Improved anti-proliferative effect of doxorubicin-containing polymer nanoparticles upon surface modification with cationic groupsElectronic supplementary information (ESI) available: General descriptions of materials and instrumentation, characterization data for the monomers and polymers, data from control experiments, and additional data as referenced in the text. See DOI: 10.1039/c2jm35420a

• Main Authors: Krovi, Sai Archana, Swindell, Elden P, O'Halloran, Thomas V, Nguyen, SonBinh T
• Format: Article
• Language: English
• ISSN: 0959-9428; 1364-5501
• DOI: 10.1039/c2jm35420a

Polymer nanoparticles (PNPs) possessing a high density of drug payload have been successfully stabilized against aggregation in biological buffers after amine modification, which renders these PNPs positively charged. The resulting charge-stabilized PNPs retain their original narrow particle size distributions and well-defined spherical morphologies. This stabilization allows these PNPs to have an improved anti-proliferative effect on MDA-MB-231-Br human breast cancer cells compared to non-functionalized PNPs. As a non-cytotoxic control, similar surface-modified PNPs containing cholesterol in place of doxorubicin did not inhibit cell proliferation, indicating that the induced cytotoxic response was solely due to the doxorubicin release from the PNPs. Cationic functionalization stabilizes doxorubicin-containing polymer nanoparticles against aggregation and improved their anti-proliferative effect against MDA-MB-231-Br cancer cells.