Advancing Liposomal Coating Approaches for Improved Anticancer Drug Delivery.

IF 3 4区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY ChemPlusChem Pub Date : 2024-10-23 DOI:10.1002/cplu.202400600

Ngoc Thuy Trang Le, Anh-Minh Nguyen-Huu, Dai Hai Nguyen, Cuu Khoa Nguyen

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Abstract

Quercetin, a natural flavonoid with antioxidant, anti-inflammatory, and anticancer properties, faces limitations in clinical application due to its poor solubility and bioavailability. This study presents a novel delivery system utilizing a combination of polyoxyethylene (100) stearyl ether and folic acid to enhance quercetin's effectiveness. We developed folate-conjugated polyoxyethylene (100) stearyl ether-coated liposomes (FA-Brij-LPs) to leverage the unique properties of polyoxyethylene (100) stearyl ether in conjunction with folic acid for targeted delivery. The FA-Brij-LPs were prepared using the thin-film hydration method and characterized for their physicochemical properties, including size, zeta potential, and drug loading capacity. The optimized FA-Brij-LPs exhibited a mean particle size of 147.57 nm, a zeta potential of 32.20 mV, and a drug loading capacity of 9.33 %. In vitro studies demonstrated sustained quercetin release and significantly enhanced cellular uptake compared to free quercetin. The Resazurin cell viability assay further revealed superior anticancer efficacy of FA-Brij-LPs. This innovative approach underscores the effectiveness of combining polyoxyethylene (100) stearyl ether with folic acid in enhancing quercetin delivery and its potential applications in cancer therapy.

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推进脂质体包衣方法，改善抗癌药物的输送。

槲皮素是一种具有抗氧化、抗炎和抗癌特性的天然类黄酮，但由于其溶解性和生物利用度较差，在临床应用中受到限制。本研究提出了一种新型给药系统，利用聚氧乙烯（100）硬脂基醚和叶酸的组合来增强槲皮素的功效。我们开发了叶酸共轭聚氧乙烯（100）硬脂醯醚包被脂质体（FA-Brij-LPs），利用聚氧乙烯（100）硬脂醯醚的独特性质与叶酸结合进行靶向给药。采用薄膜水合法制备了 FA-Brij-LPs，并对其理化性质进行了表征，包括尺寸、ZETA 电位和载药量。优化后的 FA-Brij-LPs 平均粒径为 147.57 nm，zeta 电位为 32.20 mV，载药量为 9.33%。体外研究表明，与游离槲皮素相比，槲皮素可持续释放并显著提高细胞吸收率。Resazurin细胞活力测定进一步显示了FA-Brij-LPs卓越的抗癌功效。这种创新方法强调了聚氧乙烯（100）硬脂基醚与叶酸的结合在增强槲皮素递送及其在癌症治疗中的潜在应用方面的有效性。

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来源期刊

ChemPlusChem CHEMISTRY, MULTIDISCIPLINARY-

CiteScore

5.90

自引率

0.00%

发文量

200

审稿时长

1 months

期刊介绍： ChemPlusChem is a peer-reviewed, general chemistry journal that brings readers the very best in multidisciplinary research centering on chemistry. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. Fully comprehensive in its scope, ChemPlusChem publishes articles covering new results from at least two different aspects (subfields) of chemistry or one of chemistry and one of another scientific discipline (one chemistry topic plus another one, hence the title ChemPlusChem). All suitable submissions undergo balanced peer review by experts in the field to ensure the highest quality, originality, relevance, significance, and validity.