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Bioinspired Silica Offers a Novel, Green, and Biocompatible Alternative to Traditional Drug Delivery Systems

机译:Bioinspired silica为传统的药物传递系统提供了一种新颖的,绿色的和生物相容的替代品

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摘要

Development of drug delivery systems (DDS) is essential in many cases to remedy the limitations of free drug molecules. Silica has been of great interest as a DDS due to being more robust and versatile than other types of DDS (e.g., liposomes). Using ibuprofen as a model drug, we investigated bioinspired silica (BIS) as a new DDS and compared it to mesoporous silica (MS); the latter has received much attention for drug delivery applications. BIS is synthesized under benign conditions without the use of hazardous chemicals, which enables controllable in situ loading of drugs by carefully designing the DDS formulation conditions. Here, we systematically studied these conditions (e.g., chemistry, concentration, and pH) to understand BIS as a DDS and further achieve high loading and release of ibuprofen. Drug loading into BIS could be enhanced (up to 70%) by increasing the concentration of the bioinspired additive. Increasing the silicate concentration increased the release to 50%. Finally, acidic synthesis conditions could raise loading efficiency to 62% while also increasing the total mass of drug released. By identifying ideal formulation conditions for BIS, we produced a DDS that was able to release fivefold more drug per weight of silica when compared with MCM-41. Biocompatibility of BIS was also investigated, and it was found that, although ∼20% of BIS was able to pass through the gut wall into the bloodstream, it was nonhemolytic (∼2% hemolysis at 500 μg mL–1) when compared to MS (10% hemolysis at the same concentration). Overall, for DDS, it is clear that BIS has several advantages over MS (ease of synthesis, controllability, and lack of hazardous chemicals) as well as being less toxic, making BIS a real potentially viable green alternative to DDS.
机译:在许多情况下,开发药物输送系统(DDS)对于纠正游离药物分子的局限性至关重要。二氧化硅由于比其他类型的DDS(例如脂质体)更坚固和通用,因此作为DDS引起了极大的兴趣。我们使用布洛芬作为模型药物,研究了生物启发二氧化硅(BIS)作为新的DDS,并将其与中孔二氧化硅(MS)进行了比较;后者在药物递送应用中受到了广泛关注。 BIS是在良性条件下合成的,无需使用有害化学物质,这可以通过精心设计DDS配方条件来实现可控的原位装载药物。在这里,我们系统地研究了这些条件(例如化学性质,浓度和pH),以将BIS理解为DDS,并进一步实现了布洛芬的高负载和释放。可以通过增加生物启发性添加剂的浓度来增加BIS中的药物装载量(最多70%)。硅酸盐浓度的增加将释放增加到50%。最后,酸性合成条件可以将负载效率提高到62%,同时还可以增加释放的药物的总质量。通过确定BIS的理想配方条件,我们生产了DDS,与MCM-41相比,该DDS能够释放每单位重量二氧化硅多五倍的药物。还对BIS的生物相容性进行了研究,结果发现,尽管〜20%的BIS能够通过肠壁进入血液,但与MS相比它是非溶血性的(在500μgmL–1时溶血率为2%)。 (在相同浓度下溶血率为10%)。总体而言,对于DDS,很明显,BIS具有优于MS的多项优势(易于合成,可控制性和不含有害化学物质),并且毒性较低,这使BIS成为DDS的真正可行的绿色替代品。

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