Gajda-Morszewski Przemysław, Poznańska Anna, Yus Cristina, Arruebo Manuel, Brindell Małgorzata
Department of Inorganic Chemistry, Faculty of Chemistry, Jagiellonian University in Kraków, Gronostajowa 2, 30-387 Krakow, Poland.
Doctoral School of Exact and Natural Sciences, Jagiellonian University in Kraków, Prof. St. Łojasiewicza St 11, 30-348 Krakow, Poland.
Nanomaterials (Basel). 2023 Sep 8;13(18):2524. doi: 10.3390/nano13182524.
Lactoferrin (Lf) is a globular glycoprotein found mainly in milk. It has a very high affinity for iron(III) ions, and its fully saturated form is called holoLf. The antimicrobial, antiviral, anticancer, and immunomodulatory properties of Lf have been studied extensively for the past two decades. However, to demonstrate therapeutic benefits, Lf has to be efficiently delivered to the intestinal tract in its structurally intact form. This work aimed to optimize the encapsulation of holoLf in a system based on the versatile Eudragit RS polymer to protect Lf against the proteolytic environment of the stomach. Microparticles (MPs) with entrapped holoLf were obtained with satisfactory entrapment efficiency (90-95%), high loading capacity (9.7%), and suitable morphology (spherical without cracks or pores). Detailed studies of the Lf release from the MPs under conditions that included simulated gastric or intestinal fluids, prepared according to the 10th edition of the , showed that MPs partially protected holoLf against enzymatic digestion and ionic iron release. The preincubation of MPs loaded with holoLf under conditions simulating the stomach environment resulted in the release of 40% of Lf from the MPs. The protein released was saturated with iron ions at 33%, was structurally intact, and its iron scavenging properties were preserved.
乳铁蛋白（Lf）是一种主要存在于牛奶中的球状糖蛋白。它对铁（III）离子具有很高的亲和力，其完全饱和形式称为全乳铁蛋白（holoLf）。在过去二十年中，人们对Lf的抗菌、抗病毒、抗癌和免疫调节特性进行了广泛研究。然而，为了证明其治疗益处，Lf必须以结构完整的形式有效地递送至肠道。这项工作旨在优化基于通用型Eudragit RS聚合物的系统中holoLf的包封，以保护Lf免受胃蛋白酶解环境的影响。获得了包载holoLf的微粒（MPs），其包封效率令人满意（90 - 95%），载药量高（9.7%），形态合适（球形，无裂缝或孔隙）。根据《药典》第十版制备的模拟胃液或肠液条件下对MPs中Lf释放的详细研究表明，MPs部分保护holoLf免受酶消化和离子铁释放的影响。在模拟胃环境的条件下对载有holoLf的MPs进行预孵育，导致40%的Lf从MPs中释放。释放的蛋白质中铁离子饱和度为33%，结构完整，其铁清除特性得以保留。
