Development and characterization of avenanthramide-loaded bilosomes: Bile salt-incorporated liposomes as a cholesterol substitute for enhanced oral delivery

IF 8.5 1区农林科学 Q1 CHEMISTRY, APPLIED

Food Chemistry Pub Date : 2025-05-17 DOI:10.1016/j.foodchem.2025.144809

Eunwoo Jeong, Youjin Baek, Hyeon Gyu Lee

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Abstract

Avenanthramide (AVN), a phenolamide unique to oats, offers health benefits but is limited in application due to poor solubility, instability, and low bioavailability. This study developed bilosomes (AOE-BL) by incorporating bile salts into liposomes (AOE-LP) as a cholesterol substitute to enhance the oral delivery of AVN-enriched oat extract (AOE). AOE-BL exhibited smaller particle sizes and higher encapsulation efficiency than AOE-LP. Both formulations significantly increased AVN solubility by 2.74-fold and 2.71-fold, respectively, compared to free AOE while preventing heat-induced degradation. AOE-BL demonstrated superior stability under acidic conditions, with less pronounced changes in particle size and zeta potential than AOE-LP. After in vitro digestion, AOE-BL achieved significantly higher bioaccessibility (77.31 ± 3.31 %) than AOE-LP (67.21 ± 2.37 %) and free AOE (55.69 ± 3.43 %). Cellular uptake studies in Caco-2 enterocytes revealed that bile salts enhanced intracellular uptake compared to cholesterol. These findings highlight the potential of AOE-BL as an effective oral delivery system for AVN.

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含avenanthramide的胆汁酸脂质体的发展和特性：胆汁盐脂质体作为胆固醇的替代品，增强口服递送

燕麦原胺（AVN）是燕麦特有的一种酚胺，对健康有益，但由于溶解度差、不稳定和生物利用度低，应用受到限制。本研究通过将胆汁盐掺入脂质体（AOE- lp）作为胆固醇替代品，开发了胆汁盐脂质体（AOE- bl），以增强富含avn的燕麦提取物（AOE）的口服递送。AOE-BL比AOE-LP具有更小的粒径和更高的包封效率。与游离AOE相比，这两种配方分别显著提高了AVN的溶解度2.74倍和2.71倍，同时防止了热诱导降解。AOE-BL在酸性条件下表现出更好的稳定性，其粒径和zeta电位的变化比AOE-LP要小。体外消化后,AOE-BL取得显著高于bioaccessibility(77.31 ±3.31  %)比AOE-LP(67.21 ±2.37  %)和自由效果范围(55.69 ±3.43  %)。Caco-2肠细胞的细胞摄取研究显示，与胆固醇相比，胆盐增强了细胞内摄取。这些发现突出了AOE-BL作为AVN有效口服给药系统的潜力。

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来源期刊

Food Chemistry 工程技术-食品科技

CiteScore

16.30

自引率

10.20%

发文量

3130

审稿时长

122 days

期刊介绍： Food Chemistry publishes original research papers dealing with the advancement of the chemistry and biochemistry of foods or the analytical methods/ approach used. All papers should focus on the novelty of the research carried out.