Presently, most of anticancer drugs are high toxic for normal cells and, and as a result, they have severe side effects. Moreover, most of the formulations are lipophilic and have poor selectivity. To overcome these limitations, various drug delivery systems could be proposed. The aim of the current study was to fabricate novel polysaccharide nanocontainers (NC) by one‐step ultrasonication technique and to evaluate their accumulation efficacy and cytotoxicity in 2D (monolayer culture) and 3D (tumor spheroids) in vitro models. NC with mean sizes in a range of 340–420 nm with the core‐shell structure are synthetized and characterized. The NC shell is composed from diethylaminoethyl dextran/xanthan gum polyelectrolyte complex, while the hydrophobic core was loaded with the lipophilic anticancer drug thymoquinone. To enhance NC accumulation in human breast adenocarcinoma MCF‐7 cells, the NC surface was modified with poly‐L‐lysine (PLL) or polyethylene glycol. Cell uptake of the NC loaded with Nile Red into the tumor cells was investigated by laser scanning confocal microscopy, fluorescent flow cytometry and fluorimetry. Modification of the NC with PLL allowed to obtain the optimal drug delivery system with maximal cytotoxicity, which was tested by MTT‐test. The developed NC are promising for lipophilic anticancer drug delivery.

中文翻译：

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在 3D 体外模型中制备和评估用于亲脂性抗癌药物递送的纳米容器

目前，大多数抗癌药物对正常细胞具有高毒性，因此具有严重的副作用。此外，大多数制剂是亲脂性的，选择性较差。为了克服这些限制，可以提出各种药物输送系统。本研究的目的是通过一步超声技术制造新型多糖纳米容器（NC），并在 2D（单层培养）和 3D（肿瘤球体）体外模型中评估其积累效率和细胞毒性。合成和表征了平均尺寸在 340-420 nm 范围内的核壳结构的 NC。NC 壳由二乙氨基乙基葡聚糖/黄原胶聚电解质复合物组成，而疏水核则装载有亲脂性抗癌药物百里醌。为了增强人乳腺癌 MCF-7 细胞中 NC 的积累，用聚 L-赖氨酸 (PLL) 或聚乙二醇对 NC 表面进行了修饰。通过激光扫描共聚焦显微镜、荧光流式细胞术和荧光测定法研究了载有尼罗红的 NC 进入肿瘤细胞的细胞摄取。用 PLL 修改 NC 可以获得具有最大细胞毒性的最佳药物输送系统，该系统通过 MTT 测试进行了测试。开发的NC有望用于亲脂性抗癌药物递送。用 PLL 修改 NC 可以获得具有最大细胞毒性的最佳药物输送系统，该系统通过 MTT 测试进行了测试。开发的NC有望用于亲脂性抗癌药物递送。用 PLL 修改 NC 可以获得具有最大细胞毒性的最佳药物输送系统，该系统通过 MTT 测试进行了测试。开发的NC有望用于亲脂性抗癌药物递送。