结肠药物靶向天然多糖的特性

Abhishek Kumar, Amit Pandey.K, M. Koshy
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引用次数: 0

摘要

直接将药物靶向到结肠有利于局部治疗结肠疾病,如溃疡性结肠炎和克罗恩病,并且在获得多肽和其他不稳定药物的口服递送方面显示出潜力。需要一个结肠给药系统来保护药物通过上胃肠道并允许其在结肠中释放。结肠靶向的几种方法已经被提出。这些包括利用小肠运输时间的明显一致性,利用胃肠道内pH值的变化以及利用胃肠道结肠区域的细菌酶。在实现靶向药物释放到结肠的不同方法中,使用聚合物特别是结肠细菌可生物降解的聚合物具有很大的前景。多糖是一种细菌酶,有足够的数量用于结肠靶向药物。基于这种方法,研究了多种多糖的结肠特异性药物释放。这些多糖包括果胶、瓜尔胶、直链淀粉、菊糖、葡聚糖、壳聚糖和硫酸软骨素。这种天然聚合物家族对药物递送具有吸引力,因为它由具有大量衍生基团的聚合物组成,分子量范围广,化学成分不同,并且在大多数情况下具有低毒性和生物降解性但高稳定性。这些材料最有利的特性是它们被批准作为药用辅料。多糖是细菌酶,有足够的数量来降解这些天然多糖。
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Characteristics of Natural Polysaccharides for Colon Drug Targeting
Targeting drugs directly to the colon is advantageous in the topical treatment of colonic diseases such as ulcerative colitis and Crohn’s disease and has shown potential in gaining the oral delivery of peptides and other labile drugs. A colonic drug delivery system is required to protect a drug during its transit through the upper gastro-intestinal (G.I.T.) tract and allow its release in the colon. Several methods of colonic targeting have been proposed. These include taking advantage of the apparent consistency of small intestinal transit times, the utilization of pH changes within the G.I. tract and the exploitation of bacterial enzymes localized in the colonic region of the G.I. tract. Among the different approaches to achieve targeted drug release to the colon, the use of polymers especially biodegradable by colonic bacteria holds great promise. Polysaccharides are bacterial enzymes that are available in sufficient quantity to be exploited in colon targeting of drugs. Based on this approach, various polysaccharides have been investigated for colon-specific drug release. These polysaccharides include pectin, guar gum, amylose, inulin, dextran, chitosan, and chondroitin sulfate. This family of natural polymers has an appeal to drug delivery as it is comprised of polymers with a large number of derivatizable groups, a wide range of molecular weights, varying chemical compositions, and, for the most part, low toxicity and biodegradability yet high stability. The most favorable property of these materials is their approval as pharmaceutical excipients. Polysaccharides are bacterial enzymes that are available in sufficient quantity to degrade these natural polysaccharides.
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