Quercetin is a well-known flavonoid for its potent antitumor and antiproliferative effects on a wide range of human cancer cell lines. However, the delivery of quercetin is challenging due to its extreme insolubility in water. The intention of this study was to evaluate the antitumor effect of quercetin-loaded PEGylated liposomes (PEG-Que-NLs) in vitro and in vivo. We first prepared PEG-Que-NLs by method of thin film hydration; further determined, the optimum ratios of quercetin to Soybean phosphatidylcholine (SPC), to cholesterol (CHL), and to PEG-4000 were 1 : 8, 1 : 2, and 1 : 2 (), respectively, and the optimal hydration temperature was 55°C when the mean vesicle diameter and apparent Zeta potential of PEG-Que-NLs were found to be  nm and  mV, respectively; the encapsulation efficiency and the drug loading of PEG-Que-NLs were and , respectively. Drug release study in vitro showed that PEG-Que-NLs exhibited a slow-release effect without significant burst effect. Furthermore, the inhibition effect of PEG-Que-NLs on HeLa cells was considerably higher than free quercetin (free-Que) and quercetin liposomes (Que-NLs). Intravenous injection of PEG-Que-NLs into U14 bearing mouse models inhibited the cervical carcinoma growth significantly, and the tumor inhibition rate was much higher than free-Que and Que-NLs. These results of this study indicated that PEG-Que-NLs exhibited potential application prospects in the treatment of malignant tumors because of its tumor targeting, slow-release properties, and the solubility improvement of quercetin.

中文翻译：

---

由槲皮素制成的药物递送系统配制成聚乙二醇化脂质体对体外和体内宫颈癌的影响

槲皮素是一种众所周知的黄酮类化合物，因其对多种人类癌细胞系具有有效的抗肿瘤和抗增殖作用。然而，由于槲皮素极难溶于水，因此其递送具有挑战性。本研究的目的是评估载有槲皮素的聚乙二醇化脂质体 (PEG-Que-NLs)在体外和体内的抗肿瘤作用。我们首先通过薄膜水化的方法制备了PEG-Que-NLs；进一步确定，槲皮素与大豆磷脂酰胆碱 (SPC)、胆固醇 (CHL) 和 PEG-4000 的最佳比例为 1:8、1:2 和 1:2 ()，当发现 PEG-Que-NLs 的平均囊泡直径和表观 Zeta 电位为 55°C 时，最佳水合温度为 纳米和  mV，分别；PEG-Que-NLs 的包封率和载药量分别为 和 ，分别。体外药物释放研究表明，PEG-Que-NLs 具有缓释作用，但没有明显的爆发效应。此外，PEG-Que-NLs 对 HeLa 细胞的抑制作用明显高于游离槲皮素 (free-Que) 和槲皮素脂质体 (Que-NLs)。U14小鼠模型静脉注射PEG-Que-NLs可显着抑制宫颈癌的生长，抑瘤率远高于free-Que和Que-NLs。本研究结果表明，PEG-Que-NLs由于其肿瘤靶向性、缓释特性以及槲皮素溶解度的提高，在恶性肿瘤的治疗中具有潜在的应用前景。