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载酮康唑赖氨酸的核/壳纤维素基微球口服给药。

Core/shell cellulose-based microspheres for oral administration of Ketoprofen Lysinate.

机构信息

Department of Chemical Sciences & Materials Technology, Institute for Polymers, Composites and Biomaterials, National Research Council of Italy, 80125, Naples, Italy.

IMAST SCaRL, Piazza Bovio 22, 80133, Naples, Italy.

出版信息

J Biomed Mater Res B Appl Biomater. 2018 Oct;106(7):2636-2644. doi: 10.1002/jbm.b.34080. Epub 2018 Jan 26.

Abstract

Herein, we propose the fabrication of a new carrier with core/shell structure-inner core of cellulose acetate (CA) coated by a micrometric layer of chitosan (CS)-fabricated through an integrated process, which combines Electro Dynamic Atomization (EDA) and layer-by-layer (LbL) technique. We demonstrate that CA based microspheres possess a unique capability to relevantly retain the drugs-that is, Ketoprofen Lysinate (KL)-along the gastric tract, while providing a massive release along the intestine. CS shell slightly influences the morphology and water retention under different pH conditions, improving drug encapsulation without compromising drug release kinetics. In vitro studies in simulated gastric and intestine fluids (SGF, SIF) with physiological enzymes, show a moderate release of LSK during the first 2 h (ca. 20% at pH 2), followed by a sustained release during the next 6 h (ca. 80% at pH 7). The obtained results demonstrate that CA-based microspheres hold strong potential to be used as carriers for a delayed oral administration of anti-inflammatory drugs. © 2018 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 106B: 2636-2644, 2018.

摘要

在此,我们提出了一种新的载体的制造具有核/壳结构的内芯醋酸纤维素(CA)通过一个集成的过程,它结合了静电动态雾化(EDA)和层层(LbL)技术涂有壳聚糖(CS)的微米层。我们证明,基于 CA 的微球具有独特的能力,以保持相关药物 - 即赖氨酸酮洛芬(KL) - 沿胃肠道,同时沿肠道提供大量释放。CS 壳在不同 pH 条件下对形态和保水能力略有影响,在不影响药物释放动力学的情况下提高药物包封率。在模拟胃液和肠液(SGF,SIF)中进行的体外研究具有生理酶,表明 LSK 在最初的 2 小时内(pH2 时约 20%)适度释放,随后在接下来的 6 小时内持续释放(pH7 时约 80%)。所得结果表明,基于 CA 的微球具有作为延迟口服抗炎药物载体的强大潜力。©2018 年威利父子公司。生物医学材料研究杂志 B:应用生物材料,106B:2636-2644,2018 年。

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