多功能的、靶向CD44v6的有机硅纳米颗粒增强癌细胞中的药物毒性。
Multifunctional, CD44v6-Targeted ORMOSIL Nanoparticles Enhance Drugs Toxicity in Cancer Cells.
作者信息
Morillas-Becerril Lucía, Peta Elektra, Gabrielli Luca, Russo Venera, Lubian Elisa, Nodari Luca, Ferlin Maria Grazia, Scrimin Paolo, Palù Giorgio, Barzon Luisa, Castagliuolo Ignazio, Mancin Fabrizio, Trevisan Marta
机构信息
Dipartimento di Scienze Chimiche, Università di Padova, via Marzolo 1, 35131 Padova, Italy.
Department of Molecular Medicine, University of Padova, via Gabelli 63, 35121 Padova, Italy.
出版信息
Nanomaterials (Basel). 2020 Feb 10;10(2):298. doi: 10.3390/nano10020298.
Drug-loaded, PEGylated, organic-modified silica (ORMOSIL) nanoparticles prepared by microemulsion condensation of vinyltriethoxysilane (VTES) were investigated as potential nanovectors for cancer therapy. To target cancer stem cells, anti-CD44v6 antibody and hyaluronic acid (HA) were conjugated to amine-functionalized PEGylated ORMOSIL nanoparticles through thiol-maleimide and amide coupling chemistries, respectively. Specific binding and uptake of conjugated nanoparticles were studied on cells overexpressing the CD44v6 receptor. Cytotoxicity was subsequently evaluated in the same cells after the uptake of the nanoparticles. Internalization of nanocarriers loaded with the anticancer drug 3N-cyclopropylmethyl-7-phenyl-pyrrolo- quinolinone (MG2477) into cells resulted in a substantial increase of the cytotoxicity with respect to the free formulation. Targeting with anti-CD44v6 antibodies or HA yielded nanoparticles with similar effectiveness, in their optimized formulation.
通过乙烯基三乙氧基硅烷（VTES）的微乳液缩合制备的载药聚乙二醇化有机改性二氧化硅（ORMOSIL）纳米颗粒被研究作为癌症治疗的潜在纳米载体。为了靶向癌症干细胞，抗CD44v6抗体和透明质酸（HA）分别通过硫醇-马来酰亚胺和酰胺偶联化学与胺功能化的聚乙二醇化ORMOSIL纳米颗粒缀合。在过表达CD44v6受体的细胞上研究了缀合纳米颗粒的特异性结合和摄取。随后在摄取纳米颗粒后在相同细胞中评估细胞毒性。载有抗癌药物3N-环丙基甲基-7-苯基-吡咯并喹啉酮（MG2477）的纳米载体内化到细胞中导致相对于游离制剂细胞毒性大幅增加。在其优化制剂中，用抗CD44v6抗体或HA靶向产生具有相似效力的纳米颗粒。
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