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Stealth cross-linked polymeric nanoparticles for passive drug targeting: a combination of molecular docking and comprehensive in vitro assay
Bulletin of Materials Science ( IF 1.9 ) Pub Date : 2020-08-20 , DOI: 10.1007/s12034-020-02166-8
ABBAS HEMATI AZANDARYANI , SOHEILA KASHANIAN , YADOLLAH BAHRAMI , MOHSEN SHAHLAEI , KATAYOUN DERAKHSHANDEH , SAJAD MORADI

Till date, several studies have reported magnetic drug targeting as well as passive drug delivery. In this study, the passive characteristic of PEGylated carriers with a neutral surface charge rather than chitosan (CS)-based nanoparticles (NPs) with a positive charge was proved using molecular docking. The complete and without flaw stealth CS-coated magnetic NPs (mNPs) loaded with an anticancer drug for intravenous drug delivery were prepared using a modified ionic-crosslinking method. The physicochemical properties of the prepared magnetic-CS NPs were characterized in detail. The transmission electron micrographs of NPs showed an uniform particle morphology with an average diameter of smaller than 10 nm. The average IC50 values of the drug in PEGylated NPs for MCF-7 and PC-12 cells were 44 and 72 µM, respectively. The fabricated stealth NPs can increase the cytotoxicity and cell permeability of formulation that may release the entire drug in targeted shape to objective tissues that were firstly proved by molecular docking. This strategy showed a reduction in uptaking of mNPs by the reticuloendothelial system, which indeed increases the concentration of therapeutic agent(s) in the target site.

中文翻译:

用于被动药物靶向的隐形交联聚合物纳米颗粒:分子对接和综合体外检测的结合

迄今为止,已有多项研究报道了磁性药物靶向和被动药物递送。在这项研究中,使用分子对接证明了具有中性表面电荷的聚乙二醇化载体的被动特性,而不是具有正电荷的基于壳聚糖 (CS) 的纳米粒子 (NPs)。使用改进的离子交联方法制备了完整且无缺陷的隐形 CS 涂层磁性纳米颗粒(mNPs),其负载抗癌药物用于静脉给药。详细表征了制备的磁性 CS NPs 的理化性质。NPs 的透射电子显微照片显示出均匀的颗粒形态,平均直径小于 10 nm。对于 MCF-7 和 PC-12 细胞,该药物在聚乙二醇化 NPs 中的平均 IC50 值分别为 44 和 72 µM。制造的隐形纳米颗粒可以增加制剂的细胞毒性和细胞渗透性,可以将整个药物以靶向形状释放到目标组织,这首先通过分子对接得到证实。该策略显示网状内皮系统对 mNP 的摄取减少,这确实增加了靶位点中治疗剂的浓度。
更新日期:2020-08-20
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