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

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 mu m), 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.

Automated summary

The study developed a core-shell microparticle system composed of eco-friendly materials, with Cur loaded in the core and shellac coating on the surface, showing high efficiency in colon-targeting drug delivery. In the treatment of acute experimental colitis, the shellac@Cur/zein MPs demonstrated better anti-inflammatory effects compared to free Cur or Cur/zein MPs.