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黏附性微复合材料:壳聚糖包覆的海泡石纳米管用于持续药物输送。

Mucoadhesive micro-composites: Chitosan coated halloysite nanotubes for sustained drug delivery.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University, Multan, 60000, Pakistan.

Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University, Multan, 60000, Pakistan; Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.

出版信息

Colloids Surf B Biointerfaces. 2019 Dec 1;184:110527. doi: 10.1016/j.colsurfb.2019.110527. Epub 2019 Sep 24.

Abstract

It was aim of this study to synthesize micro-composites comprising halloysite nanotubes (HNTs) and the cationic polymer chitosan as mucoadhesive sustained release drug delivery system. Micro-composites were characterized for preparation yield, size, micromeritic properties and swelling behavior. Chemical composition of micro-composites was characterized by FTIR, XRD and TGA. Scanning electron microscopy (SEM) was used to study their surface morphology. Micro-composites were studied for adhesion on intestinal mucosa as well as for release behavior of metoclopramide hydrochloride used as model drug. Preparation yield was found to be in the range of 35.14 ± 1.5-53.97 ± 5.23%. Micro-composites exhibited a mean size range of 0.151 ± 0.49 μm. SEM showed a spherical shape with rough curved porous surface. Micro-composites exhibited excellent flowability and maximum swelling at acidic pH. XRD results showed crystalline nature of micro-composites. HNTs/micro-composites with highest concentration of chitosan displayed maximum adherence of 89 ± 1.79% on intestinal mucosa after 3 h. Drug release recorded was 66.8% at pH 1.2 and 46.7% at pH 5.5 within 25 h. Chitosan coated HNTs showed remarkable mucoadhesion and sustained release of metoclopramide proving their suitability as mucoadhesive drug delivery system.

摘要

本研究旨在合成包含埃洛石纳米管(HNTs)和阳离子聚合物壳聚糖的微复合材料,作为一种具有黏膜黏附性的缓释药物传递系统。对微复合材料的制备产率、粒径、微粉学性质和溶胀行为进行了表征。通过傅里叶变换红外光谱(FTIR)、X 射线衍射(XRD)和热重分析(TGA)对微复合材料的化学组成进行了表征。扫描电子显微镜(SEM)用于研究其表面形态。研究了微复合材料对肠黏膜的黏附性以及作为模型药物的盐酸甲氧氯普胺的释放行为。制备产率在 35.14±1.5-53.97±5.23%的范围内。微复合材料的平均粒径范围为 0.151±0.49μm。SEM 显示出球形形状,具有粗糙弯曲的多孔表面。微复合材料在酸性 pH 值下表现出优异的流动性和最大的溶胀性。XRD 结果表明微复合材料具有结晶性质。壳聚糖浓度最高的 HNTs/微复合材料在 3 小时后对肠黏膜的黏附率最高,达到 89±1.79%。在 pH 值为 1.2 时,药物释放记录为 66.8%,在 pH 值为 5.5 时,在 25 小时内释放 46.7%。壳聚糖包覆的 HNTs 表现出显著的黏膜黏附性和盐酸甲氧氯普胺的持续释放,证明其适合作为黏膜黏附性药物传递系统。

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