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定制化碳量子点的海藻酸钙水凝胶用于 pH 响应型万古霉素控释。

Carbon quantum dot tailored calcium alginate hydrogel for pH responsive controlled delivery of vancomycin.

机构信息

Department of Chemistry, Veer Surendra Sai University of Technology, Burla, Sambalpur 768018, Odisha, India.

Department of Chemistry, Veer Surendra Sai University of Technology, Burla, Sambalpur 768018, Odisha, India.

出版信息

Eur J Pharm Sci. 2017 Nov 15;109:359-371. doi: 10.1016/j.ejps.2017.08.015. Epub 2017 Aug 15.

Abstract

Herein, we demonstrate the preparation of highly luminescent carbon quantum dots (CQDs) from Aloe vera leaf gel; in just 2h at 250°C through carbonization pathway. The prepared CQDs are structurally characterized with high resolution transmission electron microscopy (HRTEM), hydrodynamic diameter, surface polarity, Fourier transform infrared spectroscopy (FTIR), X-ray photoelectron spectroscopy (XPS), Raman, UV-visible absorption spectrophotometry and fluorescence spectroscopy. The functional carbon nanoparticles are observed as non-cytotoxic materials. The biocompatibility, less cytotoxicity and high aqueous dispersibility of as-synthesized CQDs are motivated to design carbon quantum dot (CQD) tailored calcium alginate (CA) hydrogel films with an aim to controlled delivery of glycopeptides antibiotic vancomycin in the gastrointestinal tract (GI). With CQD, the drug loading capacity of CA/CQD film is increased to 89% from 38% (CA film), whereas; with β-cyclodextrin (β-CD) the vancomycin uptake capacity is increased more, 96%. The release of vancomycin through CA/CQD film is more pronounced at pH1.5, close to the pH of the stomach and it is found that in pH1.5 with β-CD, the release rate of vancomycin is lowered, 56% in 120h. The high drug uptake capacity (96%) and lower release rate (56% in 120h) of CA/CQD hydrogel film in pH1.5 with β-CD can be used for its applicability as drug delivery vehicle for controlled release of vancomycin into the stomach region and therefore it can offer a potential option for oral administration of vancomycin.

摘要

在此,我们展示了一种从库拉索芦荟叶凝胶中通过碳化途径在 250°C 下仅 2 小时即可制备高发光碳量子点(CQD)的方法。所制备的 CQD 通过高分辨率透射电子显微镜(HRTEM)、水动力直径、表面极性、傅里叶变换红外光谱(FTIR)、X 射线光电子能谱(XPS)、拉曼、紫外-可见吸收分光光度法和荧光光谱法进行结构表征。这些功能性碳纳米粒子被观察为非细胞毒性材料。所合成的 CQD 的生物相容性、低细胞毒性和高水分散性促使我们设计了碳量子点(CQD)定制的海藻酸钠(CA)水凝胶薄膜,以在胃肠道(GI)中控制糖肽抗生素万古霉素的递送。通过 CQD,CA/CQD 薄膜的药物载药量从 CA 薄膜的 38%增加到 89%,而β-环糊精(β-CD)则使万古霉素的摄取量增加更多,达到 96%。通过 CA/CQD 薄膜在 pH1.5 下更明显地释放万古霉素,接近胃的 pH 值,并且发现在 pH1.5 下与β-CD 一起,万古霉素的释放率降低,120 小时内降低了 56%。CA/CQD 水凝胶薄膜在 pH1.5 下具有β-CD 时的高药物摄取能力(96%)和较低的释放率(120 小时内 56%)可用于其作为药物输送载体的适用性,以控制万古霉素在胃区的释放,因此可为口服万古霉素提供一种潜在选择。

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