Faculty of Pharmacy, Pharmacological and Diagnostic Research Center, Al-Ahliyya Amman University, Amman, Jordan.
Cell Therapy Center, The University of Jordan, Amman, 11942, Jordan.
Chem Biodivers. 2023 Aug;20(8):e202300534. doi: 10.1002/cbdv.202300534. Epub 2023 Aug 4.
Olive leaf extract is a valuable source of phenolic compounds; primarily, oleuropein (major component) and rutin. This natural olive leaf extract has potential use as a therapeutic agent for cancer treatment. However, its clinical application is hindered by poor pharmacokinetics and low stability. To overcome these limitations, this study aimed to enhance the anticancer activity and stability of oleuropein and rutin by loading them into PEGylated Nano-phytosomes. The developed PEGylated Nano-phytosomes exhibited favorable characteristics in terms of size, charge, and stability. Notably, the anticolonic cancer activity of the Pegylated Nano-phytosomes loaded with oleuropein (IC50=0.14 μM) and rutin (IC50=0.44 μM) surpassed that of pure oleuropein and rutin alone. This outcome highlights the advantageous impact of Nano-phytosomes to augment the anticancer potential of oleuropein and rutin. These results present a promising pathway for the future development of oleuropein and rutin Nano-phytosomes as effective options for passive tumor-targeted therapy, given their improved stability and efficacy.
橄榄叶提取物是酚类化合物的重要来源，主要包括橄榄苦苷（主要成分）和芦丁。这种天然橄榄叶提取物具有作为癌症治疗治疗剂的潜在用途。然而，其临床应用受到药代动力学不佳和稳定性低的限制。为了克服这些限制，本研究旨在通过将橄榄苦苷和芦丁载入聚乙二醇化纳豆孢体中来增强其抗癌活性和稳定性。所开发的聚乙二醇化纳豆孢体在大小、电荷和稳定性方面表现出良好的特性。值得注意的是，载有橄榄苦苷（IC50=0.14 μM）和芦丁（IC50=0.44 μM）的聚乙二醇化纳豆孢体的抗结肠癌细胞活性超过了纯橄榄苦苷和芦丁单独使用的活性。这一结果突出了纳豆孢体的优势，增强了橄榄苦苷和芦丁的抗癌潜力。这些结果为未来开发作为被动肿瘤靶向治疗有效选择的橄榄苦苷和芦丁纳豆孢体提供了有希望的途径，因为它们提高了稳定性和功效。
