Colon-Targeted Oral Drug Delivery Systems: Design Trends and Approaches

Abstract

Abstract. Colon-specific drug delivery systems (CDDS) are desirable for the treatment of a range of local diseases such as ulcerative colitis, Crohn's disease, irritable bowel syndrome, chronic pancreatitis, and colonic cancer. In addition, the colon can be a potential site for the systemic absorption of several drugs to treat non-colonic conditions. Drugs such as proteins and peptides that are known to degrade in the extreme gastric pH, if delivered to the colon intact, can be systemically absorbed by colonic mucosa. In order to achieve effective therapeutic outcomes, it is imperative that the designed delivery system specifically targets the drugs into the colon. Several formulation approaches have been explored in the development colon-targeted drug delivery systems. These approaches involve the use of formulation components that interact with one or more aspects of gastrointestinal (GI) physiology, such as the difference in the pH along the GI tract, the presence of colonic microflora, and enzymes, to achieve colon targeting. This article highlights the factors influencing colon-specific drug delivery and colonic bioavailability, and the limitations associated with CDDS. Further, the review provides a systematic discussion of various conventional, as well as relatively newer formulation approaches/technologies currently being utilized for the development of CDDS.

Can colorectal delivery technology provide a platform for enteral oligonucleotide-based therapeutics?

“…Our systemic delivery technique for nucleic acids via the large intestine not only has the potential to be developed into a drug for use as an enema or suppository, but could also be developed into an oral drug, taking advantage of a colonic drug delivery system (18)(19)(20). Thus, this colorectal delivery technique may provide a new foundation for the development of oligonucleotide-based oral therapeutics.…”

A review on novel approaches for colon targeted drug delivery systems

“…Peristaltic motion causes the luminal pressure of the large intestine to increase more than that of the small intestine because its contents are more viscous due to the reabsorption of water. Several studies have been carried out to utilize the colonic luminal pressure to pressure to develop colon-specific drug delivery systems (S. Amidon et al, 2015). the pressure controlled drug delivery system consists of a capsule in which the drug is present.…”

“…Like crohn's disease, colonic cancer ulcerative Colitis, amebiosis and many others disorders ( (Anil and Betty, 2010). Colon targeted drug delivery system is not only the suitable for delivering the drug to the colon for local treatment but it is also a preferable approach for delivery of protein and peptide and enhance their bioavailability (Amidon et al, 2015). Bioavailability of protein and peptide may be achieved if it can be protected from acid and enzymes in the stomach and upper intestine and released and absorbed in the colon and protect it form degradation in stomach (Prasanth et al, 2012).…”

Formulation of Tetrandrine Beads Using Ionic Gelation Method Ca-Pectinate Coated Ph-Sensitive Polymers as Colon-Targeted Dosage Form

“…This pH-sensitive polymer can tolerate dissolution in the gastric acid environment; however, it can be dissolved in a higher pH in the intestine. This pH-sensitive polymer can be split in ileum terminal pH, thus providing a targeted drug delivery to the colon [4]. Several examples of pH-sensitive polymer which commonly used for colon targeted drug delivery were methacrylate polymer in acid-base, known as Eudragit.…”