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用于治疗炎症性肠病的结肠靶向壳聚糖基多单位药物传递系统的研究进展。

Advances in the colon-targeted chitosan based multiunit drug delivery systems for the treatment of inflammatory bowel disease.

机构信息

Department of Pharmaceutics, R. C. Patel Institute of Pharmaceutical Education and Research, Karwand Naka, Shirpur, 425405, Dist. Dhule, Maharashtra, India.

Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Delhi Pharmaceutical Sciences and Research University (DPSRU-Govt. of NCT Delhi), Mehrauli-Badarpur Road, Pushp Vihar Sector 3, New Delhi, 110017, India.

出版信息

Carbohydr Polym. 2022 Jul 15;288:119351. doi: 10.1016/j.carbpol.2022.119351. Epub 2022 Mar 14.

DOI:10.1016/j.carbpol.2022.119351
PMID:35450623
Abstract

Chitosan is the polymer of choice for delivery of the active moieties to the colon due to its cationic nature that enables strong mucosal attachment. Chitosan is explored for formulations such as pellets, beads, microspheres, nanoparticles and drug-polymer conjugates for colon targeting of various therapeutic agents in inflammatory bowel disease (IBD). The major challenge in the colonic delivery of drugs in IBD is altered physiological pH, which can be addressed via chitosan containing multiparticulate drug delivery systems owing to their biodegradability in the colon. Its ionic interaction with anionic polymers forms gastro-resistant multi-unit systems that ensures safe delivery of payloads to the colon. In contrast to commercial grade gastro-resistant polymers, chitosan has GRAS (generally regarded as safe) status that ensures safety for long-term therapy in case of chronic diseases such as IBD. Here, we review in detail essential properties of chitosan and chitosan based multiunit formulations for treatment/mitigation of IBD.

摘要

壳聚糖由于其阳离子性质,能够与黏膜强烈结合,成为递送至结肠的首选聚合物。壳聚糖被探索用于各种制剂,如微球、纳米粒和药物-聚合物偶联物,以实现治疗炎症性肠病(IBD)的各种治疗药物的结肠靶向。在 IBD 中,药物结肠递释的主要挑战是生理 pH 的改变,这可以通过含有壳聚糖的多颗粒药物递释系统来解决,因为它们在结肠中具有生物降解性。其与阴离子聚合物的离子相互作用形成胃耐多单位系统,确保将有效载荷安全递送至结肠。与商业级胃耐聚合物相比,壳聚糖具有 GRAS(一般认为安全)地位,确保在治疗慢性疾病(如 IBD)时长期治疗的安全性。在这里,我们详细综述了壳聚糖及其基于壳聚糖的多单位制剂在治疗/缓解 IBD 方面的重要性质。

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