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Folic acid linked amino-cellulose for in vitro evaluation of doxorubicin delivery: Synthesis and characterization

机译:叶酸连接的氨基纤维素体外评估阿霉素的递送:合成与表征

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In this study, cellulose, a biodegradable polymer, was successfully aminated. For this purpose the cellulose was converted to a bromoacetylated derivative by reaction with bromoacetyl bromide. The resulting bromide derivative was then substituted with azido groups by reaction with sodium azide. Then the azido group was reduced to amines via the formation of the triphenylphosphinimine intermediate followed by hydrolysis using aqueous hydrazine. This sequence produced amino-cellulose. To gain a tumor-targeting doxorubicin (DOX) delivery system, we conjugated an active tumor-targeting ligand, folic acid, to the end of the resulting copolymer (FA-Amino-Cell). The structure of this copolymer was confirmed by FT-IR, UV-Vis, TGA, SEM, and H-1 NMR spectroscopy. The SEM images showed that the hydrodynamic dimension of the resulted product is about 40 nm. Moreover, the Release profiles of DOX from the FA-Amino-Cell and its loading capacity were determined by UV-Vis absorption measurement at lambda(max) 483 nm. The results showed that the DOX loaded copolymer had good control on the release period of DOX. So, it seems that the FA-Amino-Cell is a potential candidate for the targeted delivery of DOX for cancer treatment.
机译:在这项研究中,纤维素,一种可生物降解的聚合物,被成功胺化。为此目的,通过与溴乙酰溴反应,将纤维素转化为溴乙酰化衍生物。然后通过与叠氮化钠反应,将所得的溴化物衍生物用叠氮基取代。然后通过形成三苯基膦亚胺中间体将叠氮基还原为胺,然后使用肼水溶液进行水解。该序列产生氨基纤维素。为了获得靶向肿瘤的阿霉素(DOX)递送系统,我们将活性靶向肿瘤的配体叶酸与所得共聚物(FA-Amino-Cell)的末端缀合。该共聚物的结构通过FT-IR,UV-Vis,TGA,SEM和H-1 NMR光谱确认。 SEM图像显示所得产物的流体动力学尺寸为约40nm。此外,通过在λ(max)483 nm处的UV-Vis吸收测量来确定DOX从FA-氨基细胞的释放曲线及其负载能力。结果表明,负载有DOX的共聚物对DOX的释放时间具有良好的控制作用。因此,似乎FA-氨基细胞是针对癌症治疗的DOX靶向递送的潜在候选者。

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