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包裹在聚乳酸-羟基乙酸共聚物(PLGA)纳米载体中的印度法贡提取物通过改善光活性代谢物的细胞内摄取表现出增强的治疗效果。

Fagonia indica extract encapsulated in PLGA nanocarriers demonstrated enhanced therapeutic efficacy through improved intracellular uptake of photoactive metabolites.

作者信息

Naz Saba, Khurshid Ahmat, Hassan Syed Mujtaba Ul, Afsar Tayyaba, Javaid Sumbal, Husain Fohad Mabood, Trembley Janeen H, Razak Suhail

机构信息

Department of Physics & Applied Mathematics (DPAM), PIEAS, Islamabad, 45650, Pakistan.

Department of Metallurgy & Materials Engineering (DMME), PIEAS, Islamabad, 45650, Pakistan.

出版信息

Sci Rep. 2025 Jul 2;15(1):23140. doi: 10.1038/s41598-025-05163-1.

Abstract

Fagonia indica (FI), a member of the Zygophyllaceae family, is known for its medicinally important components, such as glycosides, saponins, flavonoids, phenols, and alkaloids. The complex mixture of phytochemicals in the extract limits its aqueous solubility and bioavailability, resulting in low therapeutic outcomes. We aim to enhance the bioavailability of FI extract by encapsulating it into Poly (lactic-co-glycolic acid) (PLGA) nanoparticles (FI-PLGA NPs) and evaluate its cytotoxicity and phototoxicity against the BT-474 cell line. FI-PLGA NPs were prepared via a single emulsion solvent evaporation method. The optical properties, structural analysis, and hydrodynamic size of the synthesized NPs were characterised by UV-Visible spectroscopy, fluorescence spectroscopy, Fourier transform infrared (FTIR) spectrometry, X-ray diffraction (XRD) spectroscopy, and Dynamic light scattering (DLS). The measured particle size and zeta potential of FI-PLGA NPs were 217 nm and -30.5 mV, respectively. The in-vitro cytotoxicity and phototoxicity of FI extract and FI-PLGA NPs were measured using MTT assay. Results suggest that decreased cell viability is associated with higher intracellular concentration and fast drug internalisation when loaded on a nanocarrier compared to free extract. Moreover, a significant reduction in cell viability was observed after irradiation of light doses of 6 J/cm2 and 12 J/cm2. FI-PLGA NPs showed a higher cytotoxic effect against the BT-474 cell line than free FI extract, possibly due to prolonged and sustained drug release and faster cellular internalization of FI-PLGA NPs. Using a PLGA nanocarrier significantly improved the intracellular uptake of photoactive metabolites from the extract of Fagonia indica, enhancing the plant's therapeutic efficacy. The in-vivo anti-cancer potential of FI- PLGA NPs needs to be investigated to validate the effectiveness of these nano-formulations and open the door for their potential application in clinical settings.

摘要

刺山柑(Fagonia indica,FI)是蒺藜科的一员,以其具有重要药用价值的成分而闻名,如糖苷、皂苷、黄酮类化合物、酚类和生物碱。提取物中复杂的植物化学成分混合物限制了其水溶性和生物利用度,导致治疗效果不佳。我们旨在通过将FI提取物封装到聚(乳酸 - 乙醇酸)(PLGA)纳米颗粒(FI-PLGA NPs)中来提高其生物利用度,并评估其对BT-474细胞系的细胞毒性和光毒性。FI-PLGA NPs通过单乳液溶剂蒸发法制备。通过紫外 - 可见光谱、荧光光谱、傅里叶变换红外(FTIR)光谱、X射线衍射(XRD)光谱和动态光散射(DLS)对合成纳米颗粒的光学性质、结构分析和流体动力学尺寸进行了表征。测得的FI-PLGA NPs的粒径和zeta电位分别为217 nm和 -30.5 mV。使用MTT法测定了FI提取物和FI-PLGA NPs的体外细胞毒性和光毒性。结果表明,与游离提取物相比,负载在纳米载体上时,细胞活力下降与更高的细胞内浓度和更快的药物内化有关。此外,在照射6 J/cm2和12 J/cm2的光剂量后,观察到细胞活力显著降低。FI-PLGA NPs对BT-474细胞系的细胞毒性作用比游离FI提取物更高,这可能是由于FI-PLGA NPs的药物释放延长且持续,以及细胞内化更快。使用PLGA纳米载体显著提高了刺山柑提取物中光活性代谢物的细胞内摄取,增强了该植物的治疗效果。需要研究FI-PLGA NPs的体内抗癌潜力,以验证这些纳米制剂的有效性,并为其在临床环境中的潜在应用打开大门。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/28ac/12222523/d4a29cff183a/41598_2025_5163_Fig1_HTML.jpg

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