Preparation, characterization and in vitro evaluation of anticancer and antioxidant effects of luteolin-loaded nanocapsules

IF 4.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY Journal of Drug Delivery Science and Technology Pub Date : 2025-02-25 DOI:10.1016/j.jddst.2025.106754
Giuseppe Granata , Paolo Accardo , Claudia Giovanna Leotta , Giovanni Mario Pitari , Giorgia Fangano , Francesco Ruffino , Corrada Geraci , Grazia Maria Letizia Consoli
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Abstract

Luteolin (Lut) is a natural flavonoid compound endowed with medicinal properties but suffering from low water-solubility, stability, and bioavailability which limit its use in pharmaceutical applications. Encapsulation of luteolin in nanocarriers is providing a viable approach to overcome these drawbacks. Here, we used a nanoprecipitation method to prepare luteolin-loaded nanocapsules composed of poly(ε-caprolactone), Tween 80, soybean oil, and phosphatidylcholine at two different amounts. The luteolin-loaded nanocapsules showed nanometric size, very narrow polydispersity index, negative Zeta potential, excellent encapsulation efficiency, high size stability and good luteolin retention also under thermal stress conditions The phosphatidylcholine content influenced the amount of encapsulated drug, and the nanocapsules with higher luteolin content were successfully tested for ROS scavenger effects and cytotoxicity against human colon adenocarcinoma HCT116 cells. The luteolin-loaded nanocapsules that increased luteolin water solubility and stability and preserved the luteolin biological activity, appear promising for pharmaceutical applications.

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木犀草素纳米胶囊的制备、表征及抗癌抗氧化作用的体外评价
木犀草素(Lut)是一种具有药用价值的天然类黄酮化合物,但其水溶性、稳定性和生物利用度较低,限制了其在医药领域的应用。木犀草素包封在纳米载体中提供了一种可行的方法来克服这些缺点。本研究采用纳米沉淀法制备了由聚(ε-己内酯)、t80、大豆油和磷脂酰胆碱组成的载木犀草素纳米胶囊。在热应激条件下,木犀草素纳米胶囊具有纳米尺寸、极窄的多分散指数、负的Zeta电位、优良的包封效率、高的尺寸稳定性和良好的木犀草素保留率。磷脂酰胆碱含量影响包封药物的量,并成功测试了高木犀草素纳米胶囊对人大肠腺癌HCT116细胞的ROS清除作用和细胞毒性。负载木犀草素的纳米胶囊提高了木犀草素的水溶性和稳定性,并保持了木犀草素的生物活性,在医药领域具有广阔的应用前景。
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来源期刊
CiteScore
8.00
自引率
8.00%
发文量
879
审稿时长
94 days
期刊介绍: The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.
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