Development of Pegylated Nano‐Phytosome Formulation with Oleuropein and Rutin to Compare Anti‐Colonic Cancer Activity with Olea Europaea Leaves Extract

Abstract

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.

Encapsulation of gingerol into nanoliposomes: Evaluation of in vitro anti‐inflammatory and anti‐cancer activity

“…The release stability experiment was performed in triplicates where 150 μL of samples was withdrawn at different time points (0 h, 24 h, 48 h, 72 h, 96 h, 120 h, 144 h, 168 h, 1 week, 2 weeks, 3 weeks, and 4 weeks), and centrifuged at 8000 rpm for 10 min to remove free 6‐gingerol (Al‐Samydai et al, 2021; Mahmood et al, 2023). After 48 h of collection, 600 μL of acetonitrile was added to all the samples to degrade encapsulation liposomes as mentioned earlier.…”

Preparation, Characterization, and Anticancer Activity of PEGylated Nano Liposomal Loaded with Rutin against Human Carcinoma Cells (HT‐29)

“…Rutin liposomes (RLs) were prepared by the thin film hydration method previously described by Al-Samydai et al [39] The lipids utilized were Cholesterol and Hydrogenated Soybean Phosphatidylcholine (HSPC). Polyethylene Glycol (PEG) was used as a stealth stabilizer.…”

“…Rutin has been extensively studied for its anticancer properties, demonstrating its ability to induce apoptosis and halt the cell cycle in both in vivo and in vitro cancer cell studies [11,13] …”

“…[12] Rutin has been extensively studied for its anticancer properties, demonstrating its ability to induce apoptosis and halt the cell cycle in both in vivo and in vitro cancer cell studies. [11,13] Nanotechnology and nanomedicine are emerging fields that have made significant progress in enhancing the pharmacokinetics and therapeutic effectiveness of drugs. [14,15] Pharmaceutical delivery systems have been able to enhance drug distribution, achieve targeted controlled release, prolong circulation time, increase intracellular concentration, and improve the solubility and stability of drugs through the use of nanoparticles and liposomes.…”

Oleuropein impact on colorectal cancer

“…Plant-derived phenolic molecules are the most significant active compounds involved in anti-colorectal cancer actions [ 11 , 12 ]. Oleuropein (OLR) is the most efficient phenolic molecule for reducing cancer cell viability in various categories of cancer as breast, gastric and kidney [ 13 , 14 ]. OLR is a phenolic substance that is mostly discovered in various parts of the olive tree, mainly in their leaves [ 15 , 16 ].…”