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用于药物递送系统的碳水化合物聚电解质纳米颗粒的开发，该系统可穿越血脑屏障治疗脑肿瘤。

Development of Carbohydrate Polyelectrolyte Nanoparticles for Use in Drug Delivery Systems that Cross the Blood-Brain Barrier to Treat Brain Tumors.

作者信息

Silant'ev Vladimir E, Shmelev Mikhail E, Belousov Andrei S, Trukhin Fedor O, Struppul Nadezhda E, Patlay Aleksandra A, Kravchenko Anna K, Shchava Sergey P, Kumeiko Vadim V

机构信息

School of Medicine and Life Sciences, Far Eastern Federal University, Vladivostok 690922, Russia.

Laboratory of Electrochemical Processes, Institute of Chemistry, Far Eastern Branch of Russian Academy of Sciences, Vladivostok 690022, Russia.

出版信息

Polymers (Basel). 2025 Jun 18;17(12):1690. doi: 10.3390/polym17121690.

DOI:10.3390/polym17121690
PMID:40574222
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12196646/
Abstract

The low effectiveness of various brain cancer treatment methods is due to a number of significant challenges. Most of them are unable to penetrate the blood-brain barrier (BBB) when drugs are administered systemically through the bloodstream. Nanoscale particles play a special role among materials capable of binding drug molecules and successfully crossing the BBB. Biopolymeric nanoparticles (NPs) demonstrate excellent biocompatibility and have the remarkable ability to modify the environment surrounding tumor cells, thereby potentially improving cellular uptake of delivery agents. In our research, nanoscale polyelectrolyte complexes (PECs) ranging in size from 56 to 209 nm were synthesized by ionic interaction of the oppositely charged polysaccharides pectin and chitosan. The structural characteristics of these complexes were carefully characterized by infrared (FTIR) and Raman spectroscopy. The immobilization efficiency of antitumor drugs was comprehensively evaluated using UV spectrophotometry. The cytotoxicity of the NPs was evaluated in the U87-MG cell line. The preliminary data indicate a significant decrease in the metabolic activity of these tumor cells. Important details on the interaction of the NPs with an endothelial layer structurally similar to the BBB were obtained by simulating the BBB using a model based on human blood vessels. Our studies allowed us to establish a significant correlation between the kinetic parameters of drug immobilization and the ratio of biopolymer concentrations in the initial compositions, which provides valuable information for future optimization of drug delivery system design.

摘要

各种脑癌治疗方法效果不佳是由于一系列重大挑战。当通过血液循环全身给药时，它们中的大多数无法穿透血脑屏障（BBB）。在能够结合药物分子并成功穿过血脑屏障的材料中，纳米级颗粒发挥着特殊作用。生物聚合物纳米颗粒（NPs）表现出优异的生物相容性，并具有显著改变肿瘤细胞周围环境的能力，从而有可能提高递送剂的细胞摄取。在我们的研究中，通过带相反电荷的多糖果胶和壳聚糖的离子相互作用合成了尺寸范围为56至209nm的纳米级聚电解质复合物（PECs）。通过红外（FTIR）和拉曼光谱仔细表征了这些复合物的结构特征。使用紫外分光光度法全面评估了抗肿瘤药物的固定效率。在U87-MG细胞系中评估了NPs的细胞毒性。初步数据表明这些肿瘤细胞的代谢活性显著降低。通过使用基于人体血管的模型模拟血脑屏障，获得了关于NPs与结构类似于血脑屏障的内皮层相互作用的重要细节。我们的研究使我们能够确定药物固定的动力学参数与初始组合物中生物聚合物浓度之比之间的显著相关性，这为未来优化药物递送系统设计提供了有价值的信息。

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