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用于转铁蛋白受体介导的肿瘤特异性药物递送应用的HO响应性硼酸酯修饰的介孔二氧化硅纳米载体

HO-Responsive Boronic Ester-Modified Mesoporous Silica Nanocarrier for TfR Mediated Tumor-Specific Drug Delivery Applications.

作者信息

Lee Hsiao-Yen, Thirumalaivasan Natesan, Wu Shu-Pao

机构信息

Department of Applied Chemistry, National Yang Ming Chiao Tung University, Hsinchu 30010, Taiwan, Republic of China.

Department of Periodontics, Saveetha Dental College and Hospitals, Saveeta Institute of Medical and Technical Sciences (SIMATS), Chennai 600077, India.

出版信息

ACS Appl Bio Mater. 2025 Jul 21;8(7):6079-6087. doi: 10.1021/acsabm.5c00645. Epub 2025 Jun 23.

Abstract

This study introduces a drug delivery system utilizing boronic ester-functionalized mesoporous silica nanoparticles () for targeted cancer therapy. By conjugating transferrin (Tf) to the MSNP surface, the system actively targets cancer cells via transferrin receptor (TfR)-mediated endocytosis. The incorporation of boronic ester linkages enables hydrogen peroxide (HO)-responsive drug release, enhancing therapeutic efficacy. In vitro experiments demonstrated that effectively delivered doxorubicin (DOX) to cancer cells while sparing normal cells, as confirmed by fluorescence imaging and cytotoxicity assays. In vivo studies using a colon cancer xenograft model showed that inhibited tumor growth more effectively than free DOX. These findings highlight as a promising nanocarrier for cancer therapy, offering targeted and controlled drug delivery through active targeting and HO responsiveness.

摘要

本研究介绍了一种利用硼酸酯功能化介孔二氧化硅纳米颗粒()进行靶向癌症治疗的药物递送系统。通过将转铁蛋白(Tf)偶联到介孔二氧化硅纳米颗粒表面,该系统通过转铁蛋白受体(TfR)介导的内吞作用主动靶向癌细胞。硼酸酯键的引入实现了过氧化氢(HO)响应性药物释放,增强了治疗效果。体外实验表明,通过荧光成像和细胞毒性测定证实,能有效地将阿霉素(DOX)递送至癌细胞,同时使正常细胞免受影响。使用结肠癌异种移植模型的体内研究表明,比游离DOX更有效地抑制肿瘤生长。这些发现突出了作为一种有前景的癌症治疗纳米载体,通过主动靶向和HO响应性提供靶向和可控的药物递送。

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