Design of alpha mangostin-loaded chitosan/alginate controlled-release nanoparticles using genipin as crosslinker

Abstract

α–Mangostin-loaded chitosan/alginate (CS/ALG) nanoparticles cross-linked with genipin (GP) were prepared for oral controlled drug release. A full factorial design was conducted to investigate the effects of the needle gauge, stirring rate and α–mangostin loading on the size of the nanoparticles. In order to provide controlled release, the nanoparticles were modified by crosslinking with GP, and the physical and chemical characteristics of the obtained systems were studied by FT-IR, PXRD and DSC. The α–mangostin loading and release was investigated, and the antitumour activity of nanoparticles was demonstrated. The results showed that small nanoparticles were obtained by maximising needle gauge and stirring rate and minimising the α–mangostin loading. A high α–mangostin loading and insignificantly larger particle size were observed with GP cross-linked nanoparticles. Moreover, GP nanoparticles acted as drug carriers sustaining α–mangostin release, which was slower at acidic pH compared to higher pH. These patterns were beneficial for α–mangostin release in the colon. Moreover, α–mangostin loaded GP nanoparticles exhibited antitumour activity against the colorectal cancer cells. These results suggest that GP nanoparticles could possibly be a good candidate for oral controlled release drug delivery to colon.