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负载叶提取物的聚乳酸-羟基乙酸共聚物纳米颗粒:制备、表征及其对TFK-1细胞系的抗癌活性

leaves extract-loaded PLGA nanoparticles: preparation, characterization, andanticancer activity on TFK-1 cell line.

作者信息

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

机构信息

Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, 3584 CG Utrecht, The Netherlands.

Biophotonics and Photonanomedicine Research Laboratory, Department of Physics and Applied Mathematics, Pakistan Institute of Engineering and Applied Sciences (PIEAS), Nilore, Islamabad 45650, Pakistan.

出版信息

Biomed Mater. 2025 Feb 17;20(2). doi: 10.1088/1748-605X/adaff7.

Abstract

extract (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--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.

摘要

提取物(FCe)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,在癌症治疗方面受到了广泛关注。然而,由于FCe的生物利用度低和溶解度低,其作为抗癌药物的临床应用受到限制。本研究旨在制备用于癌症治疗的负载FCe的聚乳酸-乙醇酸共聚物(PLGA)纳米颗粒(NPs)。通过紫外可见光谱、动态光散射、zeta电位和透射电子显微镜对制备的NPs进行了表征。结果表明,球形的负载FCe的PLGA NPs粒径为162±0.7 nm,多分散指数为0.08±0.005,zeta电位为-4.7±0.6 mV。包封率和载药率分别为56±2.3%和14±1.5%。药物释放研究表明其释放曲线基于扩散。对肝外胆管癌(TFK-1)细胞系进行了细胞毒性评估,结果表明游离FCe和NPs中相应的FCe浓度均具有细胞毒性。细胞周期分析表明,FCe使细胞停滞在G0/G1期,与游离形式相比,负载FCe的NPs中细胞停滞率更高。光毒性研究还表明,负载FCe的PLGA NPs的光毒性具有时间依赖性,且与游离FCe相比有所增强。该研究结果表明,负载FCe的PLGA NPs作为一种基于植物和光疗剂的系统,在癌症治疗方面具有广阔前景。

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