Selmani Atiđa, Matijaković Mlinarić Nives, Falsone Salvatore Fabio, Vidaković Ivan, Leitinger Gerd, Delač Ida, Radatović Borna, Nemet Ivan, Rončević Sanda, Bernkop-Schnürch Andreas, Vuletić Tomislav, Kornmueller Karin, Roblegg Eva, Prassl Ruth
Department of Pharmaceutical Technology and Biopharmacy, Institute of Pharmaceutical Sciences, University of Graz, Graz, 8010, Austria.
Laboratory for Precipitation Processes, Division of Material Chemistry, Institute Ruđer Bošković, Zagreb, Croatia.
Int J Nanomedicine. 2024 Dec 17;19:13485-13505. doi: 10.2147/IJN.S483253. eCollection 2024.
Selenium (Se) is a vital micronutrient for maintaining homeostasis in the human body. Selenium nanoparticles (SeNPs) have demonstrated improved bioavailability compared to both inorganic and organic forms of Se. Therefore, supplementing with elemental Se in its nano-form is highly promising for biomedical applications related to Se deficiency.
The primary objective of this study was to evaluate the impact of the main gastrointestinal proteins on the physicochemical properties and stability of polymer-coated SeNPs.
SeNPs functionalized with thiolated chitosan or hyaluronic acid were characterized based on their composition, morphology, size, and zeta potential. The stability of these particles was evaluated in simulated gastric and intestinal fluids. Additionally, the interaction propensity between major gastric proteins, such as pepsin and pancreatin, and functionalized SeNPs was investigated with FTIR, fluorescence quenching titrations, and in situ adsorption measurements.
The composition of the media, including pH and ionic strength, the chemistry of polymers, and the presence of the proteins, influence the size and zeta potential of the SeNPs. The increase in NP size due to the formation of large agglomerates, along with the decrease in zeta potential magnitude, confirmed the formation of a protein corona. Both pepsin and pancreatin showed a strong affinity to the particle surface. Based on the values of the apparent equilibrium dissociation constant this affinity was more pronounced for positively charged thiolated chitosan coated SeNPs compared to those coated with negatively charged hyaluronic acid. The polymer coated SeNPs displayed antioxidative potential, which could be very beneficial for health conditions associated with Se-deficiency.
This study highlights the importance of exploring the characteristics of polymer-functionalized SeNPs under gastrointestinal conditions. Such investigations are important for developing nutritional supplements that can gradually release Se from SeNPs, thereby improving selenium absorption, bioavailability, and safety.
硒（Se）是维持人体体内平衡的重要微量营养素。与无机和有机形式的硒相比，硒纳米颗粒（SeNPs）已显示出更高的生物利用度。因此，以纳米形式补充元素硒在与硒缺乏相关的生物医学应用中极具前景。
本研究的主要目的是评估主要胃肠道蛋白对聚合物包覆的硒纳米颗粒的物理化学性质和稳定性的影响。
对用巯基化壳聚糖或透明质酸功能化的硒纳米颗粒进行组成、形态、大小和zeta电位表征。在模拟胃液和肠液中评估这些颗粒的稳定性。此外，通过傅里叶变换红外光谱（FTIR）、荧光猝灭滴定和原位吸附测量研究了主要胃蛋白（如胃蛋白酶和胰酶）与功能化硒纳米颗粒之间的相互作用倾向。
介质的组成（包括pH值和离子强度）、聚合物的化学性质以及蛋白质的存在会影响硒纳米颗粒的大小和zeta电位。由于形成大的聚集体导致纳米颗粒尺寸增加，同时zeta电位幅度降低，证实了蛋白质冠的形成。胃蛋白酶和胰酶都对颗粒表面表现出强烈的亲和力。根据表观平衡解离常数的值，与带负电荷的透明质酸包覆的硒纳米颗粒相比，带正电荷的巯基化壳聚糖包覆的硒纳米颗粒的这种亲和力更为明显。聚合物包覆的硒纳米颗粒具有抗氧化潜力，这对于与硒缺乏相关的健康状况可能非常有益。
本研究强调了在胃肠道条件下探索聚合物功能化硒纳米颗粒特性的重要性。此类研究对于开发能够从硒纳米颗粒中逐渐释放硒从而提高硒吸收、生物利用度和安全性的营养补充剂非常重要。
