Zhao Chenhui, Chang Thomas Ming Swi
Artificial Cells and Organs Research Centre, Departments of Physiology, Medicine and Biomedical Engineering, Faculty of Medicine and Health Sciences, McGill University, Montreal, QC H3G 1Y6, Canada.
Pharmaceuticals (Basel). 2025 Jun 30;18(7):980. doi: 10.3390/ph18070980.
Quercetin is a flavonoid found in various dietary sources. It is a prodrug converted by overexpressed tyrosinase in melanoma into an active o-quinone that suppresses tumour growth. However, injected quercetin is rapidly cleared from the tumour site. Our study aimed to enhance quercetin's efficacy through nanoencapsulation using biodegradable nanocapsules, which were tested in both mouse and human melanoma cell lines in 2D and 3D models. Nanoencapsulation achieved sustained release and improved bioavailability. In mouse 2D cultures, quercetin nanocapsules (Q-nanos) reduced cell viability to 28%, compared with 46% for free quercetin (Q-only) ( < 0.05). In 3D cultures simulating in vivo conditions, Q-nanos reduced viability to 43%, showing significant anti-melanoma activity, while Q-only resulted in 72% viability ( > 0.05 vs. control). A similar trend was observed in human melanotic melanoma, where both Q-nanos and Q-only were effective compared with the controls, with Q-nanos demonstrating superior tumour inhibition ( < 0.05). These findings show the superior efficacy of nanoencapsulated quercetin over free quercetin. Nanoencapsulation prolonged quercetin's bioavailability, enhanced tumour regression, and addressed limitations associated with the rapid clearance of free quercetin.
槲皮素是一种存在于多种膳食来源中的类黄酮。它是一种前体药物，在黑色素瘤中由过度表达的酪氨酸酶转化为具有抑制肿瘤生长作用的活性邻醌。然而，注射的槲皮素会迅速从肿瘤部位清除。我们的研究旨在通过使用可生物降解的纳米胶囊进行纳米封装来提高槲皮素的疗效，并在二维和三维模型的小鼠和人类黑色素瘤细胞系中进行了测试。纳米封装实现了持续释放并提高了生物利用度。在小鼠二维培养中，槲皮素纳米胶囊（Q-纳米）将细胞活力降低至28%，而游离槲皮素（仅Q）为46%（<0.05）。在模拟体内条件的三维培养中，Q-纳米将活力降低至43%，显示出显著的抗黑色素瘤活性，而仅Q导致72%的活力（与对照组相比>0.05）。在人类黑色素瘤中也观察到了类似的趋势，其中与对照组相比，Q-纳米和仅Q均有效，Q-纳米显示出更强的肿瘤抑制作用（<0.05）。这些发现表明纳米封装的槲皮素比游离槲皮素具有更高的疗效。纳米封装延长了槲皮素的生物利用度，增强了肿瘤消退，并解决了与游离槲皮素快速清除相关的局限性。
