Quercetin, a bioactive flavonoid derived from plants, exhibits broad-spectrum antitumor effects but suffers from limited clinical translation due to its low water solubility and poor pharmacokinetic profile. This study presents a novel quercetin-loaded Soluplus micellar system designed to overcome these limitations through enhanced solubilization and targeted delivery. The micelles were fabricated via thin-film hydration, resulting in nanoparticles with an average size of 55.3 ± 1.8 nm, high stability over nine months, and near-complete encapsulation efficiency at an optimal Soluplus-to-quercetin ratio of 16:1. These physicochemical properties indicate suitability for systemic administration and sustained drug release.
In vitro evaluations using human umbilical vein endothelial cells (HUVECs) demonstrated that Soluplus-Que micelles significantly improved cellular internalization of quercetin compared to free quercetin. Confocal microscopy confirmed that the micelles were efficiently taken up by HUVECs and localized within lysosomes and mitochondria—organelles central to drug action and cytotoxicity. As a result, MTT assays revealed a marked increase in cytotoxicity, with greater inhibition of cell proliferation observed in the micelle-treated group after 48 hours.28399-31-7 site
Functional assays further confirmed the anti-angiogenic potential of the formulation.KCNN4 Antibody Protocol Soluplus-Que micelles effectively suppressed HUVEC migration in wound healing assays and inhibited transwell invasion, indicating interference with key steps in angiogenesis. Moreover, the ability of HUVECs to form capillary-like structures on Matrigel was significantly impaired, demonstrating disruption of vascular network formation. In vivo, the chick chorioallantoic membrane (CAM) assay showed a dose-dependent reduction in blood vessel development following treatment with Soluplus-Que, reinforcing the compound’s ability to inhibit neovascularization.PMID:34632867
In a murine H22 tumor xenograft model, oral administration of Soluplus-Que micelles led to significant suppression of tumor growth without adverse effects on body weight or organ morphology. Histological analysis revealed reduced microvessel density in tumor tissues, as evidenced by decreased CD31 immunostaining. Additionally, expression levels of key angiogenic markers—including p-PI3K, p-Akt, and VEGF—were markedly downregulated in tumors treated with Soluplus-Que, confirming pathway-specific inhibition. Notably, when combined with the PI3K inhibitor LY294002, the suppressive effect on the PI3K/Akt/VEGF axis was even more pronounced, suggesting synergistic potential.
These findings collectively demonstrate that Soluplus-based nanomicelles not only enhance the delivery and retention of quercetin in target tissues but also potentiate its antitumor activity by modulating critical signaling pathways involved in angiogenesis. By enabling sustained release, improving cellular uptake, and targeting the PI3K/Akt/VEGF cascade, this delivery system offers a robust platform for the effective use of natural compounds in cancer therapy.MedChemExpress (MCE) offers a wide range of high-quality research chemicals and biochemicals (novel life-science reagents, reference compounds and natural compounds) for scientific use. We have professionally experienced and friendly staff to meet your needs. We are a competent and trustworthy partner for your research and scientific projects.Related websites: https://www.medchemexpress.com