Lauro Maria Rosaria, Picerno Patrizia, Franceschelli Silvia, Pecoraro Michela, Aquino Rita Patrizia, Pignatello Rosario
Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 84084 Fisciano, SA, Italy.
Unesco Chair Salerno, Plantae Medicinales Mediterraneae, University of Salerno, 84084 Fisciano, SA, Italy.
Pharmaceutics. 2023 Jan 16;15(1):295. doi: 10.3390/pharmaceutics15010295.
(1) Background: Eudraguard Natural (EN) and Protect (EP) are polymers regulated for use in dietary supplements in the European Union and the United States to carry natural products, mask unpleasant smells and tastes, ameliorate product handling, and protect products from moisture, light, and oxidation. Moreover, EN and EP can control the release of encapsulated compounds. The aim of this work was the development, preparation, and control of Eudraguard spray-drying microparticles to obtain powders with easy handling and a stable dietary supplement containing a polar functional extract (SOE) from L. leaves. (2) Methods: SOE was characterized using HPLC, NMR, FTIR, DSC, and SEM methods. Furthermore, the SOE's antioxidant/free radical scavenging activity, α-glucosidase inhibition, MTT assay effect on viability in normal cells, and shelf life were evaluated in both the extract and final formulations. (3) Results: The data suggested that SOE, rich in flavonoids, is a bioactive and safe extract; however, from a technological point of view, it was sticky, difficult to handle, and had low aqueous solubility. Despite the fact that EN and EP may undergo changes with spray-drying, they effectively produced easy-to-handle micro-powders with a controlled release profile. Although EN had a weaker capability to coat SOE than EP, EN acted as a substrate that was able to swell, drawing in water and improving the extract solubility and dissolution/release; however, EP was also able to carry the extract and provide SOE with controlled release. (4) Conclusion: Both Eudraguard products were capable of carrying SOE and improving its antioxidant and α-glucosidase inhibition activities, as well as the extract stability and handling.
(1) 背景：尤特奇天然型（EN）和保护型（EP）是在欧盟和美国被监管用于膳食补充剂的聚合物，用于承载天然产物、掩盖不良气味和味道、改善产品的加工性能，并保护产品免受水分、光照和氧化的影响。此外，EN和EP可以控制被包封化合物的释放。这项工作的目的是开发、制备和控制尤特奇喷雾干燥微粒，以获得易于处理的粉末以及一种含有来自L.叶的极性功能提取物（SOE）的稳定膳食补充剂。(2) 方法：使用高效液相色谱法、核磁共振法、傅里叶变换红外光谱法、差示扫描量热法和扫描电子显微镜法对SOE进行表征。此外，还对提取物和最终制剂中的SOE的抗氧化/自由基清除活性、α-葡萄糖苷酶抑制作用、MTT法对正常细胞活力的影响以及保质期进行了评估。(3) 结果：数据表明，富含黄酮类化合物的SOE是一种具有生物活性且安全的提取物；然而，从技术角度来看，它具有粘性，难以处理，且水溶性较低。尽管EN和EP在喷雾干燥过程中可能会发生变化，但它们有效地制备出了具有可控释放特性且易于处理的微粉。尽管EN包覆SOE的能力比EP弱，但EN作为一种能够膨胀的基质，能够吸收水分并提高提取物的溶解度和溶解/释放；然而，EP也能够承载提取物并为SOE提供控释效果。(4) 结论：两种尤特奇产品都能够承载SOE并提高其抗氧化和α-葡萄糖苷酶抑制活性，以及提取物的稳定性和加工性能。
