Kržišnik Nika, Grilc Blaž, Roškar Robert
Faculty of Pharmacy, University of Ljubljana, Aškerčeva Cesta 7, 1000 Ljubljana, Slovenia.
Pharmaceutics. 2024 Dec 26;17(1):23. doi: 10.3390/pharmaceutics17010023.
BACKGROUND/OBJECTIVES: Lactoferrin (Lf), a multifunctional iron-binding protein, has considerable potential for use as an active ingredient in food supplements due to its numerous positive effects on health. As Lf is prone to degradation, we aimed to develop a formulation that would ensure sufficient stability of Lf in the gastrointestinal tract and during product storage.
A simple, efficient, and well-established technology that has potential for industrial production was used for the double-coating of neutral pellet cores with an Lf layer and a protective enteric coating.
The encapsulation efficiency was 85%, which is among the highest compared to other reported Lf formulations. The results of the dissolution tests performed indicated effective protection of Lf from gastric digestion. A comprehensive stability study showed that the stability was similar regardless of the neutral pellet core used, while a significant influence of temperature, moisture, product composition, and packaging on the stability of Lf were observed, and were therefore considered in the development of the final product. The experimentally determined shelf life is extended from 15 to almost 30 months if the product is stored in a refrigerator instead of at room temperature, which ensures the commercial applicability of the product.
We successfully transferred a technology commonly used for small molecules to a protein-containing product, effectively protected it from the destructive effects of gastric juice, and achieved an acceptable shelf life.
背景/目的：乳铁蛋白（Lf）是一种多功能铁结合蛋白，因其对健康有诸多积极作用，在用作食品补充剂的活性成分方面具有相当大的潜力。由于Lf易于降解，我们旨在开发一种制剂，以确保Lf在胃肠道和产品储存期间具有足够的稳定性。
采用一种简单、高效且成熟的、具有工业生产潜力的技术，用Lf层和保护性肠溶衣对中性丸芯进行双层包衣。
包封率为85%，与其他报道的Lf制剂相比处于最高水平。进行的溶出试验结果表明，Lf能有效免受胃消化的影响。一项全面的稳定性研究表明，无论使用何种中性丸芯，稳定性相似，同时观察到温度、湿度、产品成分和包装对Lf稳定性有显著影响，因此在最终产品的开发中予以考虑。如果产品储存在冰箱而非室温下，实验确定的保质期从15个月延长至近30个月，这确保了产品的商业适用性。
我们成功地将常用于小分子的技术转移到含蛋白质的产品上，有效保护其免受胃液的破坏作用，并实现了可接受的保质期。
