Patel Shirali, Revi Neeraja, Chakravarty Suridh, Gurgul Aleksandra, Najjar Yahya, Che Chun-Tao, Warpeha Katherine Mary, Bijukumar Divya
Blazer Nanomedicine Lab, Department of Biomedical Sciences, College of Medicine at Rockford, Rockford, IL 61107, United States of America.
Department of Pharmaceutical Sciences, College of Pharmacy, University of Illinois Chicago, Chicago, IL 60612, United States of America.
Biomed Mater. 2025 Jul 3;20(4). doi: 10.1088/1748-605X/ade7e3.
Phenylpropanoids (PA), which are plentiful in cruciferous vegetables, have not received adequate attention for their anti-inflammatory properties. Despite their potential benefits, the bioavailability and stability of these and other natural compounds under physiological conditions remain limited. This study aims to develop a natural nanovesicular delivery system that efficiently incorporates a phenylpropanoid extract-specifically, a multi-component anti-inflammatory extract derived from broccoli-with the goal of enhancing its bioavailability. This initiative serves as proof of concept for further research and application. The findings suggest that phenylpropanoids (PAs) achieve a 75% encapsulation efficiency within exosomes. Furthermore, it has been observed that PAs encapsulated in exosomes demonstrate a stability that is twice that of unencapsulated PAs under physiological conditions. The encapsulation process also improved the cytocompatibility of the PAs. Moreover, the functionality of the encapsulated PAs is significantly improved, as evidenced by a fivefold reduction in nitric oxide production from the EXO/PA nanocarriers. There is a significant decrease in the expression of pro-inflammatory genes, such as NFkB, MMP2, COX-2, and IL-1, in comparison to cells treated with LPS. Moreover, levels of TNF-, IL-6, and MCP-1 in activated macrophages treated with EXO/PAs were observed to be significantly reduced compared to those activated by LPS. It appears that the immune-suppressive effect of the extract may be mediated through both the ERK/MAPK and IkB/NFkB signaling pathways, highlighting the potential benefits of this approach. In conclusion, the results demonstrate that exosomes can effectively deliver polyphenylpropanoids while improving their stability and functionality, underscoring their potential role in future medical treatments.
苯丙烷类化合物（PA）在十字花科蔬菜中含量丰富，但其抗炎特性尚未得到充分关注。尽管它们具有潜在益处，但这些以及其他天然化合物在生理条件下的生物利用度和稳定性仍然有限。本研究旨在开发一种天然纳米囊泡递送系统，该系统能有效地包裹一种苯丙烷类提取物——具体而言，是一种源自西兰花的多组分抗炎提取物——以提高其生物利用度。这一举措为进一步的研究和应用提供了概念验证。研究结果表明，苯丙烷类化合物（PAs）在外泌体中的包封效率达到75%。此外，据观察，包裹在外泌体中的PAs在生理条件下的稳定性是未包裹PAs的两倍。包封过程还提高了PAs的细胞相容性。此外，包裹的PAs的功能显著改善，例如EXO/PA纳米载体产生的一氧化氮减少了五倍。与用脂多糖处理的细胞相比，促炎基因如NFkB、MMP2、COX - 2和IL - 1的表达显著降低。此外，与LPS激活的巨噬细胞相比，用EXO/PAs处理的激活巨噬细胞中TNF - 、IL - 6和MCP - 1的水平显著降低。提取物的免疫抑制作用似乎可能通过ERK/MAPK和IkB/NFkB信号通路介导，突出了这种方法的潜在益处。总之，结果表明外泌体可以有效地递送多聚苯丙烷类化合物，同时提高其稳定性和功能，强调了它们在未来医学治疗中的潜在作用。
