN 的生物物理相互作用。此外，使用 Franz 扩散池和旋转扩散管评估了颗粒的渗透性能。结果表明，36%的 SLN 可以穿透 1.2±0.2mm 厚的黏液层。最后，使用反离子表面活性剂混合物对颗粒在模拟黏液亚相上的铺展行为进行了表征和增强。总的来说，本研究首次研究了 SLN 的铺展和渗透性能。所开发的系统提供了一种药物输送系统，能够通过厚的黏液层实现高穿透率。
