Abstract
Colon targeted drug delivery systems have gained a great deal of attention as potential carriers for the local treatment of colonic diseases with reduced systemic side effects and also for the enhanced oral delivery of various therapeutics vulnerable to acidic and enzymatic degradation in the upper gastrointestinal tract. In recent years, the global pharmaceutical market for biologics has grown, and increasing demand for a more patient-friendly drug administration system highlights the importance of colonic drug delivery as a noninvasive delivery approach for macromolecules. Colon-targeted drug delivery systems for macromolecules can provide therapeutic benefits including better patient compliance (because they are pain-free and can be self-administered) and lower costs. Therefore, to achieve more efficient colonic drug delivery for local or systemic drug effects, various strategies have been explored including pH-dependent systems, enzyme-triggered systems, receptor-mediated systems, and magnetically-driven systems. In this review, recent advancements in various approaches for designing colon targeted drug delivery systems and their pharmaceutical applications are covered with a particular emphasis on formulation technologies.
Highlights
In the past few decades, the prevalence of colonic diseases has increased worldwide, demanding the effective local treatment of colonic diseases for more efficacious and safer drug therapies
The dynamic pH change by many internal and external factors may attenuate the efficiency of pH-dependent drug release systems, often leading to poorly site-selective drug release
Zhang et al [42] prepared folate-modified Self-microemulsifying drug delivery system (SMEDDS) (FSMEDDS) containing curcumin, which were filled into soft capsules coated with Eudragit® S 100. This curcumin-loaded FSMEDDS formulation efficiently bound to folate receptors on colon cancer cells. These results demonstrated that colon-targeted FSMEDDS capsules are a viable means through which curcumin can be delivered to the colon [42]
Summary
In the past few decades, the prevalence of colonic diseases has increased worldwide, demanding the effective local treatment of colonic diseases for more efficacious and safer drug therapies. For the local treatment of colonic diseases, colon-targeted drug delivery systems have been actively pursued since conventional non-targeted therapy may have undesirable side-effects and low efficacy due to the systemic absorption of drug before reaching the target site [4,5]. It is imperative to consider the physiological properties of the colon and the microenvironment surrounding disease site(s) for the successful development of colon-targeted drug delivery systems. Given that the pathophysiological changes in the microenvironment surrounding disease sites should be considered during formulation development, various formulation approaches have been explored to optimize the colonic drug delivery, including pH-sensitive systems, enzyme-triggered systems, and magnetically-driven systems. This review covers recent advancements in various formulation approaches in designing colon-targeted drug delivery systems and their pharmaceutical applications
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