载PLGA纳米颗粒的无花果叶提取物:制备、表征及其对TFK-1细胞系的体外抗癌活性

Bushra Aziz, Esmeralda Dc Bosman, Kim Mg van der Wurff-Jacobs, Cornelus F van Nostrum, Ahmat Khurshid
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摘要

无花果提取物(Ficus Carica extract, FC)是一种天然草药,因其对多种恶性肿瘤具有潜在的抗癌活性而在癌症治疗中受到广泛关注。然而,由于FC的低生物利用度和低溶解度,限制了其作为抗癌药物的临床应用。本研究旨在制备载fc的PLGA纳米颗粒(NPs)用于癌症治疗。采用紫外可见光谱(UV-Vis)、动态光散射(DLS)、zeta电位(zeta potential)和透射电子显微镜(TEM)对制备的NPs进行了表征。结果表明,负载fc的球形PLGA NPs粒径为162±0.7 nm,多分散性指数为0.08±0.005,zeta电位为-4.7±0.6 mV。包封率为56±2.3%,装药率为14±1.5%。一项药物释放研究表明了一种基于扩散的释放谱。对TFK-1细胞株进行细胞毒性评价,结果表明NPs中游离FC和相应浓度的FC均具有细胞毒性。细胞周期分析表明,FC在G0/G1期阻滞细胞,与自由形态相比,FC负载的NPs细胞阻滞率更高。一项光毒性研究也表明,与游离FC相比,负载FC的PLGA NPs的光毒性随时间而增强。该研究结果表明,fc封装的PLGA NPs作为一种基于植物和光治疗剂的系统,在癌症治疗中具有很大的前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Ficus caricaleaves extract-loaded PLGA nanoparticles: preparation, characterization, andin vitroanticancer activity on TFK-1 cell line.

Ficus caricaextract (FCe) is a natural herb that has received a lot of interest in cancer treatment due to its potential anticancer activities against various malignancies. However, due to FCe's low bioavailability and low solubility, its clinical use as an anti-cancer medicine is constrained. The current study aimed to prepare FCe-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) for cancer treatment. Prepared NPs were characterized by UV-v is spectroscopy, dynamic light scattering, zeta potential, and transmission electron microscopy. The results showed that the spherical FCe-loaded PLGA NPs had a particle size of 162 ± 0.7 nm, a polydispersity index of 0.08 ± 0.005, and a zeta potential of -4.7 ± 0.6 mV. The encapsulation and loading efficiency were found to be 56 ± 2.3% and 14 ± 1.5%, respectively. A drug release study indicated a diffusion-based release profile. Cytotoxicity was evaluated on the extrahepatic bile duct carcinoma (TFK-1) cell line, which showed that both free FCe and corresponding FCe concentrations in NPs were cytotoxic. Cell cycle analysis showed that the FCe arrests the cells in G0/G1 phase, and the cell arrest rate is higher in FCe-loaded NPs compared to free form. A phototoxicity study also showed that the phototoxicity of FCe-loaded PLGA NPs was time-dependent and enhanced in comparison to free FCe. The study's results demonstrated that FCe-encapsulated PLGA NPs are promising for cancer therapy as a phyto- and phototherapeutic agent-based system.

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