Department of Chemical Sciences, University of Padova, Via Marzolo 1, 35131 Padova, Italy.
ECSIN-European Center for the Sustainable Impact of Nanotechnology, ECAMRICERT SRL, Corso Stati Uniti 4, 35127 Padova, Italy.
Molecules. 2020 Dec 17;25(24):5989. doi: 10.3390/molecules25245989.
Iron is a fundament micronutrient, whose homeostasis is strictly regulated. Iron deficiency anemia is among the most widespread nutritional deficiencies and its therapy, based on dietary supplement and drugs, may lead to severe side effects. With the aim of improving iron bioavailability while reducing iron oral therapy side effects, novel dietary supplements based on innovative technologies-microencapsulation, liposomes, sucrosomes-have been produced and marketed. In the present work, six iron dietary supplements for different therapeutic targets were compared in terms of bioaccessibility, bioavailability, and safety by using an integrated in vitro approach. For general-purpose iron supplements, ME + VitC (microencapsulated) showed a fast, burst intestinal iron absorption kinetic, which maintained iron bioavailability and ferritin expression constant over time. SS + VitC (sucrosomes), on the other side, showed a slower, time-dependent iron absorption and ferritin expression trend. ME + Folate (microencapsulated) showed a behavior similar to that of ME + VitC, albeit with a lower bioavailability. Among pediatric iron supplements, a time-dependent bioavailability increase was observed for LS (liposome), while PIC (polydextrose-iron complex) bioavailability is severely limited by its poor bioaccessibility. Finally, except for SS + VitC, no adverse effects on intestinal mucosa vitality and barrier integrity were observed. Considering obtained results and the different therapeutic targets, microencapsulation-based formulations are endowed with better performance compared to the other formulations. Furthermore, performances of microencapsulated products were obtained with a lower iron daily dose, limiting the potential onset of side effects.
铁是一种基础微量营养素,其体内平衡受到严格调节。缺铁性贫血是最常见的营养缺乏症之一,其治疗方法基于饮食补充剂和药物,但可能会导致严重的副作用。为了提高铁的生物利用度,同时减少口服铁治疗的副作用,已经开发并销售了基于创新技术的新型膳食补充剂,如微胶囊化、脂质体、蔗糖酯。在本工作中,使用综合的体外方法,针对不同的治疗靶点,对六种铁膳食补充剂进行了生物利用度、生物可及性和安全性的比较。对于一般用途的铁补充剂,ME + VitC(微胶囊化)显示出快速、爆发性的肠道铁吸收动力学,可使铁的生物利用度和铁蛋白表达保持恒定。另一方面,SS + VitC(蔗糖酯)显示出较慢、随时间变化的铁吸收和铁蛋白表达趋势。ME + Folate(微胶囊化)表现出与 ME + VitC 相似的行为,尽管生物利用度较低。在儿科铁补充剂中,LS(脂质体)的生物利用度随着时间的推移而增加,而 PIC(聚葡萄糖-铁复合物)的生物利用度受到其较差的生物可及性的严重限制。最后,除 SS + VitC 外,其他制剂对肠黏膜活力和屏障完整性没有不良影响。考虑到所获得的结果和不同的治疗靶点,基于微胶囊化的制剂与其他制剂相比具有更好的性能。此外,微胶囊化产品的性能是通过降低每日铁剂量获得的,从而限制了潜在副作用的发生。