Mesalazine/hydroxypropyl-β-cyclodextrin/chitosan nanoparticles with sustained release and enhanced anti-inflammation activity

This study aimed to develop a novel sustained release system for mesalazine (MSZ) by preparing hydroxypropyl-beta-cyclodextrin (HP-beta-CD) inclusion complex loaded chitosan (CS) nanoparticles (NPs). The HP-beta-CD/MSZ complex was prepared at 1:1 stoichiometry and characterized by using various analysis techniques. The HP-beta-CD/MSZ/CS NPs prepared under the optimum condition had a spherical shape (90 +/- 17 nm diameter), a narrow size distribution, and a high loading efficiency. Compared with free MSZ, the HP-beta-CD/MSZ/CS NPs exhibited an obvious sustained release of MSZ. The activity of the NPs against a cytokine-triggered inflammatory response was evaluated in cytokine-stimulated HT-29 cell lines by monitoring key inflammatory mediators. The results revealed that compared with free MSZ, the NPs more strongly inhibited the production of NO, PGE2, and IL-8, indicating the NPs possibly had better anti-inflammatory effects. Therefore, the established HP-beta-CD/MSZ/CS NPs may be a promising delivery system of MSZ.