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用纳米纤维素增强的抗淀粉/果胶自立膜用于结肠甲氨蝶呤释放。

Resistant starch/pectin free-standing films reinforced with nanocellulose intended for colonic methotrexate release.

机构信息

Interdisciplinary Laboratory of Advanced Materials, Centro de Ciências da Natureza - CNN, Universidade Federal do Piauí - UFPI, 64049-550 Teresina, PI, Brazil; Universidade de Araraquara - UNIARA, 14801-320 Araraquara, SP, Brazil.

Department of Drugs and Pharmaceuticals, Faculty of Pharmaceutical Sciences, São Paulo State University-UNESP, 14800-903 Araraquara, SP, Brazil.

出版信息

Carbohydr Polym. 2017 Feb 10;157:1013-1023. doi: 10.1016/j.carbpol.2016.10.062. Epub 2016 Oct 21.

Abstract

Although resistant starch/pectin (RS/P) films have previously displayed suitable properties for colon-specific drug delivery, nanocomposite films were developed aiming to enhance physicochemical, thermal, mechanical and barrier properties, as well as the low oral bioavailability of methotrexate (MTX). FEG-SEM micrographs of nanocomposite films showed different interaction patterns occurring among nanocellulose and RS/P. The nanofiller addition led to an increase in the thermal stability, probably due to its interaction with RS crystalline double helices. Results also displayed an improvement of the puncture strength, while barrier properties revealed a low water vapor permeability. Ex vivo bioadhesion test displayed the nanocomposites films to interact strongly with porcine gastrointestinal mucosa. In vitro drug release studies showed that the films developed enhanced the drug dissolution rates with approximately 80% of MTX release in 150min, suggesting the potential of these materials as a poor solubility drugs carrier, which constitutes an important tool for enhancing oral bioavailability.

摘要

虽然抗性淀粉/果胶(RS/P)薄膜以前显示出适合结肠特异性药物传递的特性,但开发了纳米复合材料薄膜,旨在增强物理化学、热学、机械和阻隔性能,以及甲氨蝶呤(MTX)的低口服生物利用度。纳米复合材料薄膜的 FEG-SEM 显微照片显示了纳米纤维素和 RS/P 之间发生的不同相互作用模式。纳米填料的添加导致热稳定性提高,这可能是由于其与 RS 结晶双螺旋的相互作用。结果还显示穿刺强度提高,而阻隔性能显示水蒸气透过率低。离体生物黏附试验显示纳米复合材料薄膜与猪胃肠道黏膜强烈相互作用。体外药物释放研究表明,所开发的薄膜增强了药物的溶解速率,约 80%的 MTX 在 150 分钟内释放,这表明这些材料作为一种低溶解度药物载体的潜力,这是提高口服生物利用度的重要工具。

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