Development of Colon Targeting Tablet of a JAK Inhibitor to Combat Chronic Ulcerative Colitis: A Novel Approach for Local Drug Delivery

The colon specific drug delivery system is gaining importance not only for local drug delivery of drugs but also for the systemic delivery of protein & peptide drugs. Colon was considered as black-box as most of the drugs are absorbed from upper part of the GI tract. Colon targeting was aimed mainly because of less enzymatic activity and longer transit time. It also has drawbacks like less water content and presence of fecal content. To achieve successful colon targeted drug delivery, a drug needs to be protected from degradation, release and absorption in the upper portion of the GI tract and then to be ensured controlled release in the proximal colon. The various approaches that can be exploited to target the release of drug to the colon including formulation approaches through pH sensitive system are microbial triggered systems i.e., prodrugs and polysaccharide based system, timed release system, osmotically controlled drug system, pressure dependent release system, programmed pulsatile release system and others.

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Oral colon-targeting core–shell microparticles loading curcumin for enhanced ulcerative colitis alleviating efficacy

Chinese Medicine ◽

10.1186/s13020-021-00449-8 ◽

2021 ◽

Vol 16 (1) ◽

Author(s):

Chen Zhang ◽

Zhejie Chen ◽

Yanan He ◽

Jing Xian ◽

Ruifeng Luo ◽

...

Keyword(s):

Ulcerative Colitis ◽

Drug Delivery ◽

Gastrointestinal Tract ◽

Fluorescence Imaging ◽

Experimental Colitis ◽

Core Shell ◽

Colon Targeting ◽

Targeting Efficiency ◽

Imaging Test ◽

Accumulation Capacity

Abstract Background The oral colon-targeting drug delivery vehicle is vital for the efficient application of curcumin (Cur) in ulcerative colitis (UC) treatment because of its lipophilicity and instability in the gastrointestinal tract. Methods The core–shell microparticle (MP) system composed of eco-friendly materials, zein and shellac, was fabricated using a coaxial electrospray technique. In this manner, Cur was loaded in the zein core, with shellac shell coating on it. The colon-targeting efficiency and accumulation capacity of shellac@Cur/zein MPs were evaluated using a fluorescence imaging test. The treatment effects of free Cur, Cur/zein MPs, and shellac@Cur/zein MPs in acute experimental colitis were compared. Results With the process parameters optimized, shellac@Cur/zein MPs were facilely fabricated with a stable cone-jet mode, exhibiting standard spherical shape, uniform size distribution (2.84 ± 0.15 µm), and high encapsulation efficiency (95.97% ± 3.51%). Particularly, with the protection of shellac@zein MPs, Cur exhibited sustained drug release in the simulated gastrointestinal tract. Additionally, the in vivo fluorescence imaging test indicated that the cargo loaded in shellac@zein MPs improves the colon-targeting efficiency and accumulation capacity at the colonitis site. More importantly, compared with either free Cur or Cur/zein MPs, the continuous oral administration of shellac@Cur/zein MPs for a week could efficiently inhibit inflammation in acute experimental colitis. Conclusion The shellac@Cur/zein MPs would act as an effective oral drug delivery system for UC management.

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