Department of Pharmacy and Pharmaceutical Technology, University of Santiago de Compostela, Faculty of Pharmacy, Santiago de Compostela, Spain.
J Control Release. 2012 Feb 10;157(3):383-90. doi: 10.1016/j.jconrel.2011.08.008. Epub 2011 Aug 12.
This work presents a new dry powder system consisting of microencapsulated protein-loaded chitosan nanoparticles (CS NPs). The developed system was evaluated in vivo in rats in order to investigate its potential to transport insulin (INS), a model protein, to the deep lung, where it is absorbed into systemic circulation. The INS-loaded CS NPs were prepared by ionotropic gelation and characterized for morphology, size, zeta potential, association efficiency and loading capacity. Afterwards, the NPs were co-spray dried with mannitol resulting in a dry powder with adequate aerodynamic properties for deposition in deep lungs. The assessment of the plasmatic glucose levels following intratracheal administration to rats revealed that the microencapsulated INS-loaded CS NPs induced a more pronounced and prolonged hypoglycemic effect compared to the controls. Accordingly, the developed system constitutes a promising alternative to systemically deliver therapeutic macromolecules to the lungs, but it can also be used to provide a local effect.
本工作提出了一种由包载蛋白质的壳聚糖纳米粒子（CS NPs）组成的新型干粉系统。为了研究其将胰岛素（INS，一种模型蛋白）递送至深肺并被吸收到体循环中的潜力，该系统在大鼠体内进行了评估。通过离子凝胶化制备载胰岛素的 CS NPs，并对其形态、大小、Zeta 电位、结合效率和载药量进行了表征。随后，将 NPs 与甘露醇共喷雾干燥，得到具有适当空气动力学特性的干粉，可沉积在深肺中。经气管内给药后评估大鼠的血糖水平发现，与对照组相比，包载 INS 的 CS NPs 诱导了更显著和更持久的降血糖作用。因此，该系统为将治疗性大分子递送至肺部提供了一种有前途的替代方法，但也可用于提供局部作用。
