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富含燕麦酰胺的双分子层脂质体的开发与表征:掺入胆盐的脂质体作为胆固醇替代物用于增强口服给药。

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

作者信息

Jeong Eunwoo, Baek Youjin, Lee Hyeon Gyu

机构信息

Department of Food and Nutrition, Hanyang University, 222 Wangsimni-ro, Seongdong-gu, Seoul 04763, Republic of Korea.

Department of Food and Nutrition, Hanyang University, 222 Wangsimni-ro, Seongdong-gu, Seoul 04763, Republic of Korea.

出版信息

Food Chem. 2025 Oct 1;488:144809. doi: 10.1016/j.foodchem.2025.144809. Epub 2025 May 17.

DOI:10.1016/j.foodchem.2025.144809
PMID:40424741
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.

摘要

燕麦酰胺(AVN)是燕麦特有的一种酚酰胺,具有健康益处,但由于溶解度差、稳定性低和生物利用度低,其应用受到限制。本研究通过将胆盐作为胆固醇替代物掺入脂质体(AOE-LP)中,开发了双分子层脂质体(AOE-BL),以增强富含AVN的燕麦提取物(AOE)的口服递送。与AOE-LP相比,AOE-BL表现出更小的粒径和更高的包封率。与游离AOE相比,两种制剂分别将AVN的溶解度显著提高了2.74倍和2.71倍,同时防止了热诱导的降解。AOE-BL在酸性条件下表现出优异的稳定性,与AOE-LP相比,粒径和zeta电位的变化较小。体外消化后,AOE-BL的生物可及性(77.31±3.31%)显著高于AOE-LP(67.21±2.37%)和游离AOE(55.69±3.43%)。在Caco-2肠细胞中的细胞摄取研究表明,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有效口服递送系统的潜力。

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