Novel protein-loaded chondroitin sulfate-chitosan nanoparticles: preparation and characterization.

ABSTRACT

In this study, the potential of chondroitin sulfate (ChS)-chitosan (CS) nanoparticles (NPs) for the delivery of proteins was investigated. ChS-CS NPs were prepared by ionic cross-linking of CS solution with ChS. The aggregation line, particle size and zeta potential were investigated as a function of the pH, weight ratio and concentration. The water content and formation yield of the NPs were measured by gravimetry. Results indicated that ChS-CS NPs showed a higher degree of ionic cross-linking and formation yield than sodium tripolyphosphate-CS NPs. Fluorescein isothiocyanate conjugate bovine serum albumin (FITC-BSA), a model protein drug, was incorporated into the ChS-CS NPs. The encapsulation efficiency was obviously increased with the increase in initial FITC-BSA concentration and was as high as 90%. In vitro release studies of ChS-CS NPs showed a small burst effect following a continued and controlled release. Cytotoxicity tests with Caco-2 cells showed no toxic effects of ChS-CS NPs. The ex vivo cellular uptake studies using Caco-2 and HEK-293 cells indicated that NPs were found to be endocytosed into the cells. In conclusion, ChS-CS NPs are a potential new delivery system for the transport of hydrophilic compounds such as proteins.