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果胶和海藻酸锌:用于核壳药物递送系统的理想内外聚合物组合。

Pectin and Zinc Alginate: The Right Inner/Outer Polymer Combination for Core-Shell Drug Delivery Systems.

作者信息

Auriemma Giulia, Cerciello Andrea, Aquino Rita P, Gaudio Pasquale Del, Fusco Bruno M, Russo Paola

机构信息

Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, I-84084 Fisciano (SA), Italy.

出版信息

Pharmaceutics. 2020 Jan 21;12(2):87. doi: 10.3390/pharmaceutics12020087.

Abstract

Core-shell beads loaded with betamethasone were developed using co-axial prilling as production technique and pectin plus alginate as polymeric carriers. During this study, many operative conditions were intensively investigated to find the best ones necessary to produce uniform core-shell particle systems in a reproducible way. Particularly, feed solutions' composition, polymers mass ratios and the effect of the main process parameters on particles production, micromeritics, inner structure, drug loading and drug-release/swelling profiles in simulated biological fluids were studied. The optimized core-shell formulation F5 produced with a pectin core concentration of 4.0% and an alginate shell concentration of 2.0% (2:1 core:shell ratio) acted as a sustained drug delivery system. It was able to reduce the early release of the drug in the upper part of the gastro-intestinal tract for the presence of the zinc-alginate gastro-resistant outer layer and to specifically deliver it in the colon, thanks to the selectivity of amidated low methoxy pectin core for this district. Therefore, these particles may be proposed as colon targeted drug delivery systems useful for inflammatory bowel disease (IBD) therapy.

摘要

采用同轴造粒技术,以果胶和海藻酸钠作为聚合物载体,制备了负载倍他米松的核壳微球。在本研究中,深入研究了许多操作条件,以找到以可重复方式生产均匀核壳颗粒系统所需的最佳条件。特别地,研究了进料溶液的组成、聚合物质量比以及主要工艺参数对颗粒生产、粉体学性质、内部结构、载药量以及在模拟生物流体中的药物释放/溶胀曲线的影响。优化后的核壳制剂F5,果胶核浓度为4.0%,海藻酸钠壳浓度为2.0%(核:壳比例为2:1),作为一种缓释给药系统。由于存在海藻酸锌抗胃外层,它能够减少药物在胃肠道上部的早期释放,并由于酰胺化低甲氧基果胶核对此区域的选择性,能够将药物特异性地递送至结肠。因此,这些颗粒可被用作治疗炎症性肠病(IBD)的结肠靶向给药系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/638f/7076462/66c98a1071e7/pharmaceutics-12-00087-g001.jpg

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