Anticancer effect of green tea extract (GTE)-Loaded pH-responsive niosome Coated with PEG against different cell lines
Anticancer effect of green tea extract (GTE)-Loaded pH-responsive niosome Coated with PEG against different cell lines
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DOI：
10.1016/j.mtcomm.2020.101751
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发表时间：
2021-03-22
影响因子：
3.8
通讯作者：
Goodarzi, Vahabodin
中科院分区：
文献类型：
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作者：
Baranei, Mahmoud;Taheri, Ramezan Ali;Goodarzi, Vahabodin
尽管绿色茶提取物（GTE）具有优异的抗癌能力，但其生物利用度低、溶解度低和生物利用度差限制了其应用。本研究旨在设计和引入一种新的，稳定的血浆，pH值敏感的niosomal（NiO）配方的GTE使用薄膜水合过程。代替胆固醇，添加胆固醇半琥珀酸酯（CHEMS）以产生pH敏感性性质，并且使用聚乙二醇（PEG）（NiO / GTE / PEG / CHEMS），将pH敏感性和血浆稳定性性质同时整合到一个递送装置中。采用GC/MS、UV-vis、DLS、光学显微镜、SEM和TEM技术对制剂进行表征。在两种不同的缓冲液（pH 5和7.4）中体外评估具有pH敏感性的制剂的释放。对三种不同的MCF-7、HepG 2和HL-60癌细胞系和一种正常细胞系（HGF）进行体外pH敏感性细胞毒性实验，以保证制剂中对癌细胞的特异性。GTE的GC质量分析表明样品中含有多种抗癌多酚。pH响应制剂提供了积极的优势，包括pH敏感的缓释（在pH 5下24小时后约77%）遵循Higuchi释放动力学，球形表面的光滑形态，高捕获效率（81%），纳米直径（240 nm），以及3周后的高稳定性。将癌细胞暴露于Nio / GTE / PEG / CHEMS已经通过强细胞内化和协同毒性效应（> 50%;与游离GTE相比）证明了针对MCF-7、HepG 2和HL-60细胞系的优异性能。有趣的是，当用制剂处理时，正常细胞系（HGF）的活力百分比高于癌细胞，这表明制剂对癌细胞的选择性更高。稳定的血浆、pH敏感的类囊泡将提高生物利用度并加强GTE的细胞毒性作用。
Despite its excellent anti-cancer capacity in green tea extract (GTE), its applications are constrained by its low bioavailability solubility and poor bioavailability. This study aimed to design and introduce a new, stable plasma, pH-sensitive niosomal (Nio) formulation of GTE using a thin-film hydration process. Instead of cholesterol, cholesterol hemisuccinate (CHEMS) was added to generate pH-sensitivity properties and, using polyethylene glycol (PEG) (Nio / GTE / PEG / CHEMS), pH-sensitivity and plasma stability properties were integrated simultaneously into one delivery device. GC/MS, UV-vis, DLS, optical microscopy, SEM, and TEM techniques were used for the characterization of formulations. The release of formulations with pH-sensitivity was assessed in vitro in two different buffers (pH 5 and 7.4). In vitro pH-sensitivity cytotoxicity experiment was done on three different MCF-7, HepG2, and HL-60 cancer cell lines and one normal cell line (hGF) to guarantee specificity against cancer cells in the formulation. The GTE's mass assay with GC shows many anticancer polyphenols are in the sample. The pH-responsive formulation provided positive advantages, including pH-sensitive sustainedrelease (about 77 percent after 24 h at pH 5) followed Higuchi release kinetics, smooth morphology of the globular surface, high trapping efficiency (81 percent), nanometer diameter (240 nm), and high stability after 3 weeks. Exposure of cancer cells to Nio / GTE / PEG / CHEMS has demonstrated excellent performance against MCF-7, HepG2, and HL-60 cell lines by strong cell internalization and synergistic toxic effect (> 50 percent; compared to free GTE). Interestingly, when treated with the formulations, the viability percentage of the normal cell line (hGF) was higher than the cancer cells, which suggests the higher formulation selectivity against cancer cells. Stable plasma, pH-sensitive niosomes will improve bioavailability and strengthen GTE's cytotoxic effect.