Department of Pharmaceutical Sciences, Rangel College of Pharmacy, Texas A&M University, Kingsville, TX 78363, USA.
Division of Gastroenterology and Hepatology, Department of Medicine, University of Missouri, Columbia, MO 65212, USA.
Int J Biol Macromol. 2020 Dec 15;165(Pt A):722-737. doi: 10.1016/j.ijbiomac.2020.09.214. Epub 2020 Oct 1.
Treatments for inflammatory bowel disease (IBD) are typically immunosuppressive. Despite a range of treatment options, limited efficacy, systemic toxicities like bone marrow suppression, infections and malignancy are their serious setbacks. There exists an unmet medical need for novel therapeutic agents without safety concerns resulting from chronic, systemic immunosuppression. Of late, several natural agents with better therapeutic potential have been reported. It is very likely that restricting the release of the active molecules to the intestine would further improve their clinical efficacy and safety. To this end, novel polymer-based micro/nano formulations protect the drug from gastric environment and slowly release the drug in the colon. However, cost and side-effects associated to synthetic polymers have led to the development of biocompatible, economic and pharmaceutically well-accepted biomacromolecules in exploring their potential in IBD. Since last few years, biological proteins, polysaccharides and their combinations have shown great efficacy in colitis induced animal models. In this review, micro/nano formulations developed using biomacromolecules like chitosan, zein, pectin, casein, alginate, dextran, glucomannan and hyaluronic acid have been reviewed focusing on their potential in protecting active cargo, avoiding premature release, distal colon targeting along with their impact on reshaping the altered gut microbiota and how it can ameliorate the colitis conditions.
治疗炎症性肠病（IBD）的方法通常是免疫抑制性的。尽管有一系列的治疗选择，但疗效有限，骨髓抑制、感染和恶性肿瘤等全身毒性是它们的严重缺点。因此，需要寻找没有慢性、系统性免疫抑制相关安全问题的新型治疗药物。最近，已经报道了一些具有更好治疗潜力的天然药物。将活性分子的释放限制在肠道内，很可能会进一步提高它们的临床疗效和安全性。为此，新型基于聚合物的微/纳米制剂可以保护药物免受胃酸环境的影响，并在结肠中缓慢释放药物。然而，与合成聚合物相关的成本和副作用促使人们在探索其在 IBD 中的潜力时，开发了生物相容性、经济实惠且被广泛接受的生物大分子。在过去的几年中，生物蛋白、多糖及其组合在诱导结肠炎的动物模型中表现出了很好的疗效。在这篇综述中，我们回顾了使用壳聚糖、玉米醇溶蛋白、果胶、酪蛋白、藻酸盐、葡聚糖、魔芋葡甘露聚糖和透明质酸等生物大分子开发的微/纳米制剂，重点关注它们在保护有效载荷、避免过早释放、靶向远端结肠以及重塑改变的肠道微生物群方面的潜力，以及它们如何改善结肠炎的情况。
