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基于点击反应的树枝状β-环糊精主表面合成及其作为药物纳米载体的应用。

Synthesis of the dendritic type β-cyclodextrin on primary face via click reaction applicable as drug nanocarrier.

机构信息

Laboratory of Dendrimers and Nano-Biopolymers, Faculty of Chemistry, University of Tabriz, Tabriz, Iran.

Laboratory of Dendrimers and Nano-Biopolymers, Faculty of Chemistry, University of Tabriz, Tabriz, Iran; Research Center for Pharmaceutical Nanotechnology (RCPN), Tabriz University of Medical Science, Tabriz, Iran.

出版信息

Carbohydr Polym. 2015 Nov 5;132:205-13. doi: 10.1016/j.carbpol.2015.05.087. Epub 2015 Jun 23.

DOI:10.1016/j.carbpol.2015.05.087
PMID:26256342
Abstract

The objective of this study was the syntheses of well-defined glycodendrimer with entrapment efficiency by click reactions, with β-cyclodextrins (β-CDs) moiety to keep the biocompatibility properties, besides especially increase their capacity to load numerous appropriate sized guests. The original dendrimer containing β-CD in both periphery and central was synthesized using click reaction. The entrapment property of the β-CD-dendrimer was studied by methotrexate (MTX) drug. The chemical structure of β-CD-dendrimer was characterized by (1)H NMR, (13)C NMR and FTIR and its inclusion complex structure were investigated by SEM, DLS, DSC and FTIR techniques. The cytotoxic effect of obtained compound and its inclusion complex with MTX was analyzed using MTT test. The MTT test exhibited that the synthesized compound was not cytotoxic to the cell line considered. The in vitro drug release study turned out that the obtained β-CD dendrimer could be a suitable controlled drug delivery system for cancer treatment.

摘要

本研究的目的是通过点击反应合成具有包封效率的、结构明确的糖苷树枝状聚合物,利用β-环糊精(β-CDs)部分保持其生物相容性,此外还特别提高其负载大量合适大小客体的能力。使用点击反应合成了同时含有β-CD 的外围和中心的原始树枝状聚合物。通过甲氨蝶呤(MTX)药物研究了β-CD-树枝状聚合物的包封性能。通过 1H NMR、13C NMR 和 FTIR 对 β-CD-树枝状聚合物的化学结构进行了表征,并通过 SEM、DLS、DSC 和 FTIR 技术研究了其包合物结构。采用 MTT 试验分析了所得化合物及其与 MTX 的包合物的细胞毒性作用。MTT 试验表明,所合成的化合物对所考虑的细胞系没有细胞毒性。体外药物释放研究表明,所得的β-CD 树枝状聚合物可能是用于癌症治疗的合适的控释药物递送系统。

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