Department of Research, Development & Innovation, Apis Flora Indl. Coml. Ltd.a., Ribeirão Preto 14020-670, Brazil.
Department of Pharmaceutical Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto 14040-903, Brazil.
Molecules. 2023 Oct 17;28(20):7128. doi: 10.3390/molecules28207128.
The demand for organic and functional food continues to increase yearly. Among the available functional foods, propolis is a bee product that has various beneficial properties, including antimicrobial, antioxidant, and anti-inflammatory activities. However, it generally is only available in ethanol solution, which has poor bioavailability, as it is relatively insoluble in water. The use of such ethanol extracts is often objectionable because of the alcohol content and because they have a strong and striking taste. Development of alternatives that can efficiently and safely increase solubility in water, and that meet organic production specifications, has been a challenge. To address these concerns, microcapsules were developed using spray-dryer technology from an emulsion based on EPP-AF propolis and gum arabic (i-CAPS). These propolis-loaded microcapsules were characterized using FT-IR, SEM, TGA, HPLC, and spectrophotometric techniques, along with determination of antimicrobial, antioxidant, antitumor, anti-inflammatory, and antihypercholesterolemic activities, as well as permeability in in vitro models. The production system resulted in microcapsules with a spherical shape and an encapsulation efficiency of 93.7 ± 0.7%. They had IC50s of 2.654 ± 0.062 and 7.342 ± 0.058 µg/mL by FRAP and DPPH antioxidant methods, respectively. The EPP-AF i-CAPS also had superior antimicrobial activity against Gram-positive bacteria. Antitumor activity was calculated based on the concentration that inhibited 50% of growth of AGS, Caco-2, and MCF-7 cell strains, giving results of 154.0 ± 1.0, 117 ± 1.0, and 271.0 ± 25 µg/mL, respectively. The microcapsule presentation reduced the permeation of cholesterol by 53.7%, demonstrating antihypercholesterolemic activity, and it improved the permeability of -coumaric acid and artepillin C. The IC50 for NO production in RAW 264.7 cells was 59.0 ± 0.1 µg/mL. These findings demonstrate the potential of this new propolis product as a food and pharmaceutical ingredient, though additional studies are recommended to validate the safety of proposed dosages.
对有机和功能性食品的需求逐年增加。在现有的功能性食品中，蜂胶是一种具有多种有益特性的蜂产品，具有抗菌、抗氧化和抗炎活性。然而，它通常仅以乙醇溶液的形式存在，由于相对不溶于水，因此生物利用度较差。由于含有酒精且味道强烈刺鼻，因此使用这种乙醇提取物通常会引起反对。开发能够有效且安全地提高水中溶解度并符合有机生产规范的替代品一直是一个挑战。为了解决这些问题，使用喷雾干燥技术从基于 EPP-AF 蜂胶和阿拉伯胶（i-CAPS）的乳液中开发了微胶囊。使用 FT-IR、SEM、TGA、HPLC 和分光光度技术以及确定抗菌、抗氧化、抗肿瘤、抗炎和抗高胆固醇血症活性以及体外模型中的渗透性来表征这些负载有蜂胶的微胶囊。该生产系统产生了具有球形形状和 93.7±0.7%包封效率的微胶囊。它们的 FRAP 和 DPPH 抗氧化方法的 IC50 分别为 2.654±0.062 和 7.342±0.058 µg/mL。EPP-AF i-CAPS 对革兰氏阳性菌也具有更好的抗菌活性。抗肿瘤活性是基于抑制 AGS、Caco-2 和 MCF-7 细胞系生长 50%的浓度计算得出的，结果分别为 154.0±1.0、117±1.0 和 271.0±25 µg/mL。微胶囊的呈现降低了胆固醇的渗透 53.7%，显示出抗高胆固醇血症的活性，并且提高了 -香豆酸和 artepillin C 的渗透性。RAW 264.7 细胞中 NO 产生的 IC50 为 59.0±0.1 µg/mL。这些发现表明这种新的蜂胶产品作为食品和药物成分具有潜力，尽管建议进行更多研究来验证提议剂量的安全性。
