Kaasalainen Martti, Rytkönen Jussi, Mäkilä Ermei, Närvänen Ale, Salonen Jarno
Laboratory of Industrial Physics, Department of Physics and Astronomy, University of Turku , FI-20014 Turku, Finland.
Langmuir. 2015 Feb 10;31(5):1722-9. doi: 10.1021/la5047047. Epub 2015 Jan 30.
Porous silicon (PSi) nanoparticles' tunable properties are facilitating their use at highly challenging medical tasks such as peptide delivery. Because of many different mechanisms that are affecting the interaction between the peptide and the particle, the drug incorporation into the mesoporous delivery system is not straightforward. We have studied the adsorption and loading of incretin hormone glucagon like peptide 1 (GLP-1) on PSi nanoparticles. The results show that the highest loading degree can be achieved in pH values near the isoelectric point of peptide, and the phenomenon is independent of the surface's zeta potential. In order to study the interaction between the peptide and the nanoparticle, we studied the adsorption with lower concentrations and noticed that also non-Coulombic forces have a big role in adsorption of GLP-1. Adsorption is effective and pH-independent especially on low peptide concentrations and onto more hydrophobic nanoparticles. Reversibility of adsorption was studied as a function of buffer pH. When the loading is compared to the total mass of the formulation, the loading degree is 29%, and during desorption experiments 25% is released in 4 h and can be considered as a reversible loading degree. Thus, the peptides adsorbed first seem to create irreversibly adsorbed layer that facilitates reversible adsorption of following peptides.
多孔硅(PSi)纳米颗粒可调节的特性有助于其在极具挑战性的医学任务中发挥作用,如肽递送。由于影响肽与颗粒之间相互作用的机制多种多样,将药物掺入介孔递送系统并非易事。我们研究了肠促胰岛素激素胰高血糖素样肽1(GLP-1)在PSi纳米颗粒上的吸附和负载情况。结果表明,在接近肽等电点的pH值条件下可实现最高负载度,且该现象与表面的zeta电位无关。为了研究肽与纳米颗粒之间的相互作用,我们研究了较低浓度下的吸附情况,并注意到非库仑力在GLP-1的吸附中也起着重要作用。吸附是有效的且与pH无关,特别是在低肽浓度和更疏水的纳米颗粒上。研究了吸附的可逆性与缓冲液pH值的关系。当将负载量与制剂的总质量进行比较时,负载度为29%,在解吸实验中,4小时内释放25%,可视为可逆负载度。因此,首先吸附的肽似乎形成了不可逆吸附层,这有助于后续肽的可逆吸附。