Preparation and characterization of amphiphilic nanoparticles based on chondroitin sulfate A conjugated with hydrophobic drug for enhanced doxorubicin delivery

Novel chondroitin sulfate A conjugated doxorubicin (CSA-DOX) was synthesized and characterized. The mean diameter of CSA-DOX was 152 nm analyzed by dynamic light scattering (DLS). Further, DOX was physically encapsulated into the CSA-DOX nanoparticles. Total amounts of DOX in three kinds of DOX-loaded CSA-DOX (CSA-DOX/DOX) nanoparticles were from 21.8 to 24.2%. The mean diameters of three CSA-DOX/DOX nanoparticles were in the range of 167-177 nm. The shape of CSA-DOX/DOX nanoparticles was almost spherical. DOX released from DOX-loaded nanoparticles exhibited a biphasic way in phosphate buffered saline (PBS, pH 7.4). Cellular uptake studies exhibited that CSA-DOX and CSA-DOX/DOX nanoparticles could enhance the uptake of DOX into CD44 receptor-positive A549 cells. Moreover, the cytotoxicity of CSA-DOX/DOX nanoparticles against A549 cells significantly improved in contrast with free DOX and CSA-DOX nanoparticles. These results suggested that CSA-DOX copolymer could be a potential carrier for antitumor drug delivery.

Automated summary

A novel chondroitin sulfate A conjugated doxorubicin (CSA-DOX) was synthesized and characterized, with a mean diameter of 152 nm. The CSA-DOX/DOX nanoparticles exhibited enhanced cellular uptake of DOX into CD44 receptor-positive A549 cells, leading to significant cytotoxicity improvement against the cells.Results indicated that CSA-DOX copolymer could be a potential carrier for antitumor drug delivery.