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壳聚糖的药物应用。

Pharmaceutical applications of chitosan.

机构信息

Department of Chemistry, Amirkabir University of Technology (Tehran Polytechnic), P.O.Box: 15875-4413, Tehran, Iran.

出版信息

Adv Colloid Interface Sci. 2019 Jan;263:131-194. doi: 10.1016/j.cis.2018.11.008. Epub 2018 Nov 30.

Abstract

Chitosan (CS) is a linear polysaccharide which is achieved by deacetylation of chitin, which is the second most plentiful compound in nature, after cellulose. It is a linear copolymer of β-(1 → 4)-linked 2-acetamido-2-deoxy-β-d-glucopyranose and 2-amino-2-deoxy-β-d-glucopyranose. It has appreciated properties such as biocompatibility, biodegradability, hydrophilicity, nontoxicity, high bioavailability, simplicity of modification, favorable permselectivity of water, outstanding chemical resistance, capability to form films, gels, nanoparticles, microparticles and beads as well as affinity to metals, proteins and dyes. Also, the biodegradable CS is broken down in the human body to safe compounds (amino sugars) which are easily absorbed. At present, CS and its derivatives are broadly investigated in numerous pharmaceutical and medical applications including drug/gene delivery, wound dressings, implants, contact lenses, tissue engineering and cell encapsulation. Besides, CS has several OH and NH functional groups which allow protein binding. CS with a deacetylation degree of ~50% is soluble in aqueous acidic environment. While CS is dissolved in acidic medium, its amino groups in the polymeric chains are protonated and it becomes cationic which allows its strong interaction with different kinds of molecules. It is believed that this positive charge is responsible for the antimicrobial activity of CS through the interaction with the negatively charged cell membranes of microorganisms. This review presents properties and numerous applications of chitosan-based compounds in drug delivery, gene delivery, cell encapsulation, protein binding, tissue engineering, preparation of implants and contact lenses, wound healing, bioimaging, antimicrobial food additives, antibacterial food packaging materials and antibacterial textiles. Moreover, some recent molecular dynamics simulations accomplished on the pharmaceutical applications of chitosan were presented.

摘要

壳聚糖(CS)是一种线性多糖,通过脱乙酰化甲壳素获得,甲壳素是仅次于纤维素的自然界中第二丰富的化合物。它是β-(1→4)-连接的 2-乙酰氨基-2-脱氧-β-d-吡喃葡萄糖和 2-氨基-2-脱氧-β-d-吡喃葡萄糖的线性共聚物。它具有生物相容性、可生物降解性、亲水性、无毒、高生物利用度、修饰简单、水的良好选择透过性、优异的耐化学性、成膜、凝胶、纳米粒子、微球和珠粒的形成能力以及对金属、蛋白质和染料的亲和力等优点。此外,可生物降解的 CS 在人体内分解为安全的化合物(氨基糖),这些化合物很容易被吸收。目前,CS 及其衍生物在许多药物和医学应用中得到广泛研究,包括药物/基因传递、伤口敷料、植入物、隐形眼镜、组织工程和细胞封装。此外,CS 具有几个 OH 和 NH 官能团,允许与蛋白质结合。脱乙酰度约为 50%的 CS 在酸性水性环境中是可溶的。当 CS 在酸性介质中溶解时,其聚合物链上的氨基被质子化,变成阳离子,使其与不同种类的分子发生强烈相互作用。人们认为,这种正电荷通过与微生物的带负电荷的细胞膜相互作用,是 CS 具有抗菌活性的原因。本文综述了基于壳聚糖的化合物在药物传递、基因传递、细胞封装、蛋白质结合、组织工程、植入物和隐形眼镜制备、伤口愈合、生物成像、抗菌食品添加剂、抗菌食品包装材料和抗菌纺织品中的应用。此外,还介绍了一些最近在壳聚糖药物应用方面完成的分子动力学模拟。

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