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硫酸软骨素包覆的超顺磁性氧化铁纳米颗粒作为盐酸多柔比星的潜在载体。

Chondroitin sulfate-capped super-paramagnetic iron oxide nanoparticles as potential carriers of doxorubicin hydrochloride.

机构信息

Nanoformulation Research Lab., Faculty of Pharmacy, Hamdard University, New Delhi, India.

Department of Mechanical Engineering, IIT Kanpur, Uttar Pradesh, India.

出版信息

Carbohydr Polym. 2016 Oct 20;151:546-556. doi: 10.1016/j.carbpol.2016.05.102. Epub 2016 May 29.

Abstract

Chondroitin-4-sulfate (CS), a glycosaminoglycan, was used to prepare CS-capped super-paramagnetic iron oxide nanoparticles, which were further employed for loading a water-soluble chemotherapeutic agent (doxorubicin hydrochloride, DOX). CS-capped SPIONs have potential biomedical application in cancer targeting. The optimized formulation had a hydrodynamic size of 91.2±0.8nm (PDI; 0.228±0.004) and zeta potential of -49.1±1.66mV. DOX was loaded onto the formulation up to 2% (w/w) by physical interaction with CS. TEM showed nano-sized particles having a core-shell structure. XRD confirmed crystal phase of iron oxide. FT-IR conceived the interaction of iron oxide with CS as bidentate chelation and also confirmed DOX loading. Vibration sample magnetometry confirmed super-paramagnetic nature of nanoparticles, with saturation magnetization of 0.238emug(-1). In vitro release profile at pH 7.4 showed that 96.67% of DOX was released within 24h (first order kinetics). MTT assay in MCF7 cells showed significantly higher (p<0.0001) cytotoxicity for DOX in SPIONs than DOX solution (IC50 values 6.294±0.4169 and 11.316±0.1102μgmL(-1), respectively).

摘要

硫酸软骨素-4-硫酸盐(CS)是一种糖胺聚糖,用于制备 CS 封端的超顺磁性氧化铁纳米粒子,进一步用于负载水溶性化疗药物(盐酸多柔比星,DOX)。CS 封端的 SPION 在癌症靶向方面具有潜在的生物医学应用。优化的配方具有 91.2±0.8nm(PDI;0.228±0.004)的水动力粒径和-49.1±1.66mV 的 zeta 电位。通过与 CS 的物理相互作用,将 DOX 负载到配方中,最大载药量可达 2%(w/w)。TEM 显示具有核壳结构的纳米颗粒。XRD 证实了氧化铁的晶体相。FT-IR 推断了氧化铁与 CS 的相互作用为双齿螯合,也证实了 DOX 的负载。振动样品磁强计证实了纳米粒子的超顺磁性质,饱和磁化强度为 0.238 emu/g。在 pH 7.4 下的体外释放曲线表明,96.67%的 DOX 在 24 小时内释放(一级动力学)。在 MCF7 细胞中的 MTT 测定表明,SPION 中的 DOX 比 DOX 溶液具有显著更高的细胞毒性(IC50 值分别为 6.294±0.4169 和 11.316±0.1102μg/mL)(p<0.0001)。

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