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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Layered gadolinium hydroxides for simultaneous drug delivery and imaging
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Layered gadolinium hydroxides for simultaneous drug delivery and imaging

机译:分层氢氧化物同时药物递送和成像

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The potential of the layered gadolinium hydroxide (LGdH) [Gd-2(OH)(5)]Cl center dot yH(2)O (LGdH-Cl) for simultaneous drug delivery and magnetic resonance imaging was explored in this work. Three non-steroidal anti-inflammatory drugs (diclofenac [dic], ibuprofen [ibu], and naproxen [nap]) were intercalated into LGdH-Cl for the first time, using three different routes (ion exchange intercalation, coprecipitation, and exfoliation-self-assembly). X-ray diffraction, elemental microanalysis and IR spectroscopy confirmed successful incorporation of the drug into the interlayer spaces of the LGdH in all cases. From a comparison of the guest anion sizes and interlayer spacings, the active ingredients are believed to adopt intertwined bilayer configurations between the LGdH layers. The materials prepared by coprecipitation in general have noticeably higher drug loadings than those produced by ion exchange or self-assembly, as a result of the incorporation of some neutral drug into the composites. The LGdH-drug intercalates are stable at neutral pH, but rapidly degrade in acidic conditions to free Gd3+ into solution. While LGdH-nap releases its drug loading into solution very rapidly (within ca. 1.5 h) at pH 7.4, LGdH-dic shows sustained release over 4 h, and LGdH-ibu extends this to 24 h. The latter composites therefore can be incorporated into enteric-coated tablets to provide sustained release in the small intestine. The drug intercalates are highly biocompatible and retain the proton relaxivity properties of the parent LGdH-Cl, with the materials most promising for use as negative contrast agents in MRI. Overall, the LGdH-drug intercalation compounds appear to have great potential for use in theranostic applications.
机译:在这项工作中探讨了同时药物递送和磁共振成像的层状氢氧化钆(LGDH)[GD-2(OH)[GD-2(OH)] CL中心点YH(2)O(LGDH-CL)的电位。使用三种不同的途径(离子交换嵌入,共沉淀和去角质,第一次将三种非甾体抗炎药(双氯氟乙烯[DIC],布洛芬[DIC],布洛芬[IBU]和萘普酮[NAP])嵌入到LGDH-CL中。自组装)。 X射线衍射,元素微分析和IR光谱证实,在所有情况下,将药物的成功掺入LGDH的中间空间。根据客观阴离子尺寸和层间间距的比较,据信,活性成分在LGDH层之间采用交织的双层配置。由于将一些中性药物掺入复合材料中,由共沉淀制备的材料通常具有比通过离子交换或自组装产生的药物负荷更高。 LGDH-药物嵌入在中性pH下是稳定的,但在酸性条件下迅速降解到游离Gd3 +进入溶液中。虽然LGDH-NAP在pH 7.4的pH 7.4的迅速(在约1.5h)中释放其药物负载,但LGDH-DIC显示超过4小时的持续释放,并且LGDH-IBU将其延伸至24小时。因此,后一种复合材料可以掺入肠溶包衣片中,以在小肠中提供持续释放。药物插入物高度相容,并保留亲本LGDH-CL的质子松弛性质,其材料最有希望用作MRI中的负造影剂。总的来说,LGDH-药物嵌入化合物似乎具有很大的用途潜力。

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