Abstract Chitosan, a natural, hydrophilic and biodegradable polymer was grafted on Fe3O4 magnetic nanoparticles (MNPs) and used as a carrier of poorly water-soluble anticancer drug Telmisartan (TEL). The characteristics of MNPs and chitosan coated MNPs (MNP-CS) were determined by using X-ray diffraction, field emission scanning electron microscope, transmission electron microscope, vibrating sample magnetometer, and BET surface area analyzer. The chitosan coating of MNPs was validated by Fourier transform infrared spectroscopy (FTIR) and thermal gravimetric analysis. The drug was loaded on MNP-CS through an amide bond between amino groups of chitosan and carboxylic groups of TEL. The drug loading capacity of ~50% was obtained due to the large BET surface area (134 m2/g) of mesoporous MNP-CS. Drug loaded MNP-CS (MNP–CS–TEL) showed pH-responsive controlled release characteristics. The MNP–CS–TEL showed dose dependent cytotoxicity towards PC-3 human prostate cancer cells. The results demonstrated the significant antitumor activity of designed nanoformulation.

中文翻译：

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壳聚糖包被的磁性纳米粒子作为抗癌药物替米沙坦的载体：pH 响应控制药物释放和细胞毒性研究

摘要 壳聚糖是一种天然、亲水且可生物降解的聚合物，接枝在 Fe3O4 磁性纳米粒子 (MNPs) 上，用作水溶性差的抗癌药物替米沙坦 (TEL) 的载体。使用X射线衍射、场发射扫描电子显微镜、透射电子显微镜、振动样品磁强计和BET表面积分析仪测定了MNPs和壳聚糖包覆的MNPs（MNP-CS）的特性。通过傅里叶变换红外光谱 (FTIR) 和热重分析验证了 MNP 的壳聚糖涂层。该药物通过壳聚糖的氨基和 TEL 的羧基之间的酰胺键负载在 MNP-CS 上。由于介孔 MNP-CS 的 BET 表面积大 (134 m2/g)，因此获得了约 50% 的载药量。载药 MNP-CS (MNP-CS-TEL) 显示出 pH 响应性控释特性。MNP-CS-TEL 显示出对 PC-3 人前列腺癌细胞的剂量依赖性细胞毒性。结果表明设计的纳米制剂具有显着的抗肿瘤活性。