Oral Drug Delivery Systems for Ulcerative Colitis Therapy: A Comparative Study with Microparticles and Nanoparticles.

BACKGROUND: Oral administrations of microparticles (MPs) and nanoparticles (NPs) have been widely explored as therapeutic approaches for treatment of ulcerative colitis (UC). However, no previous study has comparatively investigated the therapeutic efficacy of MPs and NPs.

METHODS: In this study, curcumin (CUR)-loaded MPs (CUR-MPs) and CUR-loaded NPs (CUR-NPs) were fabricated using an emulsion-solvent evaporation method. Their therapeutic efficacies against UC were comparatively studied.

RESULTS: The resultant spherical MPs and NPs exhibited slightly negative zeta-potential with mean particle diameters of approximately 1.7 μm and 270 nm, respectively. We found that NPs exhibited a much higher CUR release rate than MPs within the same period of investigation. In vivo experiments demonstrated that oral administration of CUR-MPs and CUR-NPs reduced the symptoms of inflammation in a UC mouse model induced by dextran sulfate sodium. Importantly, CUR-NPs showed a higher therapeutic efficacy in alleviating colitis in comparison to CUR-MPs.

CONCLUSION: NPs can improve the anti-inflammation activity of CUR by enhancing the drug release and cellular uptake efficiency compared to MPs. Thus, it is a promising and a readily scalable drug vehicle for efficient clinical treatment of UC.