Phenylboronic acid-conjugated chitosan nanoparticles for high loading and efficient delivery of curcumin

In order to achieve high loading and efficient delivery of curcumin, phenylboronic acid-conjugated chitosan nanoparticles were prepared by a simple desolvation method. These nanoparticles exhibited a regular spherical shape with the average size about 200−230 nm and narrow size distribution, which were kinetically stable under physiological condition. Due to boronate ester formation between curcumin and phenylboronic acid groups in the nanoparticles, and the hydrogen bonding interactions between curcumin and nanocarriers, curcumin was successfully loaded into the nanoparticles with high drug loading content. These curcumin-loaded nanoparticles showed pH and reactive oxygen species (ROS)-triggered drug release behavior. In vitro cell experiments revealed that the blank nanoparticles were completely nontoxic to cultured cells, and the curcumin-loaded nanoparticles exhibited efficient antitumor efficiency against cancer cells. Moreover, the drug-loaded nanoparticles performed an enhanced growth inhibition in three-dimensional multicellular tumor spheroids. Thus, these nanocarriers would be a promising candidate for curcumin delivery in tumor treatment.