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

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.

Keywords: Colon-specific drug delivery; Colonic enzyme; Microflora; Multi-particulate; Pectin.

Publication types

  • Review

MeSH terms

  • Colon
  • Drug Carriers
  • Drug Delivery Systems*
  • Ecosystem
  • Pectins*

Substances

  • Drug Carriers
  • Pectins