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基于果胶的多颗粒载体用于治疗剂的结肠定位释放。

Pectin based multi-particulate carriers for colon-specific delivery of therapeutic agents.

机构信息

Takasago International Corporation, 5 Sunview Road, Singapore 627616, Singapore.

出版信息

Int J Pharm. 2021 Aug 10;605:120814. doi: 10.1016/j.ijpharm.2021.120814. Epub 2021 Jun 17.

Abstract

In case of colon-specific delivery of therapeutic agents through oral route, microbial/enzyme-triggered release approach has several advantages over other approaches due to unique microbial ecosystem in the colon. Multiple-unit carriers have an edge over single-unit carriers for this purpose. Among different materials/polymers explored, pectin appears as a promising biopolymer to construct microbial-triggered colon-specific carriers. Pectin is specifically degraded by colonic enzymes but insusceptible to upper gastro-intestinal enzymes. In this article, utilization of pectin solely or in combination with other polymers and/or colonic-delivery approaches is critically discussed in detail in the context of multi-particulate systems. Several studies showed that pectin-based carriers can prevent the release of payload in the stomach but start to release in the intestine. Hence, pectin alone may construct delayed release formulation but may not be sufficient for effective colon-targeting. On the other hand, combination of pectin with other materials/polymers (e.g., chitosan and Eudragit® S-100) has demonstrated huge promise for colon-specific release of payload. Hence, smartly designed pectin-based multi-particulate carriers, especially in combination with other polymers and/or colon-targeting approaches (e.g., microbial-triggered + pH-triggered or microbial-triggered + pH-triggered + time-release or microbial-triggered + pH-triggered + pressure-based), can be successful colon-specific delivery systems. However, more clinical trials are necessary to bring this idea from bench to bedside.

摘要

在通过口服途径将治疗剂递送到结肠特异性的情况下,由于结肠中存在独特的微生物生态系统,微生物/酶触发释放方法相对于其他方法具有多个优势。多单位载体在这方面优于单单位载体。在探索的不同材料/聚合物中,果胶作为构建微生物触发结肠特异性载体的有前途的生物聚合物出现。果胶可被结肠酶特异性降解,但不易被上胃肠道酶降解。在本文中,将详细讨论果胶单独或与其他聚合物和/或结肠递药方法结合使用在多颗粒系统中的情况。多项研究表明,基于果胶的载体可以防止载药在胃中释放,但开始在肠道中释放。因此,果胶本身可以构建延迟释放制剂,但可能不足以实现有效的结肠靶向。另一方面,果胶与其他材料/聚合物(例如壳聚糖和 Eudragit® S-100)的组合已显示出在载药结肠特异性释放方面具有巨大的潜力。因此,精心设计的基于果胶的多颗粒载体,特别是与其他聚合物和/或结肠靶向方法(例如,微生物触发+pH 触发或微生物触发+pH 触发+定时释放或微生物触发+pH 触发+压力释放)相结合,可以成为成功的结肠特异性给药系统。然而,需要更多的临床试验将这一想法从实验室推向临床。

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