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Lipid-based Mucus Penetrating Nanoparticles and their Biophysical Interactions with Pulmonary Mucus Layer.
European Journal of Pharmaceutics and Biopharmaceutics ( IF 4.4 ) Pub Date : 2020-01-31 , DOI: 10.1016/j.ejpb.2020.01.017
Gokce Alp 1 , Nihal Aydogan 1
Affiliation  

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.

中文翻译:

基于脂质的粘液穿透性纳米颗粒及其与肺粘液层的生物物理相互作用。

肺是不断暴露于外源性物质的重要器官。粘液层的存在通过其粘合结构和过滤机制有助于保护它们。粘液还对药物和纳米载体的药物输送起到了强大的屏障作用。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颗粒(SLN),并测试了它们在肺部药物递送中的扩散/渗透能力。通过在粘蛋白溶液中孵育SLNs并使用Langmuir-Blodgett(LB)槽形成模型粘液层,已通过光散射(LS)和zeta电位分析研究了SLNs的生物物理相互作用。另外,使用Franz扩散池和旋转扩散管评估了颗粒的渗透性能。已确定36%的SLN可以穿透1.2±0.2 mm厚的粘液层。最后,使用阳离子表面活性剂混合物表征并增强了颗粒在模拟粘液亚相上的铺展行为。总体而言,当前的研究是首次研究SLN的扩散和渗透性能。开发的系统提供了一种药物输送系统,该系统能够通过厚厚的粘液层实现高渗透率。
更新日期:2020-01-31
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