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叶酸功能化还原响应性磁性壳聚糖纳米胶囊用于药物的靶向递送和触发释放。

Folic acid functionalized reduction-responsive magnetic chitosan nanocapsules for targeted delivery and triggered release of drugs.

机构信息

College of Resources and Environment, Jilin Agricultural University, Changchun 130118, China.

School of Chemistry and Molecular Engineering, Nanjing Tech University, 30 Puzhu Road, Nanjing 211816, China.

出版信息

Carbohydr Polym. 2017 Jul 15;168:282-289. doi: 10.1016/j.carbpol.2017.03.083. Epub 2017 Mar 29.

DOI:10.1016/j.carbpol.2017.03.083
PMID:28457451
Abstract

A versatile folic acid (FA)-functionalized reduction-responsive magnetic chitosan (CS) nanocapsules (FA-RMCNCs) were designed and fabricated successfully from FA-functionalized thiolated chitosan with a simple sonochemical method. The targeting molecule (FA), red fluorescent probes (Rhodamine B isothiocyanate, RITC) and thiolated FeO magnetic nanoparticles (FeO-SH MNPs) were immobilized in and onto the shells of nanocapsules. The as-synthesized FA-RMCNCs had a well-defined spherical morphology with the size of 200-350nm. As the carriers, FA-RMCNCs showed an excellent magnetic responsive property. The CLSM analysis revealed that the proposed FA-RMCNCs with core-shell constructure could be internalized selectively by the HeLa cells through the folate-mediated endocytosis. Moreover, the reductant-triggered release of coumarin 6 suggested that the FA-RMCNCs possessed superior reduction-responsivity of drug release. This study reveals the potential of FA-RMCNCs as magnetic/reduction dual-responsive, folate-receptor-mediated targeting nanocarriers in targeted delivery and controlled release of hydrophobic drugs.

摘要

一种多功能叶酸(FA)功能化还原响应磁性壳聚糖(CS)纳米胶囊(FA-RMCNCs)是通过 FA 功能化的巯基化壳聚糖与简单的超声化学方法成功设计和制备的。靶向分子(FA)、红色荧光探针(异硫氰酸罗丹明 B,RITC)和巯基化 FeO 磁性纳米颗粒(FeO-SH MNPs)被固定在纳米胶囊的壳中。所合成的 FA-RMCNCs 具有定义良好的球形形态,尺寸为 200-350nm。作为载体,FA-RMCNCs 表现出优异的磁响应性能。CLSM 分析表明,具有核壳结构的所提出的 FA-RMCNCs 可以通过叶酸介导的内吞作用被 HeLa 细胞选择性内化。此外,香豆素 6 的还原剂触发释放表明 FA-RMCNCs 具有优越的还原响应性药物释放。这项研究揭示了 FA-RMCNCs 作为磁性/还原双重响应、叶酸受体介导靶向纳米载体在疏水性药物靶向递送和控制释放中的潜力。

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