Al-Samydai Ali, Al Qaraleh Moath, Al-Halaseh Lidia K, Abu Hajleh Maha N, Carradori Simone, Abdulmaged Maryam, Kareem Rand, Alzaidi Hasanain, Mousa Mohamad Ak, Al-Hiari Yusuf, Nsairat Hamdi, Alshaer Walhan
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Pharmacological and Diagnostic Research Centre, Al-Ahliyya Amman University, Amman, 19328, Jordan.
Department of Medical Laboratory Sciences, Faculty of Allied Medical Sciences, Al-Balqa Applied University, Al-Salt, Jordan.
Anticancer Agents Med Chem. 2025;25(12):859-872. doi: 10.2174/0118715206231749241209073759.
This study aims to enhance the delivery of polyphenols using nanotechnology.
To develop and evaluate liposomal formulations for improved delivery and stability of polyphenols, specifically focusing on Rutin.
Liposomal formulations were meticulously prepared via the Thin-Film Hydration method. Comprehensive physical characterization was conducted, including stability assessments using Dynamic Light Scattering (DLS) and Thermogravimetric Analysis (TGA). The free radical scavenging activity was measured using the DPPH• assay, and MTT cell viability assays were performed to assess anti-proliferative effects.
The results demonstrated a significant reduction in nanoparticle size from 123 nm to 116 nm and an increase in charge from -14 to -22 with rising Rutin concentrations. The formulation achieved enhanced homogeneity at a Rutin concentration of 2.0 mg/mL and showed higher stability. Incorporating Rutin improved the formulation's stability over 30 days, as evidenced by a decrease in the Differential Scanning Calorimetry peak temperature from 58.65°C to 54.42°C. Rutin-loaded and co-loaded nanoliposomes exhibited remarkable selectivity against PANC1 and MCF7 cell lines, with IC50 values of 2.13±0.35 μg/mL and 4.75±0.19 μg/mL, respectively.
PEGylated Rutin-loaded nanoliposomes offer a promising platform for biodegradable and biocompatible drug delivery systems, enhancing the bioavailability, solubility, and stability of the polyphenols.
本研究旨在利用纳米技术提高多酚的递送效果。
开发并评估脂质体制剂,以改善多酚尤其是芦丁的递送和稳定性。
通过薄膜水化法精心制备脂质体制剂。进行了全面的物理表征,包括使用动态光散射(DLS)和热重分析(TGA)进行稳定性评估。使用DPPH• 法测定自由基清除活性,并进行MTT细胞活力测定以评估抗增殖作用。
结果表明,随着芦丁浓度的增加,纳米颗粒尺寸从123 nm显著减小至116 nm,电荷从 -14增加至 -22。该制剂在芦丁浓度为2.0 mg/mL时实现了更高的均匀性,并表现出更高的稳定性。加入芦丁可使制剂在30天内的稳定性提高,差示扫描量热法峰温度从58.65°C降至54.42°C即可证明。负载芦丁和共负载的纳米脂质体对PANC1和MCF7细胞系表现出显著的选择性,IC50值分别为2.13±0.35 μg/mL和4.75±0.19 μg/mL。
聚乙二醇化负载芦丁的纳米脂质体为可生物降解和生物相容的药物递送系统提供了一个有前景的平台,提高了多酚的生物利用度、溶解度和稳定性。